SC4: FRAGMENT-BASED DRUG DESIGN: TOOLS AND TECHNIQUES

MONDAY, AUGUST 24 | 2:00 - 5:00 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 Covered:

• Pros and cons of fragment-based approaches
• Properties of 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

Instructors:

Ben Davis, PhD, Research Fellow, Biology, Vernalis Research

Dr. Ben Davis is a Research Fellow at Vernalis Research, a biotech company based in Cambridge, UK which has been at the forefront of fragment-based approaches since 1998. An NMR spectroscopist and biophysicist by training, his current research focus is the development of biophysics and FBLD methods for challenging therapeutic targets and systems. Dr Davis studied for his PhD in protein folding and molecular interactions with Professor Alan Fersht at Cambridge University, and then studied the interactions of small molecules with proteins and RNA. He has over 20 years’ experience in the drug discovery industry. He has contributed to seven books over the last decade and is an author on more than forty scientific publications. He is a frequent speaker at scientific conferences and has been running FBLD training workshops since 2007.

Daniel Erlanson, PhD, Vice President, Chemistry, Frontier Medicines

Dr. Daniel Erlanson is Vice President of Chemistry at Frontier Medicines, a pre-clinical stage biopharmaceutical company using chemoproteomics to discover and pharmacologically target new binding pockets (or hotspots) on cancer-causing proteins, making them – at long last – accessible to therapeutic intervention by small-molecule drugs. Before recently joining Frontier Medicines, Dr. Erlanson co-founded 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.

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