Dr. Brian Shoichet
Prof. of Pharmaceutical Chemistry
University of California, San Francisco
Brian Shoichet received his BSc in Chemistry from MIT (1985). In doctoral work with Tack Kuntz (UCSF), he co-developed the first molecular docking screens, applying these to lead discovery against thymidylate synthase, a cancer target (Shoichet et al., Science 1993). As a Damon-Runyon Fellow with Brian Matthews (Institute of Molecular Biology), he used crystallography, mutagenesis, and biophysics to investigate a trade-off between enzyme activity and stability (Shoichet et al, PNAS 1995). In 1996, he joined the faculty of Northwestern University and was recruited back to UCSF in 2003, where he is a professor of Pharmaceutical Chemistry.
The Arnold C. Ott Lectureship in Chemistry was created and endowed by a generous gift from Dr. Arnold C. Ott and Marion Ott. Dr. Ott received his Ph.D. in 1943 from Michigan State University in Chemistry/Physics/Bacteriology and is a leading chemist and entrepreneur in West Michigan. He is one of the co-founders of Grand Valley State University and served on the GVSU Board of Trustees for 28 years.
Thursday October 5th
Reception: 5 pm
Evening Lecture: 6 pm
Location: Grand River Room, Russel H. Kirkhof Center, Allendale Campus (Parking: Visitors to campus can use Lot H (see map) during the public lecture with no need for a parking pass)
Title: How are new drugs discovered?
Abstract: A foundation of the modern medicine that has so successfully extended life-span and quality is the treatment of disease by drugs. I will discuss the social, economic, and technological events that have enabled the flowering of drug discovery in the last 70 years, the regulatory and technological challenges of the modern field, and the new scientific discoveries that are driving it forward.
Friday October 6th
Time: 1 pm
Location: Pere Marquette Room, Russel H. Kirkhof Center, Allendale Campus (Parking: For free parking during Friday's Chemistry seminar, you can obtain a visitor's parking pass by contacting Dave Leonard)
Title: Structure-based discovery for under- and over-studied GPCRs
Abstract: Receptor binding sites are evolved to recognize a few endogenous ligands, but the degeneracy of molecular recognition ensures that many other ligands and chemotypes can bind to the same site. Sometimes these non-biological molecules will confer activities that the native ligands do not.
Structure-based docking screens large compound libraries for novel molecules that physically complement a binding site, but do not resemble known ligands. When these searches are coupled to the right biological assays, they can find new molecules conferring new biology. This can happen for three reasons: targeting of an entirely new receptor, targeting of a new site on a known receptor, and occasionally targeting a known site on a well-established receptor with new biology. This will be illustrated by example with screens for new ligands that deorphanize understudied GPCRs, like GPR68 and MRGPX2, and for ligands that target the highly studied m-opioid and D4 receptors. New opportunities arising from a huge increase in the number of readily available molecules will be considered.
Vernon Ehlers, Ph.D.
Michael D. Parker, M.B.A.
Dow Chemical Company
Carl Djerassi, Ph.D.
Robin D. Rogers, Ph.D.
University of Alabama
Virginia W. Cornish, Ph.D.
Richard N. Zare, Ph.D.
Thomas H. Lane, Ph.D.
Dow Corning Corporation
Chad A. Mirkin, Ph.D.
Gregory A. Petsko, Ph.D.
Harry B. Gray, Ph.D.
California Institute of Technology
Gary M. Hieftje, Ph.D.
Roderick MacKinnon, M.D.
Nobel Laureate in Chemistry, 2003
The Rockefeller University
Ada Yonath, Ph.D.
Nobel Laureate in Chemistry, 2009
Weizmann Institute of Science
W. Carl Lineberger, Ph.D.
University of Colorado, Boulder
Richmond Sarpong, Ph.D.
University of California, Berkeley
Jeffrey Moore, Ph.D.
University of Illinois, Ubrana-Champaign
Wilson Ho, Ph.D.
University of California, Irvine
Geraldine Richmond, Ph.D.
University of Oregon
Sara E. Skrabalak, Ph.D.
Thomas J. Meyer, Ph.D.
University of North Carolina, Chapel Hill