PMID: 22338602Feb 18, 2012Paper

Heat shock protein 90 inhibitors as therapeutic agents

Recent Patents on Anti-cancer Drug Discovery
Isabel Gomez-MonterreyPietro Campiglia

Abstract

The molecular chaperone heat shock protein 90 (HSP90) is essential for the folding stability, intracellular disposition and proteolytic turnover of many of the key regulators of cell growth, differentiation and survival. These essential functions are used by the cells during the oncogenesis process to allow the tumor transformation and facilitate the rapid somatic evolution. Inhibition of HSP90 would provide combinatorial blockade of a range of oncogenic pathways, antagonizing many of the hallmark traits of cancer. Several HSP90 inhibitors are currently under clinical trial investigation for the treatment of cancer. This review summarizes the current state and progress achieved in the development of HSP90 inhibitors targeting the N-terminal ATP pocket, C-terminal domain, different compartmentalized isoforms, and protein (cochaperones and/or client proteins)/HSP90 interactions. In the context of drug discovery, the most relevant patents which appeared recently in the literature are discussed as well.

Citations

Nov 16, 2012·PloS One·Antonio Luis de Oliveira Almeida PetersenPatrícia Sampaio Tavares Veras
Apr 3, 2016·Chemistry : a European Journal·Katherine M ByrdBrian S J Blagg
Feb 22, 2014·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Hongming LiuBaojian Wu
Sep 30, 2014·Trends in Pharmacological Sciences·Tony TaldoneGabriela Chiosis
Jul 14, 2018·Journal of Veterinary Pharmacology and Therapeutics·Fazul NabiJiakui Li
Jun 6, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yajun LiuHecheng Wang

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