An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for...
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example, the Hsp90 inhibitor geldanamycin has been used as an anti-tumor agent. The drug was originally thought to function as a kinase inhibitor but was subsequently...
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that most amenable to inhibitor generation. To date, there are 23 active Hsp90 inhibitor oncology trials, and 13 HSP90 inhibitors are currently undergoing...
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it is a resorcinylic isoxazole amide Luminespib is an inhibitor of heat shock protein 90 (Hsp90), which is a chaperone protein that plays a role in the...
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A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation...
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TopoTarget (section HSP90 inhibitors)
Protein 90 (HSP90). HSP90 is key in protein folding and maturation. TopoTarget is currently looking for small molecule drugs that inhibit HSP90 function...
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drugs. Hence small molecule inhibitors of HSPs, especially Hsp90 show promise as anticancer agents. The potent Hsp90 inhibitor 17-AAG was in clinical trials...
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Fuhrmann-Stroissnigg H, Niedernhofer LJ, Robbins PD (2018-05-03). "Hsp90 inhibitors as senolytic drugs to extend healthy aging". Cell Cycle. 17 (9). Informa...
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protein 1 (FNIP1) functions as a co-chaperone which inhibits the ATPase activity of the chaperone Hsp90 (heat shock protein-90) and decelerates its chaperone...
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Lundsten S, Spiegelberg D, Stenerlöw B, Nestor M (December 2019). "The HSP90 inhibitor onalespib potentiates 177Lu‑DOTATATE therapy in neuroendocrine tumor...
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et al. (June 2018). "Targeted cancer therapy through 17-DMAG as an Hsp90 inhibitor: Overview and current state of the art". Biomedicine & Pharmacotherapy...
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GM, Lock RB, Liu T (May 2016). "The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression...
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kinase inhibitor drugs that are in clinical trials include bosutinib, bafetinib, Saracatinib(AZD-0530), XLl-999, KX01 and XL228. HSP90 inhibitor NVP-BEP800...
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combination with BRAF inhibitors to treat melanoma CDK inhibitors, e.g. PD-0332991, LEE011 in clinical trials Hsp90 inhibitors, some in clinical trials...
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"Taiho Pharmaceutical Obtains Approval to Manufacture and Market HSP90 inhibitor Jeselhy® Tablets 40 mg (Pimitespib) for Gastrointestinal Stromal Tumor...
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Chaperone (protein) (section Hsp90)
classified based on their observed molecular weights into Hsp60, Hsp70, Hsp90, Hsp104, and small Hsps. The Hsp60 family of protein chaperones are termed...
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Archived from the original on 2012-04-16. Retrieved 2012-04-17. "Exelixis HSP90 inhibitor XL888". Archived from the original on 2016-09-18. Retrieved 2016-09-16...
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hypoxia and heat. The small molecule Hsp90 inhibitor, PU-H71, has been found to have a preferential binding to Hsp90 when it is in the highly integrated...
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rafts. Masitinib also inhibits Lck, which may have some impact on its therapeutic effects in canine mastocytoma. HSP90 inhibitor NVP-BEP800 has been described...
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rheostat that modulates signaling rather than as a binary on-off switch. HSP90 inhibitor NVP-BEP800 has been described to affect stability of LYN kinase and...
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(June 2004). "Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms". Chem. Biol. 11 (6): 775–85. doi:10.1016/j.chembiol...
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Cyclin-dependent kinase 4 (redirect from CDK4 inhibitor)
(June 1996). "Mammalian p50Cdc37 is a protein kinase-targeting subunit of Hsp90 that binds and stabilizes Cdk4". Genes & Development. 10 (12): 1491–1502...
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antibiotic that inhibits the function of Hsp90 (Heat Shock Protein 90) by binding to the unusual ADP/ATP-binding pocket of the protein. HSP90 client proteins...
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July 2015. Additionally, luminespib (AUY922) is a novel intravenous Hsp90 inhibitor with the potential to target a range of cancers, which arose from a...
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1002/cber.187600902133. Sidera, K.; Patsavoudi, E. (January 2014). "HSP90 inhibitors: current development and potential in cancer therapy". Recent Patents...
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Novobiocin (category Topoisomerase inhibitors)
[citation needed] Novobiocin has been shown to weakly inhibit the C-terminus of the eukaryotic Hsp90 protein (high micromolar IC50). Modification of the...
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monorden, is a natural product that binds to Hsp90 (Heat Shock Protein 90) and alters its function. HSP90 client proteins play important roles in the regulation...
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functions to bind to DNA gyrase and inhibits ATPase activity. It acts as a competitive inhibitor and specifically inhibits Hsp90 and TopII. Novobiocin has been...
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that blocks the CLU mRNA transcript, enhanced heat-shock protein 90 (HSP90) inhibitor activity by suppressing the heat-shock response in castrate-resistant...
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sometimes susceptible to drugs that inhibit chaperones and disrupt proteostasis, such as Hsp90 inhibitors or proteasome inhibitors. Furthermore, cancer cells tend...
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