Thought-provoking presentations by impressive scientific pacesetters offer personal insight to innovation and achievement. Learn from them and be inspired by them.
Monday, March 28, 9:00 - 11:00 am
Beta Arrestin Mediated Signaling by 7 Transmembrane Receptors: New Therapeutic Opportunities
SBS Achievement Award Winner
Robert J. Lefkowitz, M.D.
Duke University School of Medicine
Durham, North Carolina
Robert Lefkowitz studies receptor biology and signal transduction and is most well known for his detailed characterizations of the sequence, structure and function of the beta-adrenergic receptor and the proteins required for its regulation. Upon recognizing the sequence and functional homology with the visual protein rhodopsin, Dr. Lefkowitz proposed that adrenergic receptors and rhodopsin were related and the first members of a new protein family, the seven transmembrane receptors or G-protein coupled receptors. This superfamily is now known to be the largest, most diverse, and most therapeutically accessible. Author or co-author of more than 800 publications, Dr. Lefkowitz is among the most highly cited researchers in the fields of biology, biochemistry, pharmacology, toxicology, and clinical medicine according to Thomson-ISI.
Dr. Lefkowitz earned a bachelor's degree in chemistry from Columbia University in 1962. In 1966 he earned his M.D. from Columbia University College of Physicians and Surgeons. He completed an internship and residency in general medicine at Columbia-Presbyterian Medical Center. After a clinical and research fellowship at the National Institutes of Health, Dr. Lefkowitz completed residency and research and clinical fellowship training in cardiovascular disease at Massachusetts General Hospital and concurrently served as a teaching fellow and research assistant at Harvard Medical School. In 1973 Dr. Lefkowitz joined the Duke University School of Medicine as an associate professor of medicine and assistant professor of biochemistry. In 1976, he was named an investigator of the Howard Hughes Medical Institute, a position he still holds. By 1977, he was a professor of medicine, and just five years later he was named a James B. Duke Professor of Medicine. He is also currently a professor of biochemistry and of immunology. Dr. Lefkowitz has served as president of the American Society for Clinical Investigation and of the Association of American Physicians, and on the Council of the USA National Academy of Sciences. He holds 10 U.S. patents and has served on the pharmaceutical and biotechnology boards of a number of organizations.
Mechanism and Effects of Colloidal Aggregation in Early Discovery and Drug Pharmacology
SBS Accomplishment Award Winner
Brian Shoichet, Ph.D.
University of California, San Francisco
San Francisco, California
Research in the Shoichet Lab at the University of the California San Francisco (UCSF) seeks to bring chemical reagents to biology, using a combination of computational simulation and experiment. Using a protein-centric approach, new ligands are sought to complement protein structures. This typically involves molecular docking and the development of model experimental systems to experimentally test new algorithms. A new direction adopts a ligand-centric approach that seeks new targets for known drugs and reagents. Whereas this lacks the physical foundation of the structure-based docking, it returns to an older, pharmacological view of biological relationships, bringing to it a quantitative model. A biological focus for both areas is the discovery of reagents to modulate GPCRs. It is supported by the National Institutes of Health.
Dr. Shoichet received bachelor's degrees in chemistry and history from the Massachusetts Institute of Technology in 1985. In 1991 he earned his Ph.D. from UCSF for his work with Tack Kuntz on molecular docking. Dr. Shoichet's postdoctoral research was largely experimental, focusing on protein structure and stability with Brian Matthews at the Institute of Molecular Biology in Eugene, OR, as a Damon Runyon Fellow. Dr. Shoichet joined the faculty at Northwestern University in the Department of Molecular Pharmacology and Biological Chemistry as an Assistant Professor in 1996 and received tenure in 2002. Around that time he was recruited back to UCSF, where he is now a professor in the Department of Pharmaceutical Chemistry.
Thursday, March 31, 12:00 - 1:30 pm
Allostery and S1P Receptors: A Syzygy of Pharmacology and High-Resolution Crystal Structure
Hugh Rosen, MD, PhD
The Scripps Research Institute
Approaches to S1P1 receptor therapeutics will be presented, including uHTS approaches, pharmacological clues for allostery, pocket mapping by mutagenesis, insights from a high-resolution S1P1 crystal structure, implications for signal bias and the biological consequences of receptor modulation.
Hugh Rosen is Professor of Chemical Physiology at The Scripps Research Institute. He received his MD from the University of Cape Town and his PhD from Oxford. After 11 years at Merck, he returned to academia in early 2002 to the Scripps Research Institute, to pursue his primary interests in signaling lipids, and to contribute towards the translational infrastructure at TSRI. He chaired the Molecular Libraries Screening Network Steering Group, a part of the NIH Roadmap, and is principal investigator of the Scripps Research Institute Molecular Screening Center. He is Associate Editor of Molecular Pharmacology and Scientific Co-founder of Receptos Pharmaceuticals. A frequent invited speaker to national and international research meetings and major research universities, Dr, Rosen studies novel chemical approaches to immuno-modulation helpful in treating autoimmune and infectious diseases. Dr. Rosen currently serves on the Scientific Board of the Myeloproliferative Diseases Foundation.