PROGRAM COURSES - DRUG DESIGN 2002
Biochm/Chem 597A, Fall 2002 (3 credits)
Instructors: Arnie Hagler (Adjunct Professor
and Joanna Swain (Biochemistry) (firstname.lastname@example.org;
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
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.
to course; background on drug-receptor interactions
||Chris Lipinski, Adjunct
Senior Research Fellow, Pfizer Inc.
||Making leads into
President & CSO, 3-Dimensional Pharmaceuticals Inc.
and focused libraries: the Discovery Works platform for drug
discovery at 3D Pharmaceuticals
Wentland, Professor of Chemistry, Rensselaer Polytechnic Institute
screening and combinatorial chemistry
Senior Director of Informatics, Pfizer Inc.
||Jonathan Greer, Senior
Project Leader, Abbott Laboratories
||Design of highly potent
ligands through crystallographic screening
||Tomi Sawyer, Ariad
||Cell signalling and
||Dennis Keith, Vice
President of Chemical Development, Cubist Pharmaceuticals
||Design of antibiotics
and the challenges of resistance
||Mark Murcko, Chief
Scientific Officer, Vertex Pharmaceuticals Inc.
In Silico ADME/Tox
Chief Scientific Officer, Microbia
of COX-2 Inhibitors
Hagler, Joanna Swain
***Field trip to tour Pfizer's Groton, CT facility to be scheduled.***