Thursday April 22, 6:30 - 9:00pm
SC9: Advancing Tools and Technologies for Fragment-Based Design*
Instructors: Daniel A. Erlanson, Ph.D., Co-Founder, Carmot Therapeutics, Inc.
Edward R. Zartler, Ph.D., President & CSO, Quantum Tessera Consulting
This course aims to introduce the fundamentals of Fragment-based Lead Discovery (FBLD) to attendees. The first section will focus on the concepts of using fragments for hit generation. Special emphasis will be placed on practical pitfalls and the many ways to advance fragments to leads and drugs. The second part of the course will discuss the variety of fragment screening methods and when they are best applied. The composition of fragment libraries will also be discussed in detail. The attendees should come away from this course with a solid understanding of what FBLD is and how to apply it.
Topics to be covered:
- Why fragments – pros and cons?
- What makes a good fragment?
- What to do with a fragment – growing, linking, and more
- Design of fragment libraries
- Importance of using orthogonal/multiple screening methods
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 also editor in chief 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. He is also editor of Practical Fragments (with Dr. Erlanson) a blog devoted to fragment-based drug discovery.
*Separate registration is required