Emerging Hsp90 Inhibitors: From Discovery to Clinic

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Emerging Hsp90 Inhibitors: From Discovery to Clinic



Anti-Cancer Agents in Medicinal Chemistry, 6(1): 1-8.

Author(s): G. Chiosis, A. Rodina and K Moulick.

Affiliation: Memorial Sloan-Kettering Cancer Center, 1275 York Ave., Box 482, New York, NY10021, USA;

Abstract

Hsp90 is a chaperone with important roles in maintaining transformation and in elevating the survival and growth potential of cancer cells. Activation of signaling pathways mediated by Hsp90 protein clients is necessary for cell proliferation, regulation of cell cycle progression and apoptosis. Additionally, gain-of-function mutations responsible for transformation often require Hsp90 for the maintenance of their folded, functionally active conformations. These characteristics promise Hsp90 as an important target in cancer therapy and prompt for the identification, development and clinical translation of small molecule inhibitors of the chaperone. This review intends to update the reader on the status of several existing and emerging classes of direct inhibitors of Hsp90 ATPase activity.

Keywords:

17AAG, 17DMAG, PU-class Hsp90 inhibitors, radicicol and derivatives, 3,4-diarylpyrazoles, anti-cancer therapeutics.



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Article Details

Volume: 6
Issue Number: 1
First Page: 1
Last Page: 8
Page Count: 8
DOI: 10.2174/187152006774755483
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