Bench to Bedside: Chemistry of Health Care

Fragment-based Lead Discovery (#145)

Fragment-based lead discovery (FBLD) is a powerful method to identify drug leads. While typical high throughput screening relies on libraries containing a million or more drug-sized molecules, fragment-based screening relies on smaller libraries of perhaps a few thousand small molecular fragments, each only half the size of a typical drug molecule, generally less than 300 Daltons. Because fragments are small, the techniques to find and validate them must be sensitive, specific, and, often, specialized. Moreover, it can be difficult to improve the potency of a fragment from a millimolar hit to a nanomolar drug lead.

Despite these challenges, FBLD has become widely embraced by the pharmaceutical and biotech industries, as well as academia. The approach is responsible for putting more than 28 drugs into clinical trials, including the anticancer drug vemurafenib, approved in 2011.

This symposium will include all aspects of FBLD, from library design and the various biophysical, biochemical, and computational fragment-identification methods, through fragment-to-lead campaigns, and finally, lead optimization and success stories. Contributors from organizations that have not previously presented at fragment meetings are particularly welcome.
Last update: Dec 28, 2015