SC14: Advancing Tools and Technologies for Fragment-Based Design
THURSDAY, SEPTEMBER 27, 7:00 - 9:30 PM
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 Discussed:
- Why fragments – pros and cons
- What makes a good fragment, and a good fragment library
- Finding, validating and characterizing low affinity ligands
- The importance of using orthogonal screening methods
- What to do with a fragment – growing, linking, and more
Daniel A. Erlanson, PhD, Co-Founder, Carmot Therapeutics, Inc.
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 two books on fragment-based drug discovery, Dr. Erlanson is an inventor on more than a dozen issued patents and an author of more than forty scientific publications. He is also editor of Practical Fragments, a blog devoted to fragment-based drug discovery.
Mary Harner, PhD, Research Investigator II, Mechanistic Biochemistry, Bristol-Myers Squibb R&D
Dr. Mary Harner is a Research Investigator within the Mechanistic Biochemistry group of Leads Discovery & Optimization at Bristol-Myers Squibb. With a broad training in biophysics and structural biology, Mary uses techniques such as NMR, SPR, TSA and fluorescence to perform fragment screening, hit assessment, and SAR support on relevant targets across multiple therapeutic areas. She also uses biophysical techniques for deeper mechanistic and structural understanding of ligand-binding events. Mary trained as a Damon Runyon Postdoctoral Fellow at Vanderbilt University under the guidance of Stephen W. Fesik, utilizing NMR for fragment screening of challenging targets and X-ray crystallography to drive structure-based drug design efforts. As a graduate student at the University of North Carolina, she studied enzyme conformational dynamics using NMR, X-ray crystallography, and fluorescence methods under the direction of Andrew L. Lee
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