| Hsp90 inhibitor | |
|---|---|
| Drug class | |
 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.