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Cruentaren A binds F1F0 ATP synthase to modulate the Hsp90 protein folding machinery.

Abstract：

:The molecular chaperone Hsp90 requires the assistance of immunophilins, co-chaperones, and partner proteins for the conformational maturation of client proteins. Hsp90 inhibition represents a promising anticancer strategy due to the dependence of numerous oncogenic signaling pathways upon Hsp90 function. Historically, small molecules have been designed to inhibit ATPase activity at the Hsp90 N-terminus; however, these molecules also induce the pro-survival heat shock response (HSR). Therefore, inhibitors that exhibit alternative mechanisms of action that do not elicit the HSR are actively sought. Small molecules that disrupt Hsp90-co-chaperone interactions can destabilize the Hsp90 complex without induction of the HSR, which leads to inhibition of cell proliferation. In this article, selective inhibition of F1F0 ATP synthase by cruentaren A was shown to disrupt the Hsp90-F1F0 ATP synthase interaction and result in client protein degradation without induction of the HSR.

journal_name

ACS Chem Biol

journal_title

ACS chemical biology

authors

Hall JA,Kusuma BR,Brandt GE,Blagg BS

doi

10.1021/cb400906e

subject

Has Abstract

pub_date

2014-04-18 00:00:00

pages

976-85

issue

4

eissn

1554-8929

issn

1554-8937

journal_volume

9

pub_type

杂志文章

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