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Exploiting protein homeostasis for cancer therapy

Deshaies, Raymond and Li, Jing (2015) Exploiting protein homeostasis for cancer therapy. In: 250th American Chemical Society National Meeting & Exposition, August 16-20, 2015, Boston, MA.

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Cancer cells often harbor numerous genomic insults and an altered metab. 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 mol. 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 Mol. Libraries Program. Anal. 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 compds. 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 mol. probes for UPS enzymes.

Item Type:Conference or Workshop Item (Paper)
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Deshaies, Raymond0000-0002-3671-9354
Additional Information:© 2015 American Chemical Society.
Record Number:CaltechAUTHORS:20151021-133303640
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Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:61389
Deposited By: Tony Diaz
Deposited On:21 Oct 2015 20:44
Last Modified:03 Oct 2019 09:07

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