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Dr. Santi received a Ph.D. in Medicinal Chemistry from SUNY in 1967 and a M.D. from UCSF in 1981. He was Assistant Professor of Chemistry at UCSB from 1968 to 1974. He joined the UCSF faculty in 1974 and was Professor of Biochemistry and Biophysics, and of Pharmaceutical Chemistry at UCSF until 2000 when he became CEO of Kosan Biosciences. He returned to UCSF in 2007 where he served as interim Director of the UCSF CTSI and then Director of Translational Research at QB3. He became an Associate Dean of External Relationships in the School of Pharmacy in 2009, and manages an Industry Outreach Program. Dr. Santi has published over 300 scientific papers and is co-inventor on over 40 US patents.

Santi was a member of the original Scientific Advisory Board of Chiron Corp. and has co-founded five biotechnology companies. In 1988, he founded and was Chairman of the peptide-combinatorial chemistry company Protos Corp., which merged with Chiron in 1992. He was also a co-founder of Parnassus Pharmaceuticals, and of Prospect Genomics which merged with Structural Genomix in 2001. In 1996, he co-founded Kosan Biosciences where he served as CEO and Chairman until 2006 when Kosan was acquired by Bristol Myers Squibb. He co-founded the platform technology company ProLynx LLC in 2010, where he currently serves as President.