11th Annual

Fragment-Based Drug Discovery

From Hits to Leads and Lessons Learned

April 20-21, 2016

Fragment-Based Drug Discovery icon  

Fragment-based drug discovery (FBDD) is an approach for finding new drug leads that over the past decade has increasingly been adopted by research departments at biotechnology and pharmaceutical companies. However, rarely is FBDD the only funnel for providing small molecule lead compounds and often medicinal chemists are faced with the challenge of using information from high-throughput as well as other efforts to optimize and develop compounds with the best drug potential. But with more than thirty compounds in clinical trials and at least one drug on the market whose origins can be traced to fragment-based approaches, there is a wealth of experience and information to be shared for moving the field forward. Join fellow biophysical and medicinal chemists to discuss and debate pitfalls, solutions and best practices in this growing area of drug discovery.

Preliminary Agenda

Case Studies

Fragment-Screening Antibacterial Targets Using Surface Plasmon Resonance Methods

Adam Renslo, Ph.D., Associate Professor, Department of Pharmaceutical Chemistry, University of California San Francisco

Fragment-Based Discovery of Novel MAP4K4 Inhibitors: Tales of Two Fragments

Huifen Chen, Ph.D., Senior Scientist, Discovery Chemistry, Genentech

Inhibition by Destabilization: Allosteric Inhibitors of a Calcium-Dependent Enzyme Identified by Fragment Screening

Mary Harner, Ph.D., Research Investigator, Mechanistic Biochemistry, Bristol-Myers Squibb

Best Practices

Building FBDD Infrastructure at Takeda

Xiaolun Wang, Ph.D., Senior Scientist, Medicinal Chemistry, Takeda San Diego

Combining Biophysical Methods to Improve the Robustness of FBLD

Ben Davis, Ph.D., Research Fellow, Biology, Vernalis

New Approaches

Protein-Observed Fluorine NMR for Fragment Screening

William Pomerantz, Ph.D., Assistant Professor, Department of Chemistry, University of Minnesota

A Fully Automated Pipeline for Fragment Based Screening through Macromolecular Crystallography

Jose A. Marquez, Ph.D., Team Leader, Head of Crystallization Facility, Grenoble Outstation, European Molecular Biology Laboratory

A New Approach for Quality-Control Screening of Fragment Libraries

Yutao Jiang, M.S., Senior Research Associate, Medicinal Chemistry, Genentech

X-ray and Activity Fragment Screening across Subfamilies of Lysine Demethylases and Ribosomal Hydroxylases for Active-site Characterization

Radek Nowak, Ph.D. Student, Laboratory of Udo Oppermann, Structural Genomics Consortium, University of Oxford

For more details on the conference, please contact:
Anjani Shah, Ph.D.
Conference Director Cambridge Healthtech Institute
Phone: (914) 723-0255
Email: ashah@healthtech.com

For partnering & sponsorship information, please contact:
Carolyn Benton
Business Development Manager
Cambridge Healthtech Institute
Phone: (+1) 781-972-5412
Email: cbenton@healthtech.com