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Exploiting protein homeostasis for cancer therapy

Deshaies, Raymond and Chou, Tsui-Fen and Li, Jing and Mackinnon, Andy and Parlati, Francesco (2014) Exploiting protein homeostasis for cancer therapy. FASEB Journal, 28 (1). 472.2. ISSN 0892-6638. https://resolver.caltech.edu/CaltechAUTHORS:20150205-100227097

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Abstract

Cancer cells often harbor numerous genomic insults and an altered metabolism. Together, these changes impede protein folding and assembly. As a result, cancer cells can have an elevated dependence on mechanisms that sustain protein assembly and quality control. To test whether cancer cells are hypersensitive to inhibition of protein homeostasis pathways, we seek to develop small molecule antagonists of ubiquitin system enzymes involved in protein quality control. In particular, we have been pursuing the proteasome, the COP9-Signalosome, and the ubiquitin-selective ‘segregase’ p97/VCP. Over the past 5 years we have carried out HTS against these targets through the NIH’s Molecular Libraries Program. Analysis of structure-activity relationships for the resulting hits has led to enzyme inhibitors with IC50 ~0.1-1 μM that are active in cells. These compounds are useful tools for basic research and represent starting points for drug discovery. My talk will focus on our recent progress in developing novel small molecule probes for UPS enzymes.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://www.fasebj.org/content/28/1_Supplement/472.2PublisherArticle
http://experimentalbiology.org/2014/home.aspxOrganizationConference Website
ORCID:
AuthorORCID
Deshaies, Raymond0000-0002-3671-9354
Chou, Tsui-Fen0000-0003-2410-2186
Additional Information:© 2014 Federation of American Societies for Experimental Biology.
Issue or Number:1
Record Number:CaltechAUTHORS:20150205-100227097
Persistent URL:https://resolver.caltech.edu/CaltechAUTHORS:20150205-100227097
Official Citation:Raymond Deshaies, Tsui-Fen Chou, Jing Li, Andy Mackinnon, and Francesco Parlati Exploiting protein homeostasis for cancer therapy (472.2) FASEB J April 2014 28:472.2
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:54415
Collection:CaltechAUTHORS
Deposited By: Tony Diaz
Deposited On:05 Feb 2015 20:58
Last Modified:03 Oct 2019 07:57

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