Structure-based Lead Generation and Optimization
About the Lead Generation Event
Once a protein target has been validated for therapeutic intervention, the challenge is to find lead molecules that will ligand to the target in a productive fashion. In the last decade, high throughput screening (HTS) has been used as a standard method for generating chemical matter with some notable successes. However, where structural information is available and HTS is not readily applicable, an alternate approach to lead finding can be taken.
Come join Henry W. Pauls from Campbell Family Institute for Breast Cancer Research, Therapeutics, as he discusses:
- Several protein structure based strategies for finding leads
- How structural information can significantly advance lead optimization through models and co-complex crystal structures
Dr Pauls’ presentation will highlight pharma and biotech industry cases and lay the groundwork for a discussion on the use of structure-based design on lead generation and optimization in the search for novel therapeutic compounds.
Presenter: Dr. Henry W. Pauls
Director, Medicinal Chemistry
Campbell Family Institute for Breast Cancer Research, Therapeutics
Chief Scientific Officer & Vice President, Research Programs
DATE | TIME | LOCATION
August 31, 200611:30AM - 1:00PM
MaRS Centre
101 College St, Toronto
ABOUT THE PRESENTER
Dr. Pauls received his Ph. D. from Duke University where he explored the use of synthons from the carbohydrate chiral pool for natural products synthesis. This was followed by stints at Syntex's Bioorganic Chemistry Department (NSERC Postdoctoral Fellowship) and Allelix Biopharmaceuticals in Canada. During this time he was involved in the design of mechanism-based inhibitors of serine and cysteine proteases.
In 1990 he joined Rhone-Poulenc Rorer (currently Sanofi-Aventis-New Jersey site) where he held Section Manager and Chemistry Team Leader positions in Medicinal Chemistry. Dr. Pauls' research activities at Aventis centered on the structure based design and synthesis of novel inhibitors of trypsin like serine protease. As leader of the factor Xa and trypase projects he was involved in the discovery and development of novel clinical candidates for the treatment of thrombosis and asthma respectively.
Henry returned to Canada in 2003 to join Affinium Pharmaceuticals as Senior Director of Medicinal Chemistry. Affinium's mandate was the structure based discovery and development of new classes of antibacterial agents. Novel enoyl-ACP reductase inhibitors identified during his tenure as project leader have been selected for clinical microdosing studies. Dr. Pauls recently joined the Campbell Family Institute for Breast Cancer Research as Director of Medicinal Chemistry in the therapeutics group.
ABOUT THE DRUG DEVELOPMENT DISCUSSION GROUP
The Drug Development Discussion Group (DDD Group) is an informal moderated forum bringing together research professionals and clinicians interested in drug development.
Think of DDD Group as a Journal Club focused on global drug development issues; a place to hear candid comments from the practitioners in the field, a chance to debate and develop a rapport with industry and academic professionals you do not necessarily deal with on a daily basis.
If you are interested in moderating future sessions please contact Veronika Litinski (vlitinski@marsdd.com).
Click here for more information about the Drug Development Discussion Group (DDD Group).
UPCOMING EVENTS
PAST EVENTS
- March 27, 2008
MaRS Drug Development Discussion Group - Structure-Guided Discovery Without Structures: Computer-aided design of GPCR ligands - February 27, 2008
MaRS Drug Development Discussion Group - Formulation: Giving new life to naturally occurring un-patentable compounds - January 25, 2008
Drug Development Discussion Group - Novel therapeutic targets for preventing bone loss in osteolytic disease - December 18, 2007
MaRS Drug Development Discussion Group - Outsourcing Preclinical Development - October 23, 2006
MaRS Drug Development Discussion Group - Chance and Necessity in Drug Discovery: The case history of calcimimetic drugs - August 31, 2006
Drug Development Discussion Group - Structure-based Lead Generation and Optimization - June 29, 2006
Drug Development Discussion Group - Exploratory IND - April 27, 2006
Drug Discussion Group - BioMarkers in Clinical Trials
