Geldanamycin, the first discovered Hsp90 inhibitor.[1]
Class identifiers
Use
Antineoplastic
Biological target
Hsp90
Legal status
In Wikidata
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 survival of cancer cells, these substances may have therapeutic benefit in the treatment of various types of malignancies.[2] Furthermore, a number of Hsp90 inhibitors are currently undergoing clinical trials for a variety of cancers.[3] Hsp90 inhibitors include the natural products geldanamycin, Retaspimycin hydrochloride (IPI 504, a hydroquinone hydrochloride salt derivative of 17-AAG) and radicicol as well as semisynthetic derivatives 17-N-Allylamino-17-demethoxygeldanamycin (17AAG).
^Whitesell L, Mimnaugh EG, De Costa B, Myers CE, Neckers LM (August 1994). "Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation". Proc. Natl. Acad. Sci. U.S.A. 91 (18): 8324–8. doi:10.1073/pnas.91.18.8324. PMC 44598. PMID 8078881.
^Porter JR, Fritz CC, Depew KM (June 2010). "Discovery and development of Hsp90 inhibitors: a promising pathway for cancer therapy". Curr Opin Chem Biol. 14 (3): 412–20. doi:10.1016/j.cbpa.2010.03.019. PMID 20409745.
^Kim YS, Alarcon SV, Lee S, Lee MJ, Giaccone G, Neckers L, Trepel JB (2009). "Update on Hsp90 inhibitors in clinical trial". Curr Top Med Chem. 9 (15): 1479–92. doi:10.2174/156802609789895728. PMC 7241864. PMID 19860730.
An Hsp90inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for...
example, the Hsp90inhibitor geldanamycin has been used as an anti-tumor agent. The drug was originally thought to function as a kinase inhibitor but was subsequently...
A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation...
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...
drugs. Hence small molecule inhibitors of HSPs, especially Hsp90 show promise as anticancer agents. The potent Hsp90inhibitor 17-AAG was in clinical trials...
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...
Protein 90 (HSP90). HSP90 is key in protein folding and maturation. TopoTarget is currently looking for small molecule drugs that inhibitHSP90 function...
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...
et al. (June 2018). "Targeted cancer therapy through 17-DMAG as an Hsp90inhibitor: Overview and current state of the art". Biomedicine & Pharmacotherapy...
GM, Lock RB, Liu T (May 2016). "The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression...
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...
July 2015. Additionally, luminespib (AUY922) is a novel intravenous Hsp90inhibitor with the potential to target a range of cancers, which arose from a...
hypoxia and heat. The small molecule Hsp90inhibitor, PU-H71, has been found to have a preferential binding to Hsp90 when it is in the highly integrated...
combination with BRAF inhibitors to treat melanoma CDK inhibitors, e.g. PD-0332991, LEE011 in clinical trials Hsp90inhibitors, some in clinical trials...
rheostat that modulates signaling rather than as a binary on-off switch. HSP90inhibitor NVP-BEP800 has been described to affect stability of LYN kinase and...
Archived from the original on 2012-04-16. Retrieved 2012-04-17. "Exelixis HSP90inhibitor XL888". Archived from the original on 2016-09-18. Retrieved 2016-09-16...
1002/cber.187600902133. Sidera, K.; Patsavoudi, E. (January 2014). "HSP90inhibitors: current development and potential in cancer therapy". Recent Patents...
[citation needed] Novobiocin has been shown to weakly inhibit the C-terminus of the eukaryotic Hsp90 protein (high micromolar IC50). Modification of the...
towards the Hsp90inhibitors. Mollapour’s laboratory has discovered the tumor suppressor TSC1 and FNIPs function as the new co-chaperones of Hsp90. These two...
that blocks the CLU mRNA transcript, enhanced heat-shock protein 90 (HSP90) inhibitor activity by suppressing the heat-shock response in castrate-resistant...
functions to bind to DNA gyrase and inhibits ATPase activity. It acts as a competitive inhibitor and specifically inhibitsHsp90 and TopII. Novobiocin has been...
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