Wednesday, November 07, 2018
4:00 PM - 5:00 PM
Noyes 153 (J. Holmes Sturdivant Lecture Hall)

Organic Chemistry Seminar

Tackling Challenging Drug Targets, a Biophysical Perspective
Michelle Arkin, Professor, Department of Pharmaceutical Chemistry, UC San Francisco,
Speaker's Bio:
Michelle Arkin is a Professor in Pharmaceutical Chemistry and the co-Director of the Small Molecule Discovery Center at UCSF and an adjunct professor at the Buck Institute for Aging Research. Michelle's research interests include developing biological tools and drug leads for cancer and neurodegenerative diseases and designing compounds to modulate the function of allosterically regulated enzymes and protein-protein interactions (PPI). As co-director of the SMDC, Michelle oversees the high-throughput screening operation and collaborates with many academic and pharmaceutical laboratories to tackle challenging problems in drug discovery. Michelle has been very active in the academic drug discovery community. She is the current president of the board of directors for the Academic Drug Discovery Consortium, serves as PI for the UCSF Center in the NCI Chemical Biology Consortium, and is on the editorial board of the Assay Guidance Manual and Current Protocols in Chemical Biology. She recently completed a term as reviews editor at Cell Chemical Biology. Michelle earned her Ph.D. in chemistry at Caltech in Jackie Barton's lab and then held a Daymon Runyon postdoctoral fellowship with Jim Wells at Genentech. She was among the first scientists at Sunesis Pharmaceuticals, where she developed inhibitors of PPI, including lifitigrast, an FDA approved drug for dry eye (SARcode/Shire). From 2005 to 2007, she was the Associate Director of Cell Biology at Sunesis and led the translational science team for Vosaroxin, an anti-cancer agent in phase 3 clinical trials. She has been at UCSF since 2007.

Many potential drug targets are known to be relevant for disease, but have been 'undruggable' by current approaches.  Our lab seeks to understand to what extent this failure has been due to the features of the biological target vs the methodologies used to discover small-molecule modulators.  In particular, we have focused on protein-protein interactions and the larger networks controlled by these interactions.  This seminar will describe our discoveries of first-in-class compounds with unusual mechanisms for inhibiting 'challenging' targets, including allosteric inhibitors of p97, protein-protein stabilizing compounds, and selective covalent inhibitors of proteases.

For more information, please phone 626-395-6016 or email aluymes@caltech.edu or