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Journal articles on the topic 'Potent anti-cancer agent'

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Author: Grafiati
Published: 6 September 2023

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1

Bhat, Smitha S., Shashanka K. Prasad, Chandan Shivamallu, Kollur Shiva Prasad, Asad Syed, Pruthvish Reddy, Charley A. Cull, and Raghavendra G. Amachawadi. "Genistein: A Potent Anti-Breast Cancer Agent." Current Issues in Molecular Biology 43, no. 3 (October 10, 2021): 1502–17. http://dx.doi.org/10.3390/cimb43030106.

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Genistein is an isoflavonoid present in high quantities in soybeans. Possessing a wide range of bioactives, it is being studied extensively for its tumoricidal effects. Investigations into mechanisms of the anti-cancer activity have revealed many pathways including induction of cell proliferation, suppression of tyrosine kinases, regulation of Hedgehog-Gli1 signaling, modulation of epigenetic activities, seizing of cell cycle and Akt and MEK signaling pathways, among others via which the cancer cell proliferation can be controlled. Notwithstanding, the observed activities have been time- and dose-dependent. In addition, genistein has also shown varying results in women depending on the physiological parameters, such as the early or post-menopausal states.
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2

Ibrahim, Mona, Donia Wafaa, and Ghada El Nady. "Ginger Extract as Potent Anti-Cancer Agent against Breast Cancer." Journal of Agricultural Chemistry and Biotechnology 13, no. 12 (December 1, 2022): 139–43. http://dx.doi.org/10.21608/jacb.2023.183821.1042.

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3

SAXENA, B., L. ZHU, M. HAO, E. KISILIS, M. KATDARE, O. OKTEM, A. BOMSHTEYN, and P. RATHNAM. "Boc-lysinated-betulonic acid: A potent, anti-prostate cancer agent." Bioorganic & Medicinal Chemistry 14, no. 18 (September 15, 2006): 6349–58. http://dx.doi.org/10.1016/j.bmc.2006.05.048.

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4

Samuel, Samson, Elizabeth Varghese, Peter Kubatka, Chris Triggle, and Dietrich Büsselberg. "Metformin: The Answer to Cancer in a Flower? Current Knowledge and Future Prospects of Metformin as an Anti-Cancer Agent in Breast Cancer." Biomolecules 9, no. 12 (December 9, 2019): 846. http://dx.doi.org/10.3390/biom9120846.

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Interest has grown in studying the possible use of well-known anti-diabetic drugs as anti-cancer agents individually or in combination with, frequently used, chemotherapeutic agents and/or radiation, owing to the fact that diabetes heightens the risk, incidence, and rapid progression of cancers, including breast cancer, in an individual. In this regard, metformin (1, 1-dimethylbiguanide), well known as ‘Glucophage’ among diabetics, was reported to be cancer preventive while also being a potent anti-proliferative and anti-cancer agent. While meta-analysis studies reported a lower risk and incidence of breast cancer among diabetic individuals on a metformin treatment regimen, several in vitro, pre-clinical, and clinical studies reported the efficacy of using metformin individually as an anti-cancer/anti-tumor agent or in combination with chemotherapeutic drugs or radiation in the treatment of different forms of breast cancer. However, unanswered questions remain with regards to areas such as cancer treatment specific therapeutic dosing of metformin, specificity to cancer cells at high concentrations, resistance to metformin therapy, efficacy of combinatory therapeutic approaches, post-therapeutic relapse of the disease, and efficacy in cancer prevention in non-diabetic individuals. In the current article, we discuss the biology of metformin and its molecular mechanism of action, the existing cellular, pre-clinical, and clinical studies that have tested the anti-tumor potential of metformin as a potential anti-cancer/anti-tumor agent in breast cancer therapy, and outline the future prospects and directions for a better understanding and re-purposing of metformin as an anti-cancer drug in the treatment of breast cancer.
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Purushottamachar, Puranik, Aakanksha Khandelwal, Tadas S. Vasaitis, Robert D. Bruno, Lalji K. Gediya, and Vincent C. O. Njar. "Potent anti-prostate cancer agents derived from a novel androgen receptor down-regulating agent." Bioorganic & Medicinal Chemistry 16, no. 7 (April 1, 2008): 3519–29. http://dx.doi.org/10.1016/j.bmc.2008.02.031.

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Sameem, Bilqees, Ebrahim Saeedian Moghadam, Majid Darabi, Zahra Shahsavari, and Mohsen Amini. "Triarylpyrazole Derivatives as Potent Cytotoxic Agents; Synthesis and Bioactivity Evaluation “Pyrazole Derivatives as Anticancer Agent”." Drug Research 71, no. 07 (May 19, 2021): 388–94. http://dx.doi.org/10.1055/a-1498-1714.

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Abstract Background During the last recent years, several anti-cancer agents were introduced for the treatment of diverse kinds of cancer. Despite their potential in the treatment of cancer, drug resistance and adverse toxicity such as peripheral neuropathy are some of the negative criteria of anti-cancer agents and for this reason, the design and synthesis of new anti-cancer agents are important. Objective Design, synthesis, and anticancer activity evaluation of some pyrazole derivatives. Methods A series of Target compounds were prepared using multistep synthesis. Their cytotoxic activity against three different human cancer cell lines namely human colon carcinoma cells (HT-29), epithelial carcinoma cells (U-87MG), pancreatic cancerous cells (Panc-1) as well as AGO1522 normal cell line using in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was investigated. Results 1,3-Diaryl-5-(3,4,5-trimethoxyphenyl)-4,5-dihydro-1H-pyrazole and 1,3-Diaryl-5-(3,4,5-trimethoxyphenyl)- 1H-pyrazole were synthesized in good yields and their structure and purity were confirmed using 1H-NMR, 13C-NMR, and elemental analysis. Generally, the synthesized scaffolds exhibited good cytotoxicity against cancerous cell lines in comparison to the reference standard, paclitaxel. Compounds 3a and 3c, in Annexin V/ PI staining assay, exerted remarkable activity in apoptosis induction in HT-29 cell lines. Both of them also led to cell cycle arrest in the sub-G1 phase which is inconsistent with the results of apoptosis assay. Conclusion Concerning obtained results, it is interesting to synthesis more pyrazole derivatives as anticancer agents.
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7

Watanabe, Coran M. H., Lubica Supekova, and Peter G. Schultz. "Transcriptional Effects of the Potent Enediyne Anti-Cancer Agent Calicheamicin γ1I." Chemistry & Biology 9, no. 2 (February 2002): 245–51. http://dx.doi.org/10.1016/s1074-5521(02)00103-5.

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8

Tundis, Rosa, Jayanta Kumar Patra, Marco Bonesi, Subrata Das, Rajat Nath, Anupam Das Talukdar, Gitishree Das, and Monica Rosa Loizzo. "Anti-Cancer Agent: The Labdane Diterpenoid-Andrographolide." Plants 12, no. 10 (May 12, 2023): 1969. http://dx.doi.org/10.3390/plants12101969.

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In spite of the progress in treatment strategies, cancer remains a major cause of death worldwide. Therefore, the main challenge should be the early diagnosis of cancer and the design of an optimal therapeutic strategy to increase the patient’s life expectancy as well as the continuation of the search for increasingly active and selective molecules for the treatment of different forms of cancer. In the recent decades, research in the field of natural compounds has increasingly shifted towards advanced and molecular level understandings, thus leading to the development of potent anti-cancer agents. Among them is the diterpene lactone andrographolide, isolated from Andrographis paniculata (Burm.f.) Wall. ex Nees that showed shows a plethora of biological activities, including not only anti-cancer activity, but also anti-inflammatory, anti-viral, anti-bacterial, neuroprotective, hepatoprotective, hypoglycemic, and immunomodulatory properties. Andrographolide has been shown to act as an anti-tumor drug by affecting specific molecular targets that play a part in the development and progression of several cancer types including breast, lung, colon, renal, and cervical cancer, as well as leukemia and hepatocarcinoma. This review comprehensively and systematically summarized the current research on the potential anti-cancer properties of andrographolide highlighting its mechanisms of action, pharmacokinetics, and potential side effects and discussing the future perspectives, challenges, and limitations of use.
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Liu, Weiya, Eugene K. Lee, Karim Pirani, Brian S. J. Blagg, and Jeffrey M. Holzbeierlein. "A new HSP90 inhibitor as therapeutic agent for bladder cancer." Journal of Clinical Oncology 35, no. 6_suppl (February 20, 2017): 416. http://dx.doi.org/10.1200/jco.2017.35.6_suppl.416.

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416 Background: Hsp90 represents one of the most promising biological targets for the treatment of cancer, including bladder cancer. A number of Hsp90 inhibitors that target the N-terminal ATP-binding pocket have demonstrated potent antiproliferative effects. However, a major drawback is that they induce a prosurvival heat shock response (HSR). We demonstrate the effects of a novel Hsp90 beta selective inhibitor on bladder cancer cells, which shows potent antiproliferative effects without inducing HSR. Methods: Cell Titer-Glo luminescent anti-proliferative assay was used to determine the IC50 numbers in UC3 cells. Trypan Blue Cytotoxicity assay was performed for 24h treatment with increasing concentrations of the inhibitor. Effects of the cmpound on Hsp90’s client protein degradation were investigated by Western Blot. Results: This new compound exhibits potent anti-proliferative in bladder cancer cells. IC50 number is determined as 0.30 µM for UC3 cancer cells. The toxicity assay was also performed over UC3 cells at 24h.1uM KU new compound has the similar effects on UC3 cells as 10 uM 17AAG: inhibit the cancer cells growth to half, but maintain over 60% viability of the cells. The western blot were also performed over UC3 cells, and some new target proteins such as FGFR3 and PKM2 were investigated. The data showed that, this new compound would not induce the heat shock response like 17AAG (Hsp27), and did cause some Hsp90β related protein degradation (CXCR4). FGFR3, PKM2, Her2, Hsf-1and B-raf all show degradation to different extent. Conclusions: A novel Hsp90 inhibitor, exhibits potent anti-proliferative and cytotoxic activity along with client protein degradation, without induction of HSR in bladder cancer cell lines. The reduction of Hsp90 beta related client protein caused by this compound suggests the potential to develop isoform specific inhibitors of Hsp90 for better antitumor therapies.
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10

Rosenthal, Gerald A. "l-Canaline: A potent antimetabolite and anti-cancer agent from leguminous plants." Life Sciences 60, no. 19 (April 1997): 1635–41. http://dx.doi.org/10.1016/s0024-3205(96)00595-4.

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11

Pardo-Andreu, Gilberto L., Yanier Nuñez-Figueredo, Valeria G. Tudella, Osmany Cuesta-Rubio, Fernando P. Rodrigues, Cezar R. Pestana, Sérgio A. Uyemura, Andréia M. Leopoldino, Luciane C. Alberici, and Carlos Curti. "The anti-cancer agent nemorosone is a new potent protonophoric mitochondrial uncoupler." Mitochondrion 11, no. 2 (March 2011): 255–63. http://dx.doi.org/10.1016/j.mito.2010.10.008.

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12

Ko, Jeong-Hyeon, Frank Arfuso, Gautam Sethi, and Kwang Ahn. "Pharmacological Utilization of Bergamottin, Derived from Grapefruits, in Cancer Prevention and Therapy." International Journal of Molecular Sciences 19, no. 12 (December 14, 2018): 4048. http://dx.doi.org/10.3390/ijms19124048.

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Cancer still remains one of the leading causes of death worldwide. In spite of significant advances in treatment options and the advent of novel targeted therapies, there still remains an unmet need for the identification of novel pharmacological agents for cancer therapy. This has led to several studies evaluating the possible application of natural agents found in vegetables, fruits, or plant-derived products that may be useful for cancer treatment. Bergamottin is a furanocoumarin derived from grapefruits and is also a well-known cytochrome P450 inhibitor. Recent studies have demonstrated potent anti-oxidative, anti-inflammatory, and anti-cancer properties of grapefruit furanocoumarin both in vitro and in vivo. The present review focuses on the potential anti-neoplastic effects of bergamottin in different tumor models and briefly describes the molecular targets affected by this agent.
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Bhutia, Sujit K., Birendra Behera, Durgesh Nandini Das, Subhadip Mukhopadhyay, Niharika Sinha, Prashanta Kumar Panda, Prajna Paramita Naik, et al. "Abrus agglutinin is a potent anti-proliferative and anti-angiogenic agent in human breast cancer." International Journal of Cancer 139, no. 2 (March 30, 2016): 457–66. http://dx.doi.org/10.1002/ijc.30055.

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14

Kothavade, Pankaj S., Dnyaneshwar M. Nagmoti, Vipin D. Bulani, and Archana R. Juvekar. "Arzanol, a Potent mPGES-1 Inhibitor: Novel Anti-Inflammatory Agent." Scientific World Journal 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/986429.

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Arzanol is a novel phloroglucinolα-pyrone, isolated from a Mediterranean plantHelichrysum italicum(Roth) Don ssp.microphyllumwhich belongs to the family Asteraceae. Arzanol has been reported to possess a variety of pharmacological activities. However, anti-inflammatory, anti-HIV, and antioxidant activities have been studied in some detail. Arzanol has been reported to inhibit inflammatory transcription factor NFκB activation, HIV replication in T cells, releases of IL-1β, IL-6, IL-8, and TNF-α, and biosynthesis of PGE2by potentially inhibiting mPGES-1 enzyme. Diversity of mechanisms of actions of arzanol may be useful in treatment of disease involving these inflammatory mediators such as autoimmune diseases and cancer. This review presents comprehensive information on the chemistry, structure-activity relationship, and pharmacological activities of arzanol. In addition this review discusses recent developments and the scope for future research in these aspects.
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15

Dahlem, Charlotte, Wei Xiong Siow, Maria Lopatniuk, William K. F. Tse, Sonja M. Kessler, Susanne H. Kirsch, Jessica Hoppstädter, et al. "Thioholgamide A, a New Anti-Proliferative Anti-Tumor Agent, Modulates Macrophage Polarization and Metabolism." Cancers 12, no. 5 (May 19, 2020): 1288. http://dx.doi.org/10.3390/cancers12051288.

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Natural products represent powerful tools searching for novel anticancer drugs. Thioholgamide A (thioA) is a ribosomally synthesized and post-translationally modified peptide, which has been identified as a product of Streptomyces sp. MUSC 136T. In this study, we provide a comprehensive biological profile of thioA, elucidating its effects on different hallmarks of cancer in tumor cells as well as in macrophages as crucial players of the tumor microenvironment. In 2D and 3D in vitro cell culture models thioA showed potent anti-proliferative activities in cancer cells at nanomolar concentrations. Anti-proliferative actions were confirmed in vivo in zebrafish embryos. Cytotoxicity was only induced at several-fold higher concentrations, as assessed by live-cell microscopy and biochemical analyses. ThioA exhibited a potent modulation of cell metabolism by inhibiting oxidative phosphorylation, as determined in a live-cell metabolic assay platform. The metabolic modulation caused a repolarization of in vitro differentiated and polarized tumor-promoting human monocyte-derived macrophages: ThioA-treated macrophages showed an altered morphology and a modulated expression of genes and surface markers. Taken together, the metabolic regulator thioA revealed low activities in non-tumorigenic cells and an interesting anti-cancer profile by orchestrating different hallmarks of cancer, both in tumor cells as well as in macrophages as part of the tumor microenvironment.
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Raut, Dattatraya G., Sandeep B. Patil, Vikas D. Kadu, Mahesh G. Hublikar, and Raghunath B. Bhosale. "Synthesis of Asymmetric 1-Thiocarbamoyl Pyrazoles as Potent Anti- Colon Cancer, Antioxidant and Anti-Inflammatory Agent." Anti-Cancer Agents in Medicinal Chemistry 18, no. 15 (February 28, 2019): 2117–23. http://dx.doi.org/10.2174/1871520618666181112122528.

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Background: Cancer is one of the leading diseases responsible for deaths in the society. According to the American cancer society, there will be 95,270 new cases of colon cancer in the U.S. in 2016. When a normal cell turns cancerous they develop into tumours, which produce various pro-inflammatory and inflammatory cytokines and chemokines that attract leukocytes to the site of growth. The main aim of this paper is to introduce readers about the increased number of cancer patient, effects of cancer and need of research on same. Methods: The target molecules were prepared by reacting pyrazolealdehyde with appropriate aromatic ketone by using polyethylene glycol (PEG-300) as green solvent and catalyst to yield chalcone. Furthermore, the reaction of chalcones with thiosemicabazide yields asymmetric 1-thiocarbamoyl pyrazoles. All the newly synthesized compounds were in vitro screened for their anticancer activities against Colon SW-620 by employing the sulforhodamine B (SRB) assay method. Also all the synthesized compounds tested for in vitro antioxidant and anti-inflammatory activity by using known literature methods. Results: Preliminary in vitro evaluation indicated that most of the compounds 4c, 4d and 4e possess distinct cytotoxicity profile against Colon SW-620 cell line compared to standard drug adriamycin. All the tested compounds showed good to excellent antioxidant activity against one or more reactive (H2O2, DPPH, SOR and NO) radical scavenging species. Additionally, all the synthesized compounds were screened for their in vitro antiinflammatory activity. Compounds 4a, 4b and 4e shows potent anti-inflammatory activity as compared to diclofenac sodium as a standard reference. Conclusion: New anti- Colon SW-620 cancer agents are the need of time, we trust that 1-thiocarbamoyl pyrazole derivatives 4c, 4d and 4e constitute an interesting template for the evaluation of new anticancer agent also antioxidant and anti-inflammatory work may provide an interesting insight for further development.
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SUN, YUAN-WAN, KUEN-YUAN CHEN, CHUL-HOON KWON, and KUN-MING CHEN. "CK0403, a 9-aminoacridine, is a potent anti-cancer agent in human breast cancer cells." Molecular Medicine Reports 13, no. 1 (November 23, 2015): 933–38. http://dx.doi.org/10.3892/mmr.2015.4604.

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18

Varakumar, Potlapati, Kalirajan Rajagopal, Baliwada Aparna, Kannan Raman, Gowramma Byran, Clara Mariana Gonçalves Lima, Salma Rashid, Mohammed H. Nafady, Talha Bin Emran, and Sławomir Wybraniec. "Acridine as an Anti-Tumour Agent: A Critical Review." Molecules 28, no. 1 (December 26, 2022): 193. http://dx.doi.org/10.3390/molecules28010193.

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This review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines are well-known for their high cytotoxic activity; however, their clinical application is restricted or even excluded as a result of side effects. The photocytotoxicity of propyl acridine acts against leukaemia cell lines, with C1748 being a promising anti-tumour drug against UDP-UGT’s. CK0403 is reported in breast cancer treatment and is more potent than CK0402 against estrogen receptor-negative HER2. Acridine platinum (Pt) complexes have shown specificity on the evaluated DNA sequences; 9-anilinoacridine core, which intercalates DNA, and a methyl triazene DNA-methylating moiety were also studied. Acridine thiourea gold and acridinone derivatives act against cell lines such as MDA-MB-231, SK-BR-3, and MCF-7. Benzimidazole acridine compounds demonstrated cytotoxic activity against Dual Topo and PARP-1. Quinacrine, thiazacridine, and azacridine are reported as anti-cancer agents, which have been reported in the previous decade and were addressed in this review article.
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Kotlarczyk, Kari, Mario Sepulveda, Tong Wang, Maggie Murray, Paul Gonzales, and Stephen Thomas Gately. "Abstract 1359: Selective HDAC6 inhibition by GB-1101 revokes tumor immune privilege and synergizes with immune checkpoint therapies to induce tumor regressions." Cancer Research 82, no. 12_Supplement (June 15, 2022): 1359. http://dx.doi.org/10.1158/1538-7445.am2022-1359.

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Abstract HDAC6 is a cytoplasmic class IIB HDAC isoenzyme that is involved in the deacetylation of cytoplasmic proteins. HDAC6 also binds ubiquitinated proteins, facilitating the formation of the aggresome, to remove misfolded proteins. Previously, HDAC6-selective inhibitors were shown to decrease immunosuppression and enhance immune function of melanoma patient T-cells demonstrating an important role for HDAC6 inhibition for cancer immunotherapy. GB-1101 is a novel, orally bioavailable, nanomolar potent inhibitor of HDAC6. GB-1101 tested in vitro did not induce direct cytotoxicity to CD4+/CD8+ or NK cells at concentrations up to 300 nM. RNA-seq on GB-1101 exposed MHC-null human MSS colon cancer cell lines reveal potent induction of MHC Class I/II genes and expression numerous cancer neoantigens. To test the activity of GB-1101 in vivo, we established large (~450mm3) 4T1-luc syngeneic tumors and initiated treatment of GB-1101 given orally once daily alone and combined with anti-PD1, anti-CTLA4, and anti-PD1/anti-CTLA4 combination. The activity of anti-PD1 in this model was minimal (TGI: 3%); GB-1101 as a single agent showed more potent anti-tumor activity (TGI: 50%) compared to anti-PD1. We observed synergistic benefit when GB-1101 was combined with anti-PD1 (Combination TGI: 78%). GB-1101 showed comparable anti-tumor activity to single agent anti-CTLA4 (TGI: 43%) but revealed significant tumor regressions of large and well-established tumors when combined with anti-CTLA4 (Combination TGI: >100%). As a single agent, GB-1101 was superior to anti-PD1+anti-CTLA4 (TGI: 7%) and induced significant tumor regressions when combined with anti-PD1+anti-CTLA4 (Triple Combination TGI: >100%). In the TC-1, HPV-positive syngeneic model, GB-1101 reprogrammed the tumor immune microenvironment reducing the number of M-MDSC and TReg cells and increase the numbers of CD4+/CD8+ and NK cells. Taken together, these data support GB-1101 as an important new targeted epigenetic immunomodulator able to revoke immune privilege to enhance the clinical activity of immune checkpoint therapies. Citation Format: Kari Kotlarczyk, Mario Sepulveda, Tong Wang, Maggie Murray, Paul Gonzales, Stephen Thomas Gately. Selective HDAC6 inhibition by GB-1101 revokes tumor immune privilege and synergizes with immune checkpoint therapies to induce tumor regressions [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 1359.
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20

Kang, Sung Nam, Eunmyong Lee, Mi-Kyung Lee, and Soo-Jeong Lim. "Preparation and evaluation of tributyrin emulsion as a potent anti-cancer agent against melanoma." Drug Delivery 18, no. 2 (October 14, 2010): 143–49. http://dx.doi.org/10.3109/10717544.2010.522610.

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21

Boichuk, Sergei, Aigul Galembikova, Firuza Bikinieva, Pavel Dunaev, Aida Aukhadieva, Kirill Syuzov, Svetlana Zykova, Nazim Igidov, Alexander Ksenofontov, and Pavel Bocharov. "2-APCAs, the Novel Microtubule Targeting Agents Active against Distinct Cancer Cell Lines." Molecules 26, no. 3 (January 25, 2021): 616. http://dx.doi.org/10.3390/molecules26030616.

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Microtubules are known as the most attractive molecular targets for anti-cancer drugs. However, the number of serious limitations of the microtubule targeting agents (MTAs) including poor bioavailability, adverse effects (e.g., systemic and neural toxicity), and acquired resistance after initiation of MTA-based therapy remain the driving forces to develop the novel therapeutic agents effectively targeting microtubules and exhibiting potent anti-tumor activities. Here, we report the discovery of 2-amino-pyrrole-carboxamides (2-APCAs), a novel class of MTA, which effectively inhibited the growth of the broad spectrum of cancer cell lines in vitro, including various types of breast, prostate, and non-small lung cancer (NSLC), soft tissue sarcomas (STS) (e.g., leio-, rhabdomyo-, and fibrosarcomas), osteosarcomas and gastrointestinal stromal tumors (GISTs). Importantly, 2-APCAs were also effective in cancer cell lines exhibiting resistance to certain chemotherapeutic agents, including MTAs and topoisomerase II inhibitors. The anti-proliferative effect of 2-APCAs was due to their ability to interfere with the polymerization of tubulin and thereby leading to the accumulation of tumor cells in the M-phase. As an outcome of the mitotic arrest, cancer cells underwent apoptotic cell death which was evidenced by increased expression of cleaved forms of the poly-ADP-ribose polymerase (PARP) and caspase-3 and the increased numbers of Annexin V-positive cells, as well. Among the compounds exhibiting the potent anti-cancer activities against the various cancer cell lines indicated above, 2-APCA-III was found the most active. Importantly, its cytotoxic activities correlated with its highest potency to interfere with the dynamics of tubulin polymerization and inducement of cell cycle arrest in the G2/M phase. Interestingly, the cytotoxic and tubulin polymerization activities of 2-APCAs correlated with the stability of the «tubulin—2-АРСА» complexes, illustrating the “tubulin-2-APCA-III” complex as the most stable. Molecular docking showed that the binding site for 2-АРСА-III is located in α tubulin by forming a hydrogen bond with Leu23. Of note, single-cell electrophoresis (Comet assay) data illustrated the low genotoxic activities of 2-APCAs when compared to certain anti-cancer chemotherapeutic agents. Taken together, our study describes the novel MTAs with potent anti-proliferative and pro-apoptotic activities, thereby illustrating them as a scaffold for the development of successful chemotherapeutic anti-cancer agent targeting microtubules.
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Sun, Yunpeng, Chonglin Tao, Fuxiang Yu, Wenjun Yang, Yunfeng Shan, Zhengping Yu, Hongqi Shi, Mengtao Zhou, Qiyu Zhang, and Huanhuan Wu. "Discovery of a novel human lactate dehydrogenase A (LDHA) inhibitor as an anti-proliferation agent against MIA PaCa-2 pancreatic cancer cells." RSC Advances 6, no. 28 (2016): 23218–22. http://dx.doi.org/10.1039/c5ra27736a.

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KIM, Jun Hyun, Joo Hee KIM, Gun Eui Lee, Sang Woong KIM, and I. Kwon CHUNG. "Identification of a quinoxaline derivative that is a potent telomerase inhibitor leading to cellular senescence of human cancer cells." Biochemical Journal 373, no. 2 (July 15, 2003): 523–29. http://dx.doi.org/10.1042/bj20030363.

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Telomere maintenance is essential for the continued proliferation of dividing cells, and is implicated in chromosome stability and cell immortalization. Telomerase activity allows cells to maintain their telomeric DNA and contributes to the indefinite replicative capacity of cancer cells. Telomerase is expressed in most cancer cells, but not in normal somatic cells, suggesting that telomerase is an attractive target for cancer chemotherapy. Here we screened a chemical library for inhibition of human telomerase, and identified 2,3,7-trichloro-5-nitroquinoxaline (TNQX) as a potent inhibitor. TNQX showed a potent inhibitory effect, with 50% inhibition at ~1.4 μM, and did not inhibit DNA and RNA polymerases, including retroviral reverse trancriptase. A series of enzyme kinetic experiments suggested that TNQX is a mixed-type non-competitive inhibitor, with an inhibitor-binding site distinct from the binding sites for the telomeric substrate (TS) primer and the dNTPs. Long-term cultivation of the MCF7 cell line with a drug concentration that did not cause acute cytotoxicity resulted in progressive telomere erosion followed by an increased incidence of chromosome abnormalities and induction of the senescence phenotype. The results presented here indicate that TNQX is a highly potent and selective anti-telomerase agent with good potential for further development as a promising anti-cancer agent.
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Khattak, Shahana, Gul Rehman Elmi, Farah Azhar, Hina Ahsan, Kalsoom Saleem, and Faryal Jahan. "Biological Applications of Magnetic Nanoparticles; A Review." Pharmaceutical Communications 1, no. 01 (December 31, 2022): 07–29. http://dx.doi.org/10.55627/pharma.001.001.0200.

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In nanotechnology field, iron oxide magnetic nanoparticles (IONPs) have gained much interest. The magnetic nanoparticles have been widely explored for applications due to ease of manufacturing and functionalization with polymers and other materials which makes them highly sensitive for many biological and biomedical applications. They transform electromagnetic energy into heat when exposed to magnetic field, and, hence, prove themselves as potent anti-cancer agent. The most advanced application of nanoscale materials towards human health is application as contrast agents in imaging modalities. MNPs proved safer as imaging contrast agents than conventional methods. MNPs have also been used in overcoming bacterial resistance and as anti-viral agent. They provide further evidences as emerging means in treatment and diagnosis of CVD and chronic inflammatory diseases like Rheumatoid arthritis. They also have employed in gene therapy to treat chronic diseases now a day.
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Al-Radadi, Najlaa S. "Green Biosynthesis of Flaxseed Gold Nanoparticles (Au-NPs) as Potent Anti-cancer Agent Against Breast Cancer Cells." Journal of Saudi Chemical Society 25, no. 6 (June 2021): 101243. http://dx.doi.org/10.1016/j.jscs.2021.101243.

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Kaufman-Szymczyk, Agnieszka, Wiktoria Kaczmarek, Krystyna Fabianowska-Majewska, and Katarzyna Lubecka-Gajewska. "Lunasin and Its Epigenetic Impact in Cancer Chemoprevention." International Journal of Molecular Sciences 24, no. 11 (May 24, 2023): 9187. http://dx.doi.org/10.3390/ijms24119187.

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Cancer diseases are a leading cause of death worldwide. Therefore, it is pivotal to search for bioactive dietary compounds that can avert tumor development. A diet rich in vegetables, including legumes, provides chemopreventive substances, which have the potential to prevent many diseases, including cancer. Lunasin is a soy-derived peptide whose anti-cancer activity has been studied for over 20 years. The results of the previous research have shown that lunasin inhibits histone acetylation, regulates the cell cycle, suppresses proliferation and induces apoptosis of cancer cells. Thus, lunasin seems to be a promising bioactive anti-cancer agent and a potent epigenetic modulator. The present review discusses studies of the underlying molecular mechanisms and new perspectives on lunasin application in epigenetic prevention and anti-cancer therapy.
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Zhang, Zhenqing, Yunli Jia, Xiaoniu Miao, Weifeng Huang, Chao Wang, Zhijun Yuan, Wenchao Jiang, Liandi Chen, Zhiyuan Li, and Andy Tsun. "Abstract 5528: A highly potent anti-CD39 biparatopic antibody and bispecific for cancer therapy." Cancer Research 82, no. 12_Supplement (June 15, 2022): 5528. http://dx.doi.org/10.1158/1538-7445.am2022-5528.

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Abstract Background: There is an increasing demand for effective combinatory agents to improve upon PD-1/PD-L1-based therapeutics. One combinatory target axis is the adenosine metabolism pathway that consists of three major players, including CD39, CD73 and A2AR. Inhibition of any of these targets have shown enhanced preclinical efficacy in combination with PD-1/PD-L1 inhibitors. CD39 is an ectonucleotidase which degrades extracellular ATP to adenosine monophosphate (AMP). This is considered a rate-limiting step for the further degradation to adenosine by CD73. Adenosine is an immunosuppressive metabolite that can suppress NK and T cells. Blockade of CD39-mediated degradation of ATP to AMP may therefore recover anti-tumor immunity through preventing the enrichment of adenosine in the tumor microenvironment. Method: Two anti-CD39 VHH molecules were generated, named Ye-37 and Ye-46, which bind to two different epitopes on CD39. Binding experiments were carried out by bio-layer interferometry. Cell binding experiments were tested on CD39-overexpression cell lines by flow cytometry. Cellular CD39 enzymatic inhibition experiments were tested using an MOLP-8 cell line and PBMC via a luminescence-based assay. Soluble CD39 enzymatic tests were carried out on recombinant CD39 protein using a similar method. T cell proliferation assays were performed and observed on CD4+ or CD8+ T cell populations. In vivo efficacy studies were tested in B-NDG B2M-KO mice that were injected subcutaneously with A375-CD39+ tumor cells and human PBMC. An anti-PD1 x CD39 bispecific antibody was then generated by fusing the anti-CD39 biparatopic antibody to the C-terminus of an anti-PD1 IgG and tested using similar methods. Results: Two candidates, Ye-37 and Ye-46, were selected for their functional activity that recognize non-overlapping epitopes on CD39. The combination of Ye-37 and Ye-46 shows high potency in cell-based and soluble CD39 assays in blocking CD39 activity. Two biparatopic molecules were generated by fusing the biparatopic unit to the N- or C-termini of Fc (46-37-Fc and Fc-37-46) and showed similar activity to the combination. In vivo, we showed single-agent control of tumor growth and potentiation of tumor-growth inhibition when combined with anti-CD73 antibodies. An anti-PD1 x CD39 bispecific was generated and showed potent inhibition of PD-1/PD-L1 interactions by cell-based assays. Potent anti-tumor efficacy was shown, which was as effective as the combination of anti-PD1 plus anti-CD39 antibodies. Conclusion: Potent anti-CD39 and anti-PD1 x CD39 therapeutic candidates have been generated with promising activity as a combinatory or single agent, respectively. As such, we plan to file for clinical trial authorization of these programs by 2022. Citation Format: Zhenqing Zhang, Yunli Jia, Xiaoniu Miao, Weifeng Huang, Chao Wang, Zhijun Yuan, Wenchao Jiang, Liandi Chen, Zhiyuan Li, Andy Tsun. A highly potent anti-CD39 biparatopic antibody and bispecific for cancer therapy [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 5528.
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Olgierd, Batoryna, Żyła Kamila, Banyś Anna, and Morawiec Emilia. "The Pluripotent Activities of Caffeic Acid Phenethyl Ester." Molecules 26, no. 5 (March 2, 2021): 1335. http://dx.doi.org/10.3390/molecules26051335.

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Caffeic acid phenethyl ester (CAPE) is a strong antioxidant extracted from honey bee-hive propolis. The mentioned compound, a well-known NF-κB inhibitor, has been used in traditional medicine as a potent anti-inflammatory agent. CAPE has a broad spectrum of biological properties including anti-viral, anti-bacterial, anti-cancer, immunomodulatory, and wound-healing activities. This review characterizes published data about CAPE biological properties and potential therapeutic applications, that can be used in various diseases.
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Song, Jun-Hui, Juhee Park, Sung Lyea Park, Byungdoo Hwang, Wun-Jae Kim, Chan Lee, and Sung-Kwon Moon. "A Novel Cyclic Pentadepsipeptide, N-Methylsansalvamide, Suppresses Angiogenic Responses and Exhibits Antitumor Efficacy against Bladder Cancer." Cancers 13, no. 2 (January 7, 2021): 191. http://dx.doi.org/10.3390/cancers13020191.

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Here, we explored the anti-tumor efficacy of a cyclic pentadepsipeptide, N-methylsansalvamide (MSSV), in bladder cancer. MSSV inhibited the proliferation of both bladder cancer 5637 and T24 cells, which was attributed to the G1-phase cell cycle arrest, apoptosis induction, and alteration of mitogen-activated protein kinases (MAPKs) and protein kinase b (AKT) signaling pathways. Additionally, the treatment of bladder cancer cells with MSSV suppressed migratory and invasive potential via the transcription factor-mediated expression of matrix metalloproteinase 9 (MMP-9). MSSV abrogated vascular endothelial growth factor (VEGF)-induced angiogenic responses in vitro and in vivo. Furthermore, our result showed the potent anti-tumor efficacy of MSSV in a xenograft mouse model implanted with bladder cancer 5637 cells. Finally, acute toxicity test data obtained from blood biochemical test and liver staining indicated that the oral administration of MSSV at 2000 mg/kg caused no adverse cytotoxic effects. Our preclinical data described the potent anti-angiogenic and anti-tumor efficacy of MSSV and showed no signs of acute toxicity, thereby suggesting the putative potential of oral MSSV as a novel anti-tumor agent in bladder cancer treatment.
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Song, Jun-Hui, Juhee Park, Sung Lyea Park, Byungdoo Hwang, Wun-Jae Kim, Chan Lee, and Sung-Kwon Moon. "A Novel Cyclic Pentadepsipeptide, N-Methylsansalvamide, Suppresses Angiogenic Responses and Exhibits Antitumor Efficacy against Bladder Cancer." Cancers 13, no. 2 (January 7, 2021): 191. http://dx.doi.org/10.3390/cancers13020191.

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Here, we explored the anti-tumor efficacy of a cyclic pentadepsipeptide, N-methylsansalvamide (MSSV), in bladder cancer. MSSV inhibited the proliferation of both bladder cancer 5637 and T24 cells, which was attributed to the G1-phase cell cycle arrest, apoptosis induction, and alteration of mitogen-activated protein kinases (MAPKs) and protein kinase b (AKT) signaling pathways. Additionally, the treatment of bladder cancer cells with MSSV suppressed migratory and invasive potential via the transcription factor-mediated expression of matrix metalloproteinase 9 (MMP-9). MSSV abrogated vascular endothelial growth factor (VEGF)-induced angiogenic responses in vitro and in vivo. Furthermore, our result showed the potent anti-tumor efficacy of MSSV in a xenograft mouse model implanted with bladder cancer 5637 cells. Finally, acute toxicity test data obtained from blood biochemical test and liver staining indicated that the oral administration of MSSV at 2000 mg/kg caused no adverse cytotoxic effects. Our preclinical data described the potent anti-angiogenic and anti-tumor efficacy of MSSV and showed no signs of acute toxicity, thereby suggesting the putative potential of oral MSSV as a novel anti-tumor agent in bladder cancer treatment.
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Kannan, Arvind, Navam Hettiarachchy, and Satya Narayan. "Colon and Breast Anti-cancer Effects of Peptide Hydrolysates Derived from Rice Bran." Open Bioactive Compounds Journal 2, no. 1 (April 16, 2009): 17–20. http://dx.doi.org/10.2174/1874847300902010017.

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Rice bran is an economical, under-utilized co-product of rough rice milling. The objective of this study was to produce rice-bran peptides and investigate for anti-cancer activity. Protein hydrolysates were prepared by treating heat stabilized defatted rice-bran with food grade Alcalase enzyme, followed by treatment with simulated gastric and intestinal juices to obtain resistant peptides. Resistant peptides were fractionated into >50, 10-50, 5-10, and <5 kDa sizes, freeze dried, and evaluated for inhibitory and cytotoxicity activities on human colon (HCT-116) and breast (HTB-26) cancer cell lines. The results showed that <5 kDa fraction of rice-bran is a potent anti-cancer agent. The cytotoxicity of the fraction to both cancer cell types was more pronounced after the treatment with 500 µg/mL. The IC50 of the peptide fraction was approximately 750 µg/mL. These results indicate that the <5 kDa peptide fraction separated from rice bran protein hydrolysate has a potent anti-tumor activity for colon cancer cells. The peptide fractions that demonstrate anti-cancer activities have the potential for use as functional food ingredients for health benefits.
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Ding, Zhongpeng, Hejuan Cheng, Shixiao Wang, Yingwei Hou, Jianchun Zhao, Huashi Guan, and Wenbao Li. "Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent." Bioorganic & Medicinal Chemistry Letters 27, no. 6 (March 2017): 1416–19. http://dx.doi.org/10.1016/j.bmcl.2017.01.096.

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Krutilina, Raisa I., Kelli L. Hartman, Damilola Oluwalana, Hilaire C. Playa, Deanna N. Parke, Hao Chen, Duane D. Miller, Wei Li, and Tiffany N. Seagroves. "Sabizabulin, a Potent Orally Bioavailable Colchicine Binding Site Agent, Suppresses HER2+ Breast Cancer and Metastasis." Cancers 14, no. 21 (October 29, 2022): 5336. http://dx.doi.org/10.3390/cancers14215336.

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HER2+ breast cancer accounts for 15% of all breast cancer cases. Current frontline therapy for HER2+ metastatic breast cancer relies on targeted antibodies, trastuzumab and pertuzumab, combined with microtubule inhibitors in the taxane class (paclitaxel or docetaxel). It is well known that the clinical efficacy of taxanes is limited by the development of chemoresistance and hematological and neurotoxicities. The colchicine-binding site inhibitors (CBSIs) are a class of promising alternative agents to taxane therapy. Sabizabulin (formerly known as VERU-111) is a potent CBSI that overcomes P-gp-mediated taxane resistance, is orally bioavailable, and inhibits tumor growth and distant metastasis in triple negative breast cancer (TNBC). Herein, we demonstrate the efficacy of sabizabulin in HER2+ breast cancer. In vitro, sabizabulin inhibits the proliferation of HER2+ breast cancer cell lines with low nanomolar IC50 values, inhibits clonogenicity, and induces apoptosis in a concentration-dependent manner. In vivo, sabizabulin inhibits breast tumor growth in the BT474 (ER+/PR+/HER2+) xenograft model and a HER2+ (ER-/PR-) metastatic patient-derived xenograft (PDX) model, HCI-12. We demonstrate that sabizabulin is a promising alternative agent to target tubulin in HER2+ breast cancer with similar anti-metastatic efficacy to paclitaxel, but with the advantage of oral bioavailability and lower toxicity than taxanes.
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Sasmal, Sanjita, Sukanya Patra, Venkatesham Boorgu, Shankar Chithaluri, Mahesh Yanamadra, Deepika Hiremath, Hemashankar Pathange, et al. "Abstract 6369: Discovery of potent, orally bioavailable, brain penetrant RAD51 inhibitor as an anti-cancer agent." Cancer Research 82, no. 12_Supplement (June 15, 2022): 6369. http://dx.doi.org/10.1158/1538-7445.am2022-6369.

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Abstract Proliferating cells undergo DNA damage, and this is more pronounced in cancer cells due to their high rate of proliferation. Cancer cells are thus more dependent on the DNA damage repair pathway for their survival. Double-strand breaks (DSBs) are amongst the most severe type of DNA damage and are predominantly repaired by homologous recombination (HR) in an error-free manner. RAD51 is a pivotal recombinase for DSB repair by the HR pathway. Binding of RAD51 with BRCA2 followed by its nuclear translocation, is one of the key repair mechanisms for RAD51 mediated DSB repair. We have identified novel and potent RAD51 inhibitors disrupting the RAD51:BRCA2 interaction, which can address BRCA2 WT patient population. Upon induction of exogenous DNA damage, our compounds inhibit nuclear RAD51 foci formation and demonstrate sustained γH2AX accumulation in the nucleus, suggesting persistent DNA damage. Our orally bioavailable & brain penetrant lead compound shows anti-proliferative activity in multiple BRCA2 WT cancer cell lines across various indications, and excellent synergy when combined with PARP1 inhibitors such as Olaparib. Further, in a wound healing assay, treatment with our lead compound inhibits cell migration in a dose-dependent manner. TNBC patients with extensive brain metastasis have limited treatment options. Thus, a brain penetrant RAD51 inhibitor could provide a novel treatment option in this setting. Citation Format: Sanjita Sasmal, Sukanya Patra, Venkatesham Boorgu, Shankar Chithaluri, Mahesh Yanamadra, Deepika Hiremath, Hemashankar Pathange, Sandeep M. Girme, Amitkumar Pawar, Rutuja Narayan Shinde, Nilanjan Samanta. Discovery of potent, orally bioavailable, brain penetrant RAD51 inhibitor as an anti-cancer agent [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 6369.
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Lyu, Yuan, Steven Kopcho, Folnetti A. Alvarez, Bryson C. Okeoma, and Chioma M. Okeoma. "Development of a Cationic Amphiphilic Helical Peptidomimetic (B18L) As A Novel Anti-Cancer Drug Lead." Cancers 12, no. 9 (August 28, 2020): 2448. http://dx.doi.org/10.3390/cancers12092448.

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BST-2 is a novel driver of cancer progression whose expression confers oncogenic properties to breast cancer cells. As such, targeting BST-2 in tumors may be an effective therapeutic approach against breast cancer. Here, we sought to develop potent cytotoxic anti-cancer agent using the second-generation BST-2-based anti-adhesion peptide, B18, as backbone. To this end, we designed a series of five B18-derived peptidomimetics. Among these, B18L, a cationic amphiphilic α-helical peptidomimetic, was selected as the drug lead because it displayed superior anti-cancer activity against both drug-resistant and drug-sensitive cancer cells, with minimal toxicity on normal cells. Probing mechanism of action using molecular dynamics simulations, biochemical and membrane biophysics studies, we observed that B18L binds BST-2 and possesses membranolytic characteristics. Furthermore, molecular biology studies show that B18L dysregulates cancer signaling pathways resulting in decreased Src and Erk1/2 phosphorylation, increased expression of pro-apoptotic Bcl2 proteins, caspase 3 cleavage products, as well as processing of the caspase substrate, poly (ADP-ribose) polymerase-1 (PARP-1), to the characteristic apoptotic fragment. These data indicate that through the coordinated regulation of membrane, mitochondrial and signaling events, B18L executes cancer cell death and thus has the potential to be developed into a potent and selective anti-cancer compound.
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Viswanadha, Srikant, Satyanarayana Eleswarapu, Kondababu Rasamsetti, Haritha Polimati, Sridhar Veeraraghavan, and Swaroop Vakkalanka. "Abstract 5493: Activity of RP12146, a novel, selective, and potent small molecule inhibitor of PARP 1/2, in solid tumors." Cancer Research 82, no. 12_Supplement (June 15, 2022): 5493. http://dx.doi.org/10.1158/1538-7445.am2022-5493.

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Abstract Introduction: The Poly (ADP-ribose) polymerase (PARP) family plays an important role in the regulation of transcription, apoptosis and DNA damage response. Several PARP inhibitors have been approved for the treatment of BRCA-mutated ovarian, breast and pancreatic cancer. Through ‘synthetic lethality’, the applicability PARP inhibitors can be expanded to cancers beyond the well-defined BRCA defects either as monotherapy or in combination with established therapy across various solid tumor types. Herein, we describe the efficacy of RP12146 as a single agent and in combination with approved therapies in preclinical models of solid tumors. Methods: Enzymatic potency was evaluated using a PARP Chemiluminescent Activity Assay Kit (BPS biosciences). Cell growth was determined following incubation with RP12146 as a single agent or in combination with approved agents in various solid tumor cell lines. Apoptosis was evaluated following incubation of cell lines with compound for 48 or 72 h, subsequent staining with Annexin-V-PE and 7-AAD, and analysis by flow cytometry. Anti-tumor potential of RP12146 as a single agent or in combination with chemotherapeutic agents was tested in OVCAR-3 and NCI-H69 Xenografts. Expression of downstream PAR, PARP-trapping, and cleaved PARP expression were determined in cell lines and xenograft tumor samples by Western blotting. Plasma and tumor concentration of RP12146 in NCI-H69 xenograft samples were also determined. Results: RP12146 demonstrated equipotent inhibition of PARP1 (0.6 nM) and PARP2 (0.5 nM) with several fold selectivity over the other members of the PARP family. Compound caused a dose-dependent growth inhibition of both BRCA mutant and non-mutant cancer cell lines with GI50 in the range of 0.04 µM to 9.6 µM. Combination of RP12146 with Temozolomide, Topotecan, Lurbinectedin, and Abemaciclib demonstrated either additive or synergistic effects manifested by an inhibition in growth of solid tumor cell lines. RP12146 exhibited anti-tumor potential with TGI of 28% and 21.8% as a single agent in OVCAR-3 and NCI-H69 Xenograft model respectively. In NCI-H69 xenograft model, RP12146 in combination with cisplatin exhibited TGI of 69.3 %. Conclusion: Data demonstrate the therapeutic potential of RP12146 as single agent and in combination in solid tumors. RP12146 is currently being evaluated in Phase 1 clinical trials in patients with locally advanced or metastatic solid tumors (NCT05002868). Citation Format: Srikant Viswanadha, Satyanarayana Eleswarapu, Kondababu Rasamsetti, Haritha Polimati, Sridhar Veeraraghavan, Swaroop Vakkalanka. Activity of RP12146, a novel, selective, and potent small molecule inhibitor of PARP 1/2, in solid tumors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 5493.
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Cui, Qingbin, Wenwen Ding, Panpan Liu, Bingling Luo, Jing Yang, Wenhua Lu, Yumin Hu, Peng Huang, and Shijun Wen. "Developing Bi-Gold Compound BGC2a to Target Mitochondria for the Elimination of Cancer Cells." International Journal of Molecular Sciences 23, no. 20 (October 12, 2022): 12169. http://dx.doi.org/10.3390/ijms232012169.

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Reactive oxygen species (ROS) homeostasis and mitochondrial metabolism are critical for the survival of cancer cells, including cancer stem cells (CSCs), which often cause drug resistance and cancer relapse. Auranofin is a mono-gold anti-rheumatic drug, and it has been repurposed as an anticancer agent working by the induction of both ROS increase and mitochondrial dysfunction. Hypothetically, increasing auranofin’s positive charges via incorporating more gold atoms to enhance its mitochondria-targeting capacity could enhance its anti-cancer efficacy. Hence, in this work, both mono-gold and bi-gold compounds were designed and evaluated to test our hypothesis. The results showed that bi-gold compounds generally suppressed cancer cells proliferation better than their mono-gold counterparts. The most potent compound, BGC2a, substantially inhibited the antioxidant enzyme TrxR and increased the cellular ROS. BGC2a induced cell apoptosis, which could not be reversed by the antioxidant agent vitamin C, implying that the ROS induced by TrxR inhibition might not be the decisive cause of cell death. As expected, a significant proportion of BGC2a accumulated within mitochondria, likely contributing to mitochondrial dysfunction, which was further confirmed by measuring oxygen consumption rate, mitochondrial membrane potential, and ATP production. Moreover, BGC2a inhibited colony formation and reduced stem-like side population (SP) cells of A549. Finally, the compound effectively suppressed the tumor growth of both A549 and PANC-1 xenografts. Our study showed that mitochondrial disturbance may be gold-based compounds’ major lethal factor in eradicating cancer cells, providing a new approach to developing potent gold-based anti-cancer drugs by increasing mitochondria-targeting capacity.
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Jiang, Linlin, Lei Zhang, and Xinran Zhang. "Eupalinilide B as a novel anti-cancer agent that inhibits proliferation and epithelial–mesenchymal transition in laryngeal cancer cells." Journal of International Medical Research 50, no. 1 (January 2022): 030006052110679. http://dx.doi.org/10.1177/03000605211067921.

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Objective To investigate the anti-cancer effects and potential mechanisms of eupalinilide B in laryngeal cancer cells. Methods Laryngeal cancer cell lines were selected to study the anti-tumor effects of eupalinilide B in vitro and in vivo. Lysine-specific demethylase 1 (LSD1) activity was assessed in vitro and dialysis experiments were performed to identify the anti-tumor target of the drug. Results Eupalinilide B concentration-dependently inhibited the proliferation of laryngeal cancer cells, exhibiting potent inhibitory activity against TU686 (IC50 = 6.73 µM), TU212 (IC50 = 1.03 µM), M4e (IC50 = 3.12 µM), AMC-HN-8 (IC50 = 2.13 µM), Hep-2 (IC50 = 9.07 µM), and LCC cells (IC50 = 4.20 µM). Subsequent target verification experiments demonstrated that eupalinilide B selectively and reversibly inhibited LSD1. Furthermore, eupalinilide B, as a natural product, suppressed epithelial–mesenchymal transition in TU212 cells. An in vivo experiment further indicated that eupalinilide B could significantly reduce the growth of tumors in TU212 xenograft mouse models. Conclusions Eupalinilide B might be a novel LSD1 inhibitor for treating laryngeal cancer.
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Flick, Hollie E., Judith M. LaLonde, William P. Malachowski, and Alexander J. Muller. "The Tumor-Selective Cytotoxic Agent β-Lapachone is a Potent Inhibitor of IDO1." International Journal of Tryptophan Research 6 (January 2013): IJTR.S12094. http://dx.doi.org/10.4137/ijtr.s12094.

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β-lapachone is a naturally occurring 1,2-naphthoquinone-based compound that has been advanced into clinical trials based on its tumor-selective cytotoxic properties. Previously, we focused on the related 1,4-naphthoquinone pharmacophore as a basic core structure for developing a series of potent indoleamine 2,3-dioxygenase 1 (IDO1) enzyme inhibitors. In this study, we identified IDO1 inhibitory activity as a previously unrecognized attribute of the clinical candidate β-lapachone. Enzyme kinetics-based analysis of β-lapachone indicated an uncompetitive mode of inhibition, while computational modeling predicted binding within the IDO1 active site consistent with other naphthoquinone derivatives. Inhibition of IDO1 has previously been shown to breach the pathogenic tolerization that constrains the immune system from being able to mount an effective anti-tumor response. Thus, the finding that β-lapachone has IDO1 inhibitory activity adds a new dimension to its potential utility as an anti-cancer agent distinct from its cytotoxic properties, and suggests that a synergistic benefit can be achieved from its combined cytotoxic and immunologic effects.
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Mittraphab, Yanisa, Nattaya Ngamrojanavanich, Kuniyoshi Shimizu, Kiminori Matsubara, and Khanitha Pudhom. "Anti-Angiogenic Activity of Rotenoids from the Stems of Derris trifoliata." Planta Medica 84, no. 11 (January 18, 2018): 779–85. http://dx.doi.org/10.1055/s-0044-100797.

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The plants in the genus Derris have proven to be a rich source of rotenoids, of which cytotoxic effect against cancer cells seem to be pronounced. However, their effect on angiogenesis playing a crucial role in both cancer growth and metastasis has been seldom investigated. This study aimed at investigating the effect of the eight rotenoids (1–8) isolated from Derris trifoliata stems on three cancer cells and angiogenesis. Among them, 12a-hydroxyrotenone (2) exhibited potent inhibition on both cell growth and migration of HCT116 colon cancer cells. Further, anti-angiogenic assay in an ex vivo model was carried out to determine the effect of the isolated rotenoids on angiogenesis. Results revealed that 12a-hydroxyrotenone (2) displayed the most potent suppression of microvessel sprouting. The in vitro assay on human umbilical vein endothelial cells was performed to determine whether compound 2 elicits anti-angiogenic effect and its effect was found to occur via suppression of endothelial cells proliferation and tube formation, but not endothelial cells migration. This study provides the first evidence that compound 2 could potently inhibit HCT116 cancer migration and anti-angiogenic activity, demonstrating that 2 might be a potential agent or a lead compound for cancer therapy.
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Chen, Liping, Di Feng, Yafang Qian, Xiao Cheng, Huizhu Song, Yifan Qian, Xu Zhang, et al. "Valtrate as a novel therapeutic agent exhibits potent anti-pancreatic cancer activity by inhibiting Stat3 signaling." Phytomedicine 85 (May 2021): 153537. http://dx.doi.org/10.1016/j.phymed.2021.153537.

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Dhakal, Bimala, Yoko Tomita, Paul Drew, Timothy Price, Guy Maddern, Eric Smith, and Kevin Fenix. "Perhexiline: Old Drug, New Tricks? A Summary of Its Anti-Cancer Effects." Molecules 28, no. 8 (April 21, 2023): 3624. http://dx.doi.org/10.3390/molecules28083624.

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Cancer metabolic plasticity, including changes in fatty acid metabolism utilisation, is now widely appreciated as a key driver for cancer cell growth, survival and malignancy. Hence, cancer metabolic pathways have been the focus of much recent drug development. Perhexiline is a prophylactic antianginal drug known to act by inhibiting carnitine palmitoyltransferase 1 (CPT1) and 2 (CPT2), mitochondrial enzymes critical for fatty acid metabolism. In this review, we discuss the growing evidence that perhexiline has potent anti-cancer properties when tested as a monotherapy or in combination with traditional chemotherapeutics. We review the CPT1/2 dependent and independent mechanisms of its anti-cancer activities. Finally, we speculate on the clinical feasibility and utility of repurposing perhexiline as an anti-cancer agent, its limitations including known side effects and its potential added benefit of limiting cardiotoxicity induced by other chemotherapeutics.
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Krishnan, Aruna V., and David Feldman. "Molecular pathways mediating the anti-inflammatory effects of calcitriol: implications for prostate cancer chemoprevention and treatment." Endocrine-Related Cancer 17, no. 1 (March 2010): R19—R38. http://dx.doi.org/10.1677/erc-09-0139.

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Calcitriol, the hormonally active form of vitamin D, exerts multiple anti-proliferative and pro-differentiating actions including cell cycle arrest and induction of apoptosis in many malignant cells, and the hormone is currently being evaluated in clinical trials as an anti-cancer agent. Recent research reveals that calcitriol also exhibits multiple anti-inflammatory effects. First, calcitriol inhibits the synthesis and biological actions of pro-inflammatory prostaglandins (PGs) by three mechanisms: i) suppression of the expression of cyclooxygenase-2, the enzyme that synthesizes PGs; ii) up-regulation of the expression of 15-hydroxyprostaglandin dehydrogenase, the enzyme that inactivates PGs; and iii) down-regulation of the expression of PG receptors that are essential for PG signaling. The combination of calcitriol and nonsteroidal anti-inflammatory drugs results in a synergistic inhibition of the growth of prostate cancer (PCa) cells and offers a potential therapeutic strategy for PCa. Second, calcitriol increases the expression of mitogen-activated protein kinase phosphatase 5 in prostate cells resulting in the subsequent inhibition of p38 stress kinase signaling and the attenuation of the production of pro-inflammatory cytokines. Third, calcitriol also exerts anti-inflammatory activity in PCa through the inhibition of nuclear factor-κB signaling that results in potent anti-inflammatory and anti-angiogenic effects. Other important direct effects of calcitriol as well as the consequences of its anti-inflammatory effects include the inhibition of tumor angiogenesis, invasion, and metastasis. We hypothesize that these anti-inflammatory actions, in addition to the other known anti-cancer effects of calcitriol, play an important role in its potential use as a therapeutic agent for PCa. Calcitriol or its analogs may have utility as chemopreventive agents and should be evaluated in clinical trials in PCa patients with early or precancerous disease.
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Hemalatha, C. N., and A. M. Vijey. "3D QSAR AND DOCKING STUDY OF PERYLENE - DI IMIDES ANALOGUES AS POTENT APOPTOSIS INDUCER AND EFFICACIOUS ANTICANCER AGENT." INDIAN DRUGS 54, no. 12 (December 28, 2017): 15–27. http://dx.doi.org/10.53879/id.54.12.11012.

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The human telomeric G-Quadruplex structure is a promising target for the design of cancer drugs. The aim of this study was to investigate the anti-cancer activity of perylene derivatives by using in silico computational approach. The perylene derivatives are designed by QSAR studies using VLife MDS Software and activities for these new compounds are predicted. The best predicted activity compounds are screened by G-Quadruplex Ligand Database. Around 59 compounds are selected for docking study. Molecular docking using G-Quadruplex Ligand Database has been carried out and from the study 9 compounds showed high binding affinities for the targets. Finally, from the QSAR and docking studies, 2 compounds showed good biological activity, possessing a strong correlation coefficient, endorsing the fact that perylene derivatives are having strong affinity with the targets. With these compounds, we also observed best pKi values, which shows that they inhibit the targets and may be effective for anti-cancer therapy.
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Shin, Seulgi, Sungsu Lim, Ji Yeon Song, Dohee Kim, Min Jeong Choi, Changdev G. Gadhe, A. Young Park, Ae Nim Pae, and Yun Kyung Kim. "Development of an Aryloxazole Derivative as a Brain-Permeable Anti-Glioblastoma Agent." Pharmaceutics 11, no. 10 (September 28, 2019): 497. http://dx.doi.org/10.3390/pharmaceutics11100497.

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Glioblastoma drug development has been difficult due to the extremely low blood brain barrier (BBB) penetration of conventional anti-cancer agents. P-glycoprotein, an efflux membrane transporter, is responsible for the poor brain uptake of small and hydrophobic drug substances. To develop brain-penetrable anti-tumor agents, we designed colchicine derivatives containing an aryloxazole moiety, which is known to inhibit P-glycoprotein. Among those tested, an aryloxazole derivative named KIST-G1 showed the strongest anti-glioblastoma cell proliferation activity (IC50 = 3.2 ± 0.8 nM). Compared to colchicine, KIST-G1 showed dramatically increased BBB-permeable properties presenting 51.7 ± 0.5 (10−6 cm/s) parallel artificial membrane permeability assay (PAMPA) permeability and 45.0 ± 6.0% of P-gp inhibition. Aid by the BBB-permeable properties, KIST-G1 (5 mg/kg) suppressed glioblastoma cell growth and migration almost completely in the brain of glioblastoma xenograft models by showing 98.2 ± 0.1% reduced tumor area compared with phosphate buffered saline (PBS)-injected control. In comparison, temozolomide, which is the most widely used drug for glioblastoma, showed only moderate effects. Our results demonstrate the effectiveness of an aryloxazole moiety in targeting brain tumors and suggest KIST-G1 as a potent anti-glioblastoma agent.
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46

Harakeh, Steve, Mohammed S. Almuhayawi, Isaac O. Akefe, Saber H. Saber, Soad K. Al Jaouni, Torki Alzughaibi, Yousef Almehmadi, Soad Shaker Ali, Dhruba J. Bharali, and Shaker Mousa. "Novel Pomegranate-Nanoparticles Ameliorate Cisplatin-Induced Nephrotoxicity and Improves Cisplatin Anti-Cancer Efficacy in Ehrlich Carcinoma Mice Model." Molecules 27, no. 5 (February 28, 2022): 1605. http://dx.doi.org/10.3390/molecules27051605.

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Cisplatin (CISP) is one of the most widely used anti-cancer chemotherapeutic agents with remarkable efficacy against various types of cancers. However, it has been associated with nephrotoxicity amongst other undesirable side effects. Pomegranate (PE) is a potent antioxidant and anti-inflammatory agent effective against cancer, with a superior benefit of not being associated with the common toxicities related to the use of conventional chemotherapeutic agents. However, the application of PE is limited by its reduced solubility and decreased bioavailability. We investigated the potential of a novel nanoparticle (NP) enclosing PE to enhance its solubility and improve its bioavailability, and efficacy to prevent CISP-associated nephrotoxicity in a mice model of Ehrlich solid carcinoma (ESC). All mice were grouped into four cohorts: (I) control, (II) tumor, (III) CISP, and (IV) CISP + PE-NPs. The data obtained demonstrated that PE-NPs was beneficial in potently ameliorating CISP-induced nephrotoxicity in ESC mice. PE-NPs significantly attenuated CISP-induced oxidative stress and lipid peroxidation in the kidney via improving activities of antioxidants (SOD, GSH, and CAT). Additionally, PE-NPs considerably decreased CISP-induced inflammation in the kidney by decreasing the levels of NF-kB, IL-1β, and TNF-α. Notably, PE-NPs did not assuage the antitumor efficacy of CISP as revealed by histological assessment and tumor weight data. In summary, PE-NPs may be a potent alternative anticancer therapy devoid of nephrotoxicity.
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47

Hu, Pengchao, Ying Wang, Yan Zhang, Hui Song, Fangfang Gao, Hongyi Lin, Zhihao Wang, Lei Wei, and Fang Yang. "Novel mononuclear ruthenium(ii) complexes as potent and low-toxicity antitumour agents: synthesis, characterization, biological evaluation and mechanism of action." RSC Advances 6, no. 36 (2016): 29963–76. http://dx.doi.org/10.1039/c6ra02571d.

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The ruthenium(ii) complex, [Ru(dmb)2(salH)]PF6(Ru-2), is considered a potential antitumour agent that could avoid the side-effects of platinum-based anti-cancer drugs, such as cisplatin, carboplatin or oxaliplatin.
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48

Ko, Jong-Hee, Hyuk-Sang Kwon, Bomin Kim, Gihong Min, Chorong Shin, Seok-Woo Yang, Seong Wook Lee, Youngmin Lee, Dahae Hong, and Yong-Sung Kim. "Preclinical Efficacy and Safety of an Anti-Human VEGFA and Anti-Human NRP1 Dual-Targeting Bispecific Antibody (IDB0076)." Biomolecules 10, no. 6 (June 17, 2020): 919. http://dx.doi.org/10.3390/biom10060919.

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Although bevacizumab (Avastin®) has been approved as an antiangiogenic agent against some cancers, the efficacy is transient and unsatisfactory in other cancers most likely owing to the presence of alternative proangiogenic factors. Therefore, simultaneous blocking of several proangiogenic factors may be a promising strategy for antiangiogenic cancer therapeutics. Accordingly, neuropilin-1 (NRP1) is an attractive target because it serves as a multifunctional receptor for the vascular endothelial growth factor (VEGF) family. Here, we aimed to generate and test an anti-VEGFA and anti-NRP1 dual-targeting bispecific antibody (named as IDB0076) by genetic fusion of an NRP1-targeting peptide to the C-terminus of the bevacizumab heavy chain. Similar to the parental antibody (bevacizumab), IDB0076 suppressed VEGFA-induced migration of human endothelial cells. In contrast, IDB0076 inhibited endothelial-cell migration induced by other angiogenesis growth factors and manifested a more potent antitumor activity than that of bevacizumab in a murine tumor xenograft model. When toxicity was preliminarily evaluated in cynomolgus monkeys, IDB0076 showed no substantial adverse effects, e.g., the absence of noticeable nephrotoxicity, which has previously been documented for the combination therapy of bevacizumab and an anti-NRP1 antibody. Thus, VEGFA-and-NRP1 dual-targeting bispecific antibody IDB0076 may be a potent and safe anticancer agent worthy of further preclinical and clinical studies.
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49

Booth, Brian W., Beau D. Inskeep, Hiral Shah, Jang Pyo Park, Elizabeth J. Hay, and Karen J. L. Burg. "Tannic Acid Preferentially Targets Estrogen Receptor-Positive Breast Cancer." International Journal of Breast Cancer 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/369609.

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Research efforts investigating the potential of natural compounds in the fight against cancer are growing. Tannic acid (TA) belongs to the class of hydrolysable tannins and is found in numerous plants and foods. TA is a potent collagen cross-linking agent; the purpose of this study was to generate TA-cross-linked beads and assess the effects on breast cancer cell growth. Collagen beads were stable at body temperature following crosslinking. Exposure to collagen beads with higher levels of TA inhibited proliferation and induced apoptosis in normal and cancer cells. TA-induced apoptosis involved activation of caspase 3/7 and caspase 9 but not caspase 8. Breast cancer cells expressing the estrogen receptor were more susceptible to the effects of TA. Taken together the results suggest that TA has the potential to become an anti-ER+breast cancer treatment or preventative agent.
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50

Chen, Ruie, Jinming Zhang, Yangyang Hu, Shengpeng Wang, Meiwan Chen, and Yitao Wang. "Potential Antineoplastic Effects of Aloe-emodin: A Comprehensive Review." American Journal of Chinese Medicine 42, no. 02 (January 2014): 275–88. http://dx.doi.org/10.1142/s0192415x14500189.

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Aloe-emodin (AE), a bioactive anthraquinone derived from both Aloe vera and Rheum officinale, has recently been demonstrated to have various pharmacological activities. With the widespread popularity of natural products, such as antineoplastic drugs, AE has attracted much attention due to its remarkable antineoplastic activity on multiple tumor cells involving multi-channel mechanisms, including the disruption of cell cycle, induction of apoptosis, anti-metastasis, antiangiogenic, and strengthening of immune function. Experimental data have revealed AE as a potentially potent anti-cancer candidate. Despite this, the pharmaceutical application of AE is still in a fledging period as most research has concentrated on the elucidation of the molecular mechanism of action of existing treatments, rather than the development of novel formulations. Therefore, the present review summarizes the potential toxicity, molecular mechanism, pharmacokinetic characteristics, and pharmaceutical development of AE as an antineoplastic agent. This is based on its physicochemical properties, in an attempt to encourage further research on AE as a potential anti-cancer agent.
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