SC8: Targeting Protein-Protein Interactions: Biophysical Approaches

Monday, September 21, 3:30-6:30 pm

Protein-protein interactions (PPIs) represent a large but largely untapped class of biological targets covering virtually every therapeutic area. Despite several success stories, many researchers still consider PPIs to be “undruggable.” This course will provide attendees with an overview of how to discover small-molecule inhibitors of PPIs. Attendees will also learn about potential pitfalls and what not to do.

Topics to be covered will include:

• How to evaluate the feasibility of PPIs: unknown knowns and other dangers when targeting PPIs (Erlanson, 30 min.)  
• What biophysical techniques to use (Zartler, 45 min.)  
• How fragment-based lead discovery can improve success rates against particularly challenging PPIs (Zartler, 30 min.)  
• PPI success stories (Erlanson, 45 min.)  

Instructors:

Daniel A. Erlanson, Ph.D., Co-Founder and President, Carmot Therapeutics, Inc.

Edward R. Zartler, Ph.D., President & CSO, Quantum Tessera Consulting

Dr. Daniel A. Erlanson is the co-founder of Carmot Therapeutics, Inc. a small-molecule drug discovery company applying fragment-based approaches to a variety of therapeutic targets. Prior to Carmot, Dr. Erlanson spent a decade developing fragment-based drug discovery technologies at Sunesis Pharmaceuticals, which he joined at the company's inception. Before Sunesis, he was an NIH postdoctoral fellow with James A. Wells at Genentech. Dr. Erlanson earned his PhD in chemistry from Harvard University in the laboratory of Gregory L. Verdine and his BA in chemistry from Carleton College. As well as co-editing the first book on fragment-based drug discovery, Dr. Erlanson is an inventor on more than a dozen issued patents and published patent applications and an author of more than two dozen scientific publications. He is co-editor of a recently published book by Wiley-VCH called 'Fragment-based Drug Discovery: Lessons and Outlook'. And Dr. Erlanson is editor in chief (with Dr. Zartler) of Practical Fragments, a blog devoted to fragment-based drug discovery.

Dr. Edward R. Zartler is the Chief Scientific Officer of Quantum Tessera Consulting. Dr. Zartler works with clients developing practical applications of Fragments and biophysical methods leveraging his decade in the pharmaceutical industry (at Merck and Eli Lilly). While at Eli Lilly, Dr. Zartler implemented and led all fragment efforts there and coined the term "Fragonomics." Prior to joining Lilly, Dr. Zartler did his post-doctoral training with James Prestegard at the University of Georgia. He earned his Ph.D. from the University of Pennsylvania under Ponzy Lu and his B.A. in Chemistry from Goucher College. Dr. Zartler is co-editor of the second book on Fragment-based Drug Discovery and coming in 2016, Applied Biophysics in Drug Discovery. He is also editor (with Dr. Erlanson) of Practical Fragments, a blog devoted to fragment-based drug discovery.

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