Littérature scientifique sur le sujet « DRUG LEADS TARGETING »
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Articles de revues sur le sujet "DRUG LEADS TARGETING"
Zhu, W., Y. Zhang, W. Sinko, M. E. Hensler, J. Olson, K. J. Molohon, S. Lindert et al. « Antibacterial drug leads targeting isoprenoid biosynthesis ». Proceedings of the National Academy of Sciences 110, no 1 (17 décembre 2012) : 123–28. http://dx.doi.org/10.1073/pnas.1219899110.
Texte intégralChaitanya, MVNL, Asha Jose, P. Ramalingam, SC Mandal et PNarendra Kumar. « Multi-targeting cytotoxic drug leads from mushrooms ». Asian Pacific Journal of Tropical Medicine 12, no 12 (2019) : 531. http://dx.doi.org/10.4103/1995-7645.272482.
Texte intégralKumar, Bhumika, Mukesh Pandey, Faheem H. Pottoo, Faizana Fayaz, Anjali Sharma et P. K. Sahoo. « Liposomes : Novel Drug Delivery Approach for Targeting Parkinson’s Disease ». Current Pharmaceutical Design 26, no 37 (26 octobre 2020) : 4721–37. http://dx.doi.org/10.2174/1381612826666200128145124.
Texte intégralSuresh, Amaroju, Singireddi Srinivasarao, Yogesh Mahadu Khetmalis, Shashidhar Nizalapur, Murugesan Sankaranarayanan et Kondapalli Venkata Gowri Chandra Sekhar. « Inhibitors of pantothenate synthetase of Mycobacterium tuberculosis – a medicinal chemist perspective ». RSC Advances 10, no 61 (2020) : 37098–115. http://dx.doi.org/10.1039/d0ra07398a.
Texte intégralSingh, Vijai, et Pallavi Somvanshi. « Targeting the Peptide Deformylase of Mycobacterium tuberculosis Leads to Drug Discovery ». Letters in Drug Design & ; Discovery 6, no 7 (1 octobre 2009) : 487–93. http://dx.doi.org/10.2174/157018009789108286.
Texte intégralPal, Rahul, Saif Hameed et Zeeshan Fatima. « Iron Deprivation Affects Drug Susceptibilities of Mycobacteria Targeting Membrane Integrity ». Journal of Pathogens 2015 (2015) : 1–10. http://dx.doi.org/10.1155/2015/938523.
Texte intégralJonchere, Barbara, Jennifer Stripay, Allison Pribnow, Frederique Zindy, Jaeki Min, Burgess Freeman, Anang Shelat, Zoran Rankovic et Martine Roussel. « PDTM-02. TARGETING THE RB PATHWAY IN MEDULLOBLASTOMA ». Neuro-Oncology 21, Supplement_6 (novembre 2019) : vi187. http://dx.doi.org/10.1093/neuonc/noz175.778.
Texte intégralOjima, Iwao. « Tumor-targeting drug delivery of chemotherapeutic agents ». Pure and Applied Chemistry 83, no 9 (24 juin 2011) : 1685–98. http://dx.doi.org/10.1351/pac-con-11-02-10.
Texte intégralSrikanth A, Shivakmar T, Shankar Sheshu R et Selva kumar S. « Molecular modelling and evaluation of antihyperthyroid drug compound ». International Journal of Review in Life Sciences 9, no 4 (27 décembre 2019) : 30–32. http://dx.doi.org/10.26452/ijrls.v9i4.1350.
Texte intégralKaminska, Kamila K., Helene C. Bertrand, Hisashi Tajima, William C. Stafford, Qing Cheng, Wan Chen, Geoffrey Wells, Elias S. J. Arner et Eng-Hui Chew. « Indolin-2-one compounds targeting thioredoxin reductase as potential anticancer drug leads ». Oncotarget 7, no 26 (24 mai 2016) : 40233–51. http://dx.doi.org/10.18632/oncotarget.9579.
Texte intégralThèses sur le sujet "DRUG LEADS TARGETING"
Sandhaus, Shayna. « Drug Candidate Discovery : Targeting Bacterial Topoisomerase I Enzymes for Novel Antibiotic Leads ». FIU Digital Commons, 2017. https://digitalcommons.fiu.edu/etd/3561.
Texte intégralMateo, Campins Patricia. « Recerca i caracterització de nous "leads" per al tractament del càncer ». Doctoral thesis, Universitat de Barcelona, 2018. http://hdl.handle.net/10803/663545.
Texte intégralThis doctoral thesis focuses on the development of new small molecules against different cancer targets. Recent findings arisen from human cancer genome sequencing have revealed that many genes involved in the regulation of chromatin that modify histones are often mutated in a wide variety of cancers. Among these histone modifiers, multiproteic complexes named Polycomb Repressive Complex (PRC) are implicated in epigenetic silencing mainly affecting the structure of chromatin, stem cell pluripotency and expression of specific genes involved in cell differentiation and development. In particular, the catalytic component of PRC2 called Enhancer of Zeste Homolog 2 (EZH2) has drawn special attention since its overexpression has been found in several cancer types and its regulators seem to be critical for cellular proliferation, tumour formation and stem cell function maintenance. Moreover, we are looking for multitarget compounds that inhibit essential enzymes for cancer progression and development that show selectiveness against cancerous cells in order to reduce side effects. Three different synthetic routes have been set: preparation of 1,4-benzodioxan derivatives, preparation of diarylamine intermediates and preparation of diarylethers. All compounds have been prepared using classic organic reactions, purified using common separation techniques (chromatography) and their structure elucidation has been carried out through Nuclear Magnetic Resonance (NMR), Mass Spectroscopy (MS) and Infrared Spectroscopy (IS). In order to assess their biological activities, a high throughput screening has been performed at Eli Lilly laboratories over different disorders (cancer, autoimmunity, neurodegeneration and pain, endocrine and vascular diseases, etc.). In addition, MTT assays have been performed in osteosarcoma cell lines since diverse studies suggest that EZH2 expression is significantly associated with more aggressive osteosarcoma tumour behaviour and poorer patient outcome. Thus, an epigenetic therapy that pharmacologically targets EZH2 via specific inhibitors may constitute a novel approach to the treatment of osteosarcoma.
Hu, Yanmei, Jiantao Zhang, Rami Musharrafieh, Raymond Hau, Chunlong Ma et Jun Wang. « Chemical Genomics Approach Leads to the Identification of Hesperadin, an Aurora B Kinase Inhibitor, as a Broad-Spectrum Influenza Antiviral ». MDPI AG, 2017. http://hdl.handle.net/10150/626106.
Texte intégralMcGinley, Susan. « New Leads for Cancer Drugs : Targeting a Specific Biochemical Pathway in Tumors ». College of Agriculture and Life Sciences, University of Arizona (Tucson, AZ), 2007. http://hdl.handle.net/10150/622135.
Texte intégralIbba, Roberta. « Antiviral drug discovery : from synthesis of virus-targeting molecules to fragment-based lead discovery for a novel host target ». Doctoral thesis, Università degli Studi di Cagliari, 2020. http://hdl.handle.net/11584/284395.
Texte intégralGUPTA, ANKITA. « COMPUTATIONAL CHARACTERIZATION OF NON-ACTIVE SITE MUTATION V77I IN HIV-1 PROTEASE : POSSIBLE CONTRIBUTION TO NELFINAVIR RESISTANCE AND DEVELOPMENT OF NEW DRUG LEADS TARGETING HIV-1 PROTEASE ». Thesis, 2016. http://dspace.dtu.ac.in:8080/jspui/handle/repository/16058.
Texte intégralPaterna, Angela. « Indole alkaloids as leads for developing effective anticancer drugs targeting multidrug resistant cancer cells ». Doctoral thesis, 2017. http://hdl.handle.net/10451/28894.
Texte intégralMultidrug resistance (MDR) is the major obstacle for cancer chemotherapy. MDR is a multifactorial phenomenon that can result from several mechanisms, including an increased drug efflux, due to overexpression of ABC drug transporter proteins (P-gp, MRP1 and ABCG2), which transport anticancer drugs out of the cells, or a failure to undergo apoptosis. The development of ABC transporter inhibitors is a promising approach for overcoming MDR. The discovery of collateral sensitivity agents (CS) and the development of effective apoptosis inducers have also been considered realistic strategies. Thus, the main goal of this work was to find out new effective anticancer indole alkaloids from African plants (Apocynaceae and Rubiaceae families), targeting MDR cancer cells. The phytochemical study of the alkaloid fraction of the methanol extract of Tabernaemontana elegans yielded three novel (4-6) and five known (7-11) bisindole alkaloids of the vobasinyl-iboga type and three monoterpene indole alkaloids of the corinanthe type (1-3). Moreover, aiming at generating a small library of monoterpene indole alkaloids, the chemical derivatization of the two epimeric monoterpene indole alkaloids dregamine (1) and tabernaemontanine (2),isolated in large amount from this species, allowed the preparation of 47 derivatives. In this way, the chemical transformation of the ketone group at C-3 of both compounds (1 and 2) afforded several aromatic and aliphatic imines (1.1-1.8 and 2.1-2.6) and azines (1.16-1.27 and 2.9-2.20), a thioketone (1.9), alcohols (1.10 and 2.7), and esters (1.11 and 2.8). The N-acyl/alkylated compounds 1.12 1.15 were also obtained. From the alkaloid fraction of the methanol extract of Voacanga thouarsii, one new monoterpene indole alkaloid (16) of the iboga type and four known (12-15), along with one indole alkaloid of the sarpagine type (17) were isolated. Moreover, a new phenol, 3,4,5-trimethoxyphenol-1-O-β-D-glucopyranosyl-4′,6′-O-(E)-dicoumaroyl ester (19), and several known phenolic compounds (18, 20-22), one steroid (23) and one triterpene (24) were also obtained. The phytochemical study of Psychotria capensis yielded two norisoprenoids (28-29) and three phenolic compounds (25-27). The structures of the compounds were established from their physical and spectroscopic data (IR, MS, 1D and 2D NMR -COSY, HMBC, HMQC and NOESY-experiments). The indole alkaloids 4-8, 9, 1.1-1.5 and 2.1-2.5 were evaluated for their ability as apoptosis inducers in HCT116, and SW620 colon and HepG2 liver cancer cells. The cytotoxicity of the compounds was evaluated in the three cell lines by the MTS and lactate dehydrogenase assays. The apoptosis induction studies included Guava ViaCount flow cytometry assays, nuclear morphology evaluation by Hoechst staining, and caspase-3/7 activity assays. To explore the association of compounds-induced growth inhibition with regulation of cell cycle progression, the cellular DNA content was determined by flow cytometry, analysing the percentage of cells in different phases of the cell cycle. Moreover, in order to determine the molecular pathways by which compounds exerted their pro-apoptotic effect, key apoptosis proteins were evaluated by immunoblot analysis, using total protein extracts from HCT116, SW620 or HepG2 cells exposed to compounds. The most significant results were obtained for some hydrazones (1.4, 2.2 and 2.4) and several bisindole alkaloids (4-7 and 9). Structure-activity relationships for compounds 1, 2 and their derivatives (1.1-1.5 e 2.1-2.5) showed that the replacement of the carbonyl group of the parent compounds 1 and 2 by a hydrazone moiety, bearing a bromo-pyridine (1.4 and 2.4) or a phenyl group (2.2) seems to be responsible for their activity, which might also depend on the stereochemistry of the tetrahedral stereocenter at C-20. The induced inhibition of proliferation of HCT116 cells by bisindole alkaloids 4 and 5 was associated with G1 phase arrest, while bisindole alkaloids 6 and 9 induced G2/M cell cycle arrest. In addition, immunoblot analysis showed that exposure to compound 7 reduced the expression of anti-apoptotic proteins in the tree cell lines. The monoterpene indole alkaloids 1, 2 and their derivatives 1.1-1.15, 2.1-2.8 were also evaluated for their effects on the reversion of MDR in cancer cells mediated by P-glycoprotein using a human ABCB1-transfected mouse T-lymphoma cell model. SAR analysis showed that different substituents at C-3 and at the indole nitrogen led to different ABCB1 modulatory effects. A remarkable enhancement in MDR reversal activity was found for the imine derivatives 1.4, 1.7, 2.3 and 2.4, sharing a new aromatic moiety. Some of these indole alkaloids (1.2-1.4, 1.7-1.9, 1.12, 1.13 e 2.2-2.4) were assayed for their antiproliferative effects in combination with doxorubicin; the results showed that the tested compounds synergistically enhanced the effect of the antitumor drug. The anti-MDR reversal activity of azine derivatives (1.16-1.27 and 2.9-2.20) was evaluated using as models transfected cancer cells NHI-3T3 overexpressing P-gp, and a transfected HEK293 cell line overexpressing either MRP1 or ABCG2. In both cancer cell lines overexpressing P-gp or MRP1, a considerable MDR reversing activity was observed for compounds with an aromatic azine moiety. The strongest activity as P-gp inhibitors was found for the epimeric azines 1.16 and 2.9, which were found to be selective for this transporter. Instead, compounds 1.22 and 2.15 inhibited selectively MRP1 drug-efflux. No compound was able to inhibit ABCG2. Azine derivatives (1.16-1.27 and 2.9-2.20) were also evaluated as collateral sensitivity agents. Compounds 2.12, with an aromatic azine moiety at C-3, and compounds 1.24, 1.25, 2.17 and 2.18, sharing a new aliphatic -C=N-N=C-R at this carbon, were considered CS agents killing selectively BHK-21-MRP1 overexpressing cells. Among the compounds with selective cytotoxic activity against cancer cells overexpressing MRP1, compounds 1.23-1.25 were able to increase the depletion of glutathione by MRP1, thus triggering cell death through apoptosis. In conclusion, several indole alkaloids of both natural origin or obtained by derivatization are promising potential lead structures as MDR reversers.
Fundação para a Ciência e a Tecnologia (FCT), projeto, PTDC/QEQ-MED/0905/2012
Livres sur le sujet "DRUG LEADS TARGETING"
Divan, Aysha, et Janice A. Royds. 7. Molecular biology in the clinic. Oxford University Press, 2016. http://dx.doi.org/10.1093/actrade/9780198723882.003.0007.
Texte intégralChapitres de livres sur le sujet "DRUG LEADS TARGETING"
Prakash, Om, et Feroz Khan. « CoSSDb : A Database of Co-crystallized Ligand Sub-structures for Anticancer Lead Designing & ; Optimization ». Dans Proceedings of the Conference BioSangam 2022 : Emerging Trends in Biotechnology (BIOSANGAM 2022), 133–41. Dordrecht : Atlantis Press International BV, 2022. http://dx.doi.org/10.2991/978-94-6463-020-6_14.
Texte intégralKumari, Archana, et Rajesh K. Singh. « Morpholine : Pharmacophore Modulating Pharmacokinetic Properties of Anticancer Leads ». Dans Key Heterocyclic Cores for Smart Anticancer Drug–Design Part II, 137–73. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815040043122020008.
Texte intégralSailaja, Inampudi, Manoj Kumar Baghel et Ivvala Anand Shaker. « Nanotechnology Based Drug Delivery for HIV-AIDS Treatment ». Dans AIDS Updates - Recent Advances and New Perspectives [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.97736.
Texte intégralKesharwani, Payal, Kajal Kumari, Smita Jain et Swapnil Sharma. « Barriers to Targeted Drug Delivery Strategies in Brain ». Dans Brain Tumor Targeting Drug Delivery Systems : Advanced Nanoscience for Theranostics Applications, 34–59. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815079722123010004.
Texte intégralChandrawanshi, Nagendra Kumar, et Shekhar Verma. « Recent Research and Development in Stem Cell Therapy for Cancer Treatment ». Dans Handbook of Research on Advancements in Cancer Therapeutics, 514–33. IGI Global, 2021. http://dx.doi.org/10.4018/978-1-7998-6530-8.ch018.
Texte intégralCesarini, Sara, Angelo Ranise et Andrea Spallarossa. « A Successful Application Of Parallel Synthesis To Computer-assisted Structural Optimization Of New Leads Targeting Human Immunodeficiency Virus-1 Reverse Transcriptase The Case Of Acylthiocarbamates And Thiocarbamates ». Dans High-Throughput Lead Optimization in Drug Discovery, 117–49. CRC Press, 2008. http://dx.doi.org/10.1201/9781420006964.ch4.
Texte intégral« A Successful Application of Parallel Synthesis to Computer-Assisted Structural Optimization of New Leads Targeting Human Immunodeciency Virus-1 Reverse Transcriptase : The Case of Acylthiocarbamates and Thiocarbamates ». Dans High-Throughput Lead Optimization in Drug Discovery, 127–60. CRC Press, 2008. http://dx.doi.org/10.1201/9781420006964-7.
Texte intégralSetia, Aseem, Ram Kumar Sahu, Ayodeji Folorunsho Ajayi et Emmanuel Tayo Adebayo. « Theranostics Dendrimer for Brain Tumor Diagnosis and Treatment ». Dans Brain Tumor Targeting Drug Delivery Systems : Advanced Nanoscience for Theranostics Applications, 121–39. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815079722123010007.
Texte intégralJ Kogan, Marcelo, Francisco Salazar-Cornejo, Abraham Gajardo et Ramón Rodrigo. « Improvement of Nitric Oxide Availability in Myocardial Ischemia/reperfusion : Role of Nanotechnology as a Therapeutic Approach ». Dans Blood Oxidant Ties : The Evolving Concepts in Myocardial Injury and Cardiovascular Disease, 148–66. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815165012123010011.
Texte intégralGarg, Ashish, Vijay Sagar Madamsetty, Sumel Ashique, Vinod Gauttam et Neeraj Mishra. « Targeted Nanocarriers-based Approach For Prostate Cancer Therapy ». Dans Therapeutic Nanocarriers in Cancer Treatment : Challenges and Future Perspective, 133–62. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815080506123010008.
Texte intégralActes de conférences sur le sujet "DRUG LEADS TARGETING"
Williams, Alicia M., et Pavlos P. Vlachos. « Dynamics of Magnetic Drug Targeting in Cardiovascular Flows ». Dans ASME 2007 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2007. http://dx.doi.org/10.1115/sbc2007-176632.
Texte intégralShi, Yihui, Chandraiah Lagisetti Lagisetti, Amanda S. Joyner, Lidia C. Sambucetti et Thomas R. Webb. « Abstract 4365 : Targeting the SF3B1 spliceosome protein : Development of a reporter for HTS screen and pharmacodynamic profiling of small molecule drug leads ». Dans Proceedings : AACR 106th Annual Meeting 2015 ; April 18-22, 2015 ; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-4365.
Texte intégralHicks, Stuart W., Katharine C. Lai, Yong Yi, Prerak Shah, Cristina L. Gavrilescu, Joe Ponte, Callum M. Sloss et Angela Romanelli. « Abstract 1073 : Increased internalization and processing of the CD37-targeting antibody-drug conjugate, naratuximab emtansine (IMGN529), in the presence of rituximab leads to enhanced potency in diffuse large B-cell lymphoma models ». Dans Proceedings : AACR Annual Meeting 2017 ; April 1-5, 2017 ; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-1073.
Texte intégralCooper, Daniel B., et Pavlos P. Vlachos. « Parametric Investigation of Magnetic Particle Transport for Targeted Drug Delivery Applications ». Dans ASME 2011 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2011. http://dx.doi.org/10.1115/sbc2011-53889.
Texte intégralGeerligs, Marion, Lambert C. A. v. Breemen, Gerrit W. M. Peters, Paul A. J. Ackermans, Cees W. J. Oomens et Frank P. T. Baaijens. « Mechanical Properties of the Epidermis and Stratum Corneum Determined by Submicron Indentation In Vitro ». Dans ASME 2009 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2009. http://dx.doi.org/10.1115/sbc2009-204412.
Texte intégralThomas, Antony, Paige Baldwin et Yaling Liu. « Ultrasound Mediated Enhancement of Nanoparticle Uptake in PC-3 Cancer Cells ». Dans ASME 2013 2nd Global Congress on NanoEngineering for Medicine and Biology. American Society of Mechanical Engineers, 2013. http://dx.doi.org/10.1115/nemb2013-93115.
Texte intégralMirkhani, Seyed Nima, Tinotenda Gwisai, Michael G. Christiansen et Simone Schuerle. « Scalable and Spatially Selective Actuation of Living Microrobots ». Dans THE HAMLYN SYMPOSIUM ON MEDICAL ROBOTICS. The Hamlyn Centre, Imperial College London London, UK, 2023. http://dx.doi.org/10.31256/hsmr2023.55.
Texte intégralShahat, Ayman EL, Mohamed Osama Abd Elmeguid, Luis Gerardo, Abdalla Saleh Saleh, Saeed Mohamed Almazrouei, Ali Sulaiman Bin Sumaida, Ahmed Abdulla Al Mutawa et al. « Successful Delivery of the First Extended Reach Well Using an Integrated Multidisciplinary Approach ; A Case Study in a Mature Field, Onshore Abu Dhabi UAE ». Dans ADIPEC. SPE, 2022. http://dx.doi.org/10.2118/211492-ms.
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