Biochm/Chem 597A, Fall 2002 (3 credits)

Instructors: Arnie Hagler (Adjunct Professor Chemistry) ( and Joanna Swain (Biochemistry) (; 5-1250)

Class Meeting Time/Place: Thursdays 4:00-5:30 pm, room 703 LGRT-A.

Weekly Discussion Meeting: Tuesdays 11:30 a.m.-12:30 p.m., room 1033 LGRT

Grade will be based on attendance and participation in class discussion, and a paper/project.

Outline of course: Drug design and discovery are of critical importance in human health care. Successes in drug design have been dependent on insights and advances from the combined use of chemical and biological research. Computational approaches have become a centerpiece of rational drug design and are generally combined with structural information derived from macromolecular crystallography and nuclear magnetic resonance. More recently, new methods of synthesizing very large libraries of potentially bioactive small molecules through combinatorial methods have brought screening strategies into increasingly important roles in drug discovery. Complementary biological innovations have been required to test the large arrays of molecules. We are currently witnessing an explosion of genomic information, which is revolutionizing the way drug discovery takes place. Moreover, new fields have arisen such as pharmacogenetics and pharmacogenomics and are touching the goals and guiding principles of drug design and discovery.

This course will survey the current picture in pharmaceutical research, including how targets are selected, how the rational and combinatorial methods are harnessed, as well as how the industry is evolving in this post-genomic era. The instructors will provide background and introduce various topics, which will be discussed by a series of invited lecturers who are active in drug design and discovery.

Students will read background material provided by the visiting lecturers. The instructors will pose questions and lead discussions analyzing the material presented in the lectures. Students will pick a topic for a paper by Thanksgiving, and once the topic is approved will prepare a ten page paper to be submitted by the last day of classes.


9/5/02 Joanna Swain
Introduction to course; background on drug-receptor interactions
9/12/02 Sherin Abdul-Meguid, Suntory Pharmaceuticals Target Selection
9/19/02 Chris Lipinski, Adjunct Senior Research Fellow, Pfizer Inc. Making leads into drugs
9/26/02 Ray Salemme, President & CSO, 3-Dimensional Pharmaceuticals Inc. Screening and focused libraries: the Discovery Works platform for drug discovery at 3D Pharmaceuticals
10/3/02 Mark Wentland, Professor of Chemistry, Rensselaer Polytechnic Institute High-throughput screening and combinatorial chemistry
10/10/02 Christine Humblet, Senior Director of Informatics, Pfizer Inc. Informatics at Pfizer
10/17/02 TBA  
10/24/02 Jonathan Greer, Senior Project Leader, Abbott Laboratories Design of highly potent ligands through crystallographic screening
10/31/03 TBA
11/7/02 Tomi Sawyer, Ariad Pharmaceuticals Inc. Cell signalling and breakthrough medicines
11/14/02 Dennis Keith, Vice President of Chemical Development, Cubist Pharmaceuticals Design of antibiotics and the challenges of resistance
11/21/02 Mark Murcko, Chief Scientific Officer, Vertex Pharmaceuticals Inc. Chemogenomics and In Silico ADME/Tox
12/5/02 John Talley, Chief Scientific Officer, Microbia Development of COX-2 Inhibitors
12/12/02 Arnie Hagler, Joanna Swain Review and discussion

***Field trip to tour Pfizer's Groton, CT facility to be scheduled.***