I. Introduction to Drug Discovery
II. From "Hit" to Pill
Part I: Introduction to Drug Discovery
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The modern drug discovery process integrates our deepest understanding of the molecular basis for disease with fundamental understanding of how potential drug molecules interact with specific disease targets and the whole organism. These two lectures are intended to give a broad and general introduction to the drug discovery process. Part I focuses on the early stages of drug discovery. We describe the basic stages of the drug discovery process, beginning with how disease targets are identified.
We then take you into the laboratory to show you how a popular approach, high throughput screening, is used to identify compounds that can engage the molecular target or pathway of interest. Part II focuses on the later stages of the drug discovery process. After the identification of the first hit compounds, iterative rounds of chemistry, biochemistry, cell biology, pharmacology, and toxicology are used to progressively build and polish compounds to make them ready for clinical trials. The adventure of drug discovery represents one of the most fascinating and beneficial pursuits in science.
James A. Wells, Ph.D. Dr. Wells received a B.A. degree in biochemistry from the University of California, Berkeley, and a Ph.D. degree in biochemistry from Washington State University with Dr. Ralph Yount. He is a joint Professor in the Departments of Cellular & Molecular Pharmacology, and Pharmaceutical Chemistry and Chair of the Department.
His current research uses a combination of protein design and small molecule drug discovery to study and modulate cellular processes involved in apoptosis and inflammation. Some of his awards include: the Hans Neurath and Aviv Awards given by the Protein Society, the Pfizer Award given by the American Chemical Society, the du Vignead Award given by the Peptide Society, and in 1999 was elected member of the National Academy of Sciences. See www.wellslab.ucsf.edu for more details.
Michelle R. Arkin, Ph.D. Dr. Arkin received her B.A. degree in chemistry from Bryn Mawr College and her Ph.D. in chemistry at Caltech with Dr. Jacqueline Barton. In 2005 she became the Associate Director of Cell Biology at Sunesis and led the translational science team for Voreloxin, an anti-cancer agent in phase 2 clinical trials. Since July 2007, Michelle has been the Associate Director of Biology at the Small Molecule Discovery Center (http://smdc.ucsf.edu) and Adjunct Assistant Professor in the Department of Pharmaceutical Chemistry at UCSF.
In 2005 she became the Associate Director of Cell Biology at Sunesis and led the translational science team for Voreloxin, an anti-cancer agent in phase 2 clinical trials. Since July 2007, Michelle has been the Associate Director of Biology at the Small Molecule Discovery Center (http://smdc.ucsf.edu) and Adjunct Assistant Professor in the Department of Pharmaceutical Chemistry at UCSF. In this capacity, she directs the high-throughput screening facility and engages in grant-funded drug discovery research. Dr. Arkin’s research interests are in seeking innovative approaches to tackle “undruggable” targets such as protein-protein interfaces and allosteric interactions.
- Susan Desmond-Hellmann iBioMagazine: Drug Development
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