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Issue 10, 2013
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Targeting heat-shock-protein 90 (Hsp90) by natural products: geldanamycin, a show case in cancer therapy

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Abstract

Covering: 2005 to 2013

In this review recent progress in the development of heat shock proteins (Hsp90) in oncogenesis is illuminated. Particular emphasis is put on inhibitors such as geldanamycin and analogues that serve as a natural product show case. Hsp90 has emerged as an important target in cancer therapy and/or against pathogenic cells which elicit abnormal Hsp patterns. Competition for ATP by geldanamycin and related compounds abrogate the chaperone function of Hsp90. In this context, this account pursues three topics in detail: a) Hsp90 and its biochemistry, b) Hsp90 and its role in oncogenesis and c) strategies to create compound libraries of structurally complex inhibitors like geldanamycin on which SAR studies and the development of drugs that are currently in different stages of clinical testing rely.

Graphical abstract: Targeting heat-shock-protein 90 (Hsp90) by natural products: geldanamycin, a show case in cancer therapy

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Publication details

The article was received on 09 Feb 2013 and first published on 12 Aug 2013


Article type: Review Article
DOI: 10.1039/C3NP70012G
Citation: Nat. Prod. Rep., 2013,30, 1299-1323
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    Targeting heat-shock-protein 90 (Hsp90) by natural products: geldanamycin, a show case in cancer therapy

    J. Franke, S. Eichner, C. Zeilinger and A. Kirschning, Nat. Prod. Rep., 2013, 30, 1299
    DOI: 10.1039/C3NP70012G

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