Kevan Shokat, University of California San Francisco, "Chemical Genetic Investigations of Protein and Lipid Kinase Signaling"

Jan 25 2011, 11:00 am
Distinguished Lecture Series Guest Speaker: 

Kevan Shokat

Professor and Chair, Department Cellular and Molecular Pharmacology, University of California San Francisco
Professor, Department of Chemistry, University of California, Berkeley
Investigator, Howard Hughes Medical Institute

Date & Time: 
Tuesday, January 25, 2011, 11:00AM
Klaus 1116E
Melissa Kemp
Kinases are highly regulated enzymes with diverse mechanisms controlling their catalytic output. Inhibitor discovery efforts for kinases have produced ATP-competitive compounds, allosteric regulators, irreversible binders, and highly specific inhibitors. These distinct classes of small molecules have revealed many novel aspects about kinase-mediated signaling and some have progressed from simple tool compounds into clinically validated therapeutics. My presentation will explore several small-molecule inhibitors for kinases highlighting elaborate mechanisms by which kinase function is modulated. A complete surprise of targeted kinase drug discovery has been discovery of ATP-competitive inhibitors that behave as agonists, rather than antagonists, of their direct kinase target. These studies hint at a connection between ATP binding site occupancy and networks of communication that are independent of kinase catalysis. Indeed, kinase inhibitors have been found that induce changes in protein localization, protein-protein interactions, and even enhancement of catalytic activity of the target kinase. The relevance of these findings to the therapeutic efficacy of kinase inhibitors and to the future identification of new classes of drug targets will be discussed.
Additional Info: 

Kevan Shokat has developed chemical methods to decipher the role of individual kinases and their cellular signaling networks. His goals are to understand each kinase's role in the body and to learn which kinases should be targeted to treat diseases such as cancer and immune dysfunction.

UCSF Faculty Website
UC Berkeley Faculty Website
Lab Website
HHMI Investigator Page
Kevan Shokat Flier.jpg

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