Letteratura scientifica selezionata sul tema "Small inhibitory compounds"
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Articoli di riviste sul tema "Small inhibitory compounds":
Alvarez-Gonzalez, Juan Antonio, Robert Maul, Rahul M. Kohli e Patricia J. Gearhart. "Small molecule inhibitors of Activation-Induced Deaminase". Journal of Immunology 200, n. 1_Supplement (1 maggio 2018): 48.18. http://dx.doi.org/10.4049/jimmunol.200.supp.48.18.
Yan, Hua, Tomoko Chiba Mizutani, Nobuhiko Nomura, Tadakazu Takakura, Yoshihiro Kitamura, Hideka Miura, Masako Nishizawa, Masashi Tatsumi, Naoki Yamamoto e Wataru Sugiura. "A Novel Small Molecular Weight Compound with a Carbazole Structure That Demonstrates Potent Human Immunodeficiency Virus Type-1 Integrase Inhibitory Activity". Antiviral Chemistry and Chemotherapy 16, n. 6 (dicembre 2005): 363–73. http://dx.doi.org/10.1177/095632020501600603.
Asai, Takashi, Tsutomu Takeuchi, Jeff Diffenderfer e L. David Sibley. "Identification of Small-Molecule Inhibitors of Nucleoside Triphosphate Hydrolase in Toxoplasma gondii". Antimicrobial Agents and Chemotherapy 46, n. 8 (agosto 2002): 2393–99. http://dx.doi.org/10.1128/aac.46.8.2393-2399.2002.
Patkar, Chinmay G., Martha Larsen, Michael Owston, Janet L. Smith e Richard J. Kuhn. "Identification of Inhibitors of Yellow Fever Virus Replication Using a Replicon-Based High-Throughput Assay". Antimicrobial Agents and Chemotherapy 53, n. 10 (3 agosto 2009): 4103–14. http://dx.doi.org/10.1128/aac.00074-09.
Han, Chun, Jiahong Ren, Feng Su, Xiaoqin Hu, Mengyao Li, Zhijun Wang e Lintao Wu. "Hybrids of Quinoline and Anilinopyrimidine: Novel EGFRT790M Inhibitors with Antiproliferative Activity against Non-Small Cell Lung Cancer Cell Lines". Anti-Cancer Agents in Medicinal Chemistry 20, n. 6 (14 giugno 2020): 724–33. http://dx.doi.org/10.2174/1871520620666200302113206.
Abramić, Marija, e Dejan Agić. "Survey of Dipeptidyl Peptidase III Inhibitors: From Small Molecules of Microbial or Synthetic Origin to Aprotinin". Molecules 27, n. 9 (7 maggio 2022): 3006. http://dx.doi.org/10.3390/molecules27093006.
Noueiry, Amine O., Paul D. Olivo, Urszula Slomczynska, Yi Zhou, Ben Buscher, Brian Geiss, Michael Engle et al. "Identification of Novel Small-Molecule Inhibitors of West Nile Virus Infection". Journal of Virology 81, n. 21 (22 agosto 2007): 11992–2004. http://dx.doi.org/10.1128/jvi.01358-07.
Lefas, Georgia, e George Chaconas. "High-Throughput Screening Identifies Three Inhibitor Classes of the Telomere Resolvase from the Lyme Disease Spirochete". Antimicrobial Agents and Chemotherapy 53, n. 10 (13 luglio 2009): 4441–49. http://dx.doi.org/10.1128/aac.00529-09.
Ercan-Fang, Nacide, Miriam R. Taylor, Judith L. Treadway, Carolyn B. Levy, Paul E. Genereux, E. Michael Gibbs, Virginia L. Rath, Younggil Kwon, Mary C. Gannon e Frank Q. Nuttall. "Endogenous effectors of human liver glycogen phosphorylase modulate effects of indole-site inhibitors". American Journal of Physiology-Endocrinology and Metabolism 289, n. 3 (settembre 2005): E366—E372. http://dx.doi.org/10.1152/ajpendo.00264.2004.
Yoo, Jihye, Darong Kim, Jiyoung Park, Young-Kook Kim, Hea-Young Park Choo e Hyun Ae Woo. "Novel Small Molecule Inhibitors Targeting the IL-6/STAT3 Pathway or IL-1β". Molecules 27, n. 9 (22 aprile 2022): 2696. http://dx.doi.org/10.3390/molecules27092696.
Tesi sul tema "Small inhibitory compounds":
He, Fei, e 贺斐. "In vitro growth inhibitory effects of arsenic trioxide in non-small cell lung cancer with different epidermal growth factor receptormutations". Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2010. http://hub.hku.hk/bib/B45860063.
Richmond, Oliver H. III. "Extraction, Purification and Evaluation of PRMT5-Inhibitory Phytochemical Compounds for the Treatment of Prostate Adenocarcinoma". DigitalCommons@Robert W. Woodruff Library, Atlanta University Center, 2019. http://digitalcommons.auctr.edu/cauetds/185.
García, Reyes Balbina [Verfasser]. "Validation of new Casein Kinase 1 (CK1) small molecule inhibitor compounds and characterization of Inhibitors of Wnt Production (IWPs) as inhibitors of CK1δ / Balbina García Reyes". Ulm : Universität Ulm, 2018. http://d-nb.info/1151938424/34.
Mohamed, Safwat. "Parallel synthesis of small molecule compound libraries : isoform selective Rho-Kinase inhibitors". Thesis, University of British Columbia, 2015. http://hdl.handle.net/2429/54300.
Pharmaceutical Sciences, Faculty of
Graduate
Strand, Mårten. "The discovery of antiviral compounds targeting adenovirus and herpes simplex virus : assessment of synthetic compounds and natural products". Doctoral thesis, Umeå universitet, Virologi, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-88186.
Nikjoo, Dariush. "Design and Synthesis of a Small Set of Thiourea-based Compounds as Inhibitors of AChE1 from Mosquitoes". Thesis, Umeå universitet, Kemiska institutionen, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-92551.
Stoup, Nicolas. "Rôle des domaines EGF de la mucine MUC4 dans la relation structure-fonction et le ciblage thérapeutique du complexe oncogénique MUC4-ErbB2 dans l'adénocarcinome pancréatique". Electronic Thesis or Diss., Université de Lille (2022-....), 2023. http://www.theses.fr/2023ULILS065.
Pancreatic cancer is the 4th leading cause of cancer death worldwide. It is a highly lethal pathology, whose 5-year survival does not exceed 10%. This poor prognosis is explained by a late diagnosis of the disease, most often at metastatic or locally advanced stages (80% of patients at diagnosis), but also mainly due to a lack of efficient therapies. Targeted therapies, especially those targeting the ErbB2 receptor (overexpressed in this cancer), as well as conventional therapies (FOLFIRINOX, gemcitabine, Nab-paclitaxel) remain inefficient or fail, representing palliative options more than therapeutic treatments. Moreover, the incidence of this cancer is constantly increasing since the 80's (+247.7% globally between 1980 and 2012), and epidemiologic projections indicate that it will be second leading cause of cancer death by 2030. So, this major public health problem requires the identification of new therapeutic targets in order to propose new alternative treatments, more efficient to reduce the progression of this cancer. In this way, the MUC4 membrane mucin seems to be an attractive target, since it is neo-expressed from the early stages of the disease and over-expressed during pancreatic carcinogenesis. MUC4 is a large O-glycoprotein expressed at the surface of epithelia, whose main role is to ensure cellular homeostasis, but which is strongly deregulated in tumor processes. Also, MUC4 is one of the only known partners of ErbB2 at the membrane. Previous work in the laboratory had identified a region in the extracellular part of MUC4 encompassing three EGF-like domains, and involved in the interaction with ErbB2. However, before this thesis work, nothing was known about the exact biologic modalities of the interaction between MUC4 and ErbB2, as well as if the MUC4EGF domains possessed intrinsic pro-tumoral biological activity. Also, no molecules efficiently targeting the complex have been tested so far. Hence, the aim of this project was (i) to elucidate the structure-function relationships of the MUC4-ErbB2 complex, by enlightening the importance of the EGF domains of MUC4 in the interaction with ErbB2 and the pancreatic tumor promotion, and then (ii) to characterize the effects of the first inhibitory peptide of the MUC4-ErbB2 complex targeting the mucin. This work thus shows that the EGF domains of MUC4 generate the oncogenicity of the complex, by bearing the interaction with ErbB2 on specific hostspots and by playing the role of growth factors, promoting cell proliferation and cell migration both in vitro and in vivo. We have also identified the signaling pathways specifically activated by the MUC4EGF-ErbB2 complex, and the pro-tumoral markers up-regulated by this interaction. Finally, we show that the MUC4-ErbB2 complex can be targeted by small inhibitory molecules to reduce cancer cell proliferation in vitro and to promote the reaccessibility of targeted therapies against ErbB2. Together, these results validate the therapeutic interest of targeting the MUC4-ErbB2 complex, and especially the MUC4EGF domains, as a new anti-cancer strategy in pancreatic cancer
Garbom, Sara. "A strategy to identify novel antimicrobial compounds : a bioinformatics and HTS approach". Doctoral thesis, Umeå : Department of Molecular Biology, Umeå University, 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-900.
Merkle, Ruth [Verfasser], e Ursula [Akademischer Betreuer] Klingmüller. "Impact of growth factors, therapeutic inhibitors and cytostatic compounds on the response of non-small-cell lung carcinoma cell lines / Ruth Merkle ; Betreuer: Ursula Klingmüller". Heidelberg : Universitätsbibliothek Heidelberg, 2015. http://d-nb.info/1180396413/34.
Schmidt, Thomas Christian. "Theoretical Investigations on the Interactions of Small Compounds with their Molecular Environments". Doctoral thesis, 2015. https://nbn-resolving.org/urn:nbn:de:bvb:20-opus-127860.
In the first part of this work, a combination of theoretical methods for the rational design of covalent inhibitor is presented. Starting from the crystal structure of the covalent complex of a lead compound, quantum mechanical and QM/MM calculations were used to derive the exact geometry of the preceeding non-covalent enzyme inhibitor complex. The geometry of the latter mainly determines the reactivity of the inhibitor against its target enzyme concerning the formation of the covalent bond towards an active site residue. Therefore, this geometry was used as starting point for the optimization of the substitution pattern of the inhibitor such as to increase its binding affinity without loosing its ability to covalently bind to the target protein. The optimization of the chemical structure was supported by using docking procedures, which are best suited to estimate binding affinities that arise from the introduced changes. A screening of the novel substitution patterns resulted in a first generation of model compounds which were further tested for their reactivity against the target. Dynamic simulations on the novel compounds revealed that the orientation that compounds adopt within the active site are such that a covalent interaction with the enzyme is no longer possible. Hence, the chemical structure was further modified, including not only changes in the substituents but also within the core of the molecule. Docking experiments have been conducted to assure sufficiently high binding affinities and to obtain the most favored binding poses. Those have then again been used for dynamic simulations which resulted in structures, for which the bond formation process appeared feasible. A final series of QM/MM calculations considering various protonation states was computed to estimate the reaction energies for the covalent attachment of the inhibitor to the enzyme. The theoretical results indicate a reasonable high inhibition potency of the novel compounds. The second part concentrates on the environmental influences on the electron density of an inhibitor molecule. Therefore, a vinylsulfone-based model compound was selected for which an experimental crystal structure for the pure compound as well as a theoretically determined enzyme-inhibitor complex have been available. To provide reference data for the larger systems, the conformational space of the isolated molecule was screened for favorable geometries which were later compared to those within the crystal and protein surrounding. The geometry of the crystal structure could readily be taken from the experimental data whereas calculations on the protein complex revealed four potential non-covalent complexes exhibiting different arrangements of the molecule within the active site of the protein as well as two possible protonation states of the catalytic dyad. Hence, all four protein complexes have been compared to the crystal structure of the molecule as well as against the more favorable geometries of the isolated molecule being determined within vacuum or aqueous surrounding. Whereas the molecule itself was found to adopt comparable geometries within all investigated environments, the interactions pattern between the crystal surrounding and the protein differed largely from each other. The favorable formation of dimers within the crystal has a strong stabilizing effect and explains the extraordinarily good quality of the crystal. Within the protein however, repulsive forces have been found between the protein and the inhibitor. The origin of the repulsion could be traced back to effect of on of the substituents to the vinyl scaffold. The difference in the chemical structure in comparison to a well known inhibitor might also explain the experimentally found loss of activity for the model compound in comparison to K11777
Libri sul tema "Small inhibitory compounds":
Woywodt, Alexander, e Diana Chiu. Drug-induced and toxic glomerulopathies. A cura di Neil Turner. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199592548.003.0082.
Capitoli di libri sul tema "Small inhibitory compounds":
Workman, Paul. "Reflections and Outlook on Targeting HSP90, HSP70 and HSF1 in Cancer: A Personal Perspective". In Advances in Experimental Medicine and Biology, 163–79. Cham: Springer International Publishing, 2020. http://dx.doi.org/10.1007/978-3-030-40204-4_11.
Ferrari, Stefania, Federica Pellati e Maria Paola Costi. "Protein–Protein Interaction Inhibitors: Case Studies on Small Molecules and Natural Compounds". In Disruption of Protein-Protein Interfaces, 31–60. Berlin, Heidelberg: Springer Berlin Heidelberg, 2013. http://dx.doi.org/10.1007/978-3-642-37999-4_2.
Kakkar, Rita. "In silico design of PDHK inhibitors: From small molecules to large fluorinated compounds". In Computational Chemistry Methodology in Structural Biology and Materials Sciences, 97–130. Toronto; New Jersey: Apple Academic Press, 2017.: Apple Academic Press, 2017. http://dx.doi.org/10.1201/9781315207544-4.
Hoffer, Laurent, Philippe Roche e Xavier Morelli. "Rational Design of PDZ Domain Inhibitors: Discovery of Small Organic Compounds Targeting PDZ Domains". In Methods in Molecular Biology, 277–89. New York, NY: Springer US, 2021. http://dx.doi.org/10.1007/978-1-0716-1166-1_16.
Shuldau, Mikita A., Artsemi M. Yushkevich, Ivan P. Bosko, Alexander V. Tuzikov e Alexander M. Andrianov. "Generative Autoencoders for Designing Novel Small-Molecule Compounds as Potential SARS-CoV-2 Main Protease Inhibitors". In Communications in Computer and Information Science, 120–36. Cham: Springer International Publishing, 2022. http://dx.doi.org/10.1007/978-3-030-98883-8_9.
Nock, Berthold A., e Theodosia Maina. "Theranostic Radiopeptides in Nuclear Oncology: Design, Preclinical Screening, and Clinical Translation". In Beyond Becquerel and Biology to Precision Radiomolecular Oncology: Festschrift in Honor of Richard P. Baum, 207–24. Cham: Springer International Publishing, 2024. http://dx.doi.org/10.1007/978-3-031-33533-4_22.
A. Elrashedy, Ahmed. "Targeting Inhibitor of Enterococcus faecalis: Insights from Comparative Molecular Dynamics and Binding Free Energy Analyses". In Infectious Diseases. IntechOpen, 2024. http://dx.doi.org/10.5772/intechopen.114329.
Telang, Nitin. "Stem Cell Models: Novel Experimental Approach for Testable Alternatives against Therapy-resistant Breast and Colon Cancer". In Functional Foods for Health Maintenance: Understanding their Role in Cancer Prevention, 384–97. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815179217123010018.
Madala, Sanjay, S. S. V. Kiran K e Burra V. L. S. Prasad. "In Silico Design of Natural Compound-Derived Novel Inhibitors Against RdRP OF SARS-CoV-2". In Current Trends in Drug Discovery, Development and Delivery (CTD4-2022), 142–54. Royal Society of Chemistry, 2023. http://dx.doi.org/10.1039/9781837671090-00142.
Buechter, Douglas D., e George L. Kenyon. "Inhibitors of Non-Protein Kinases". In Pre-Equilibrium Nuclear Reactions, 164–91. Oxford University PressOxford, 1992. http://dx.doi.org/10.1093/oso/9780198517344.003.0005.
Atti di convegni sul tema "Small inhibitory compounds":
Yang, Jiang, e Xintong Wang. "Effect of Thio-Chemicals Molecular Structure for Corrosion Inhibition in CO2 Corrosive Environments". In SPE International Conference on Oilfield Chemistry. SPE, 2023. http://dx.doi.org/10.2118/213847-ms.
Yang, Jiang, e Xintong Wang. "Effect of Thio-Chemicals Molecular Structure for Corrosion Inhibition in CO2 Corrosive Environments". In SPE International Conference on Oilfield Chemistry. SPE, 2023. http://dx.doi.org/10.2118/213848-ms.
Drew, Allison, Lorna Mitchell, Nathalie Rioux, Kerren Swinger, Scott Ribich, Suzanne Jacques-O'hagan, Trupti Lingaraj et al. "Abstract 5376: Identification of the first small molecule PRMT6 inhibitor tool compound". In 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.am2015-5376.
Odarenko, K. V., O. V. Salomatina, N. F. Salakhutdinov, M. A. Zenkova e A. V. Markov. "SEARCH FOR REGULATORY GENES AND SMALL-MOLECULAR INHIBITORS OF THE HIGHLY AGGRESSIVE PHENOTYPE OF GLIOBLASTOMA". In X Международная конференция молодых ученых: биоинформатиков, биотехнологов, биофизиков, вирусологов и молекулярных биологов — 2023. Novosibirsk State University, 2023. http://dx.doi.org/10.25205/978-5-4437-1526-1-279.
Wu, Jianghong, Jie Qian, Lihui Lu e Haiching Ma. "Abstract 5547: Exploration of selective small molecule compounds as caspase inhibitors for treatment of oral mucositis caused by cancer therapy." In Proceedings: AACR 104th Annual Meeting 2013; Apr 6-10, 2013; Washington, DC. American Association for Cancer Research, 2013. http://dx.doi.org/10.1158/1538-7445.am2013-5547.
Panić, Jovana J., Snežana M. Papović, Teona Teodora V. Borović, Nikolet A. Cako Baganj, Sanja D. Belić, Slobodan B. Gadžurić e Milan B. Vraneš. "The hydration and antimicrobial properties of selected imidazole-based ionic liquids with a homologous series of chloride oxyanions". In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.124p.
Kosaka, Hiromichi, Yasuo Watanabe, Michihiro Maemoto, Masamori Sugawara, Miwa Watanabe, Yoko Ono, Yoshisuke Nakasato, Masahiro Matsubara e Ryuichiro Nakai. "Abstract A155: Small molecule metabolic inhibitors, compound A and the derivatives specifically inhibit the cell growth of Ewing's sarcoma cells harbor EWS-FLI1 in vitro and in vivo". In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1535-7163.targ-15-a155.
Chen, L. C., e C. Y. Yang. "Case Report: A Rare Epidermal Growth Factor Receptor (EGFR) H773L/V774M Compound Mutation in Advanced Non-Small Cell Lung Cancer with Poor Response to EGFR Tyrosine Kinase Inhibitor". In American Thoracic Society 2019 International Conference, May 17-22, 2019 - Dallas, TX. American Thoracic Society, 2019. http://dx.doi.org/10.1164/ajrccm-conference.2019.199.1_meetingabstracts.a6993.
Li, Fengzhi, Xiang Ling, Shousong Cao e Qiuying Cheng. "Abstract 4525: Discovery and characterization of a small chemical compound that shows exceptional antitumor activity and targets multiple antiapoptotic proteins in the inhibitor of apoptosis (IAP) and Bcl-2 families". In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-4525.
Rapporti di organizzazioni sul tema "Small inhibitory compounds":
Chamovitz, Daniel A., e Zhenbiao Yang. Chemical Genetics of the COP9 Signalosome: Identification of Novel Regulators of Plant Development. United States Department of Agriculture, gennaio 2011. http://dx.doi.org/10.32747/2011.7699844.bard.