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Kenneth A. Jacobson, Ph.D.

Dr. Kenneth A. Jacobson received his B.A. in Liberal Arts from Reed College in Portland, Oregon and his M.S. and Ph.D. (1981) in Chemistry with Prof. Murray Goodman at the University of California, San Diego. After completing his Postdoctoral work with Professor A. Patchornik at the Dept. of Organic Chemistry, Weizmann Institute in Israel, he joined the National Institute of Diabetes & Digestive and Kidney Diseases at NIH in Bethesda, MD in 1983. He currently serves as Chief of both the Molecular Recognition Section, which he founded in 1993, and the Laboratory of Bioorganic Chemistry. He began the NIDDK Chemical Biology Core Laboratory as Director in 2003.

His creativity and his ability to combine the field of chemistry with those of pharmacology and molecular biology have had a major impact on biomedical research and therapeutic development. Over the course of two decades at NIH, Dr. Jacobson has made major contributions to the pharmacology of cell surface receptors, in particular purinergic receptors. He has studied recognition at the binding sites of G protein-coupled receptors (GPCRs) by structural modification, both from the perspective of the small molecular ligands and of their protein targets. His group began the computer modeling of adenosine receptors as a tool for interpreting site-directed mutagenesis data soon after their cloning. Early in his career he pioneered the concept of “functionalized congeners,” a now widely used approach in drug development, which has recently led to the design of multivalent conjugates of GPCR ligands using dendrimers as nanocarriers. He also introduced the concept of “neoceptors” as a strategy for re-engineering the binding site of a GPCR for activation by chemically tailored small molecules. His research has led to agents in clinical trials for cystic fibrosis, cancer, degenerative diseases, and autoimmune inflammatory diseases. Two nucleosides from the Jacobson laboratory that act as selective A3 adenosine receptor agonists are currently in clinical trials for rheumatoid arthritis, hepatocarcinoma, psoriasis, and dry eye disease. Dozens of ligands used as pharmacological probes in research on adenosine receptors and P2 (nucleotide) receptors were introduced by Dr. Jacobson and colleagues. Many of these substances bear the designation “MRS” after the name of his Section.

Dr. Jacobson has authored or co-authored over 500 scientific publications and is an inventor on 35 issued U.S. patents. He has served the ACS Division of Medicinal Chemistry as Chair in 2004 and has planned and chaired numerous symposia at ACS National Meetings. Dr. Jacobson is or has been on the editorial advisory boards of the Journal of Medicinal ChemistryBioconjugate ChemistryMolecular Pharmacology, Current Topics in Medicinal Chemistry, Medicinal Research Reviews, and Future Medicinal Chemistry, and he is an Associate Editor ofPurinergic Signalling. He has mentored 63 postdoctoral fellows, both chemists and biologists. He received the 2003 Hillebrand Prize, the 2008 Sato International Memorial Prize from the Pharmaceutical Soc. of Japan, and the 2009 Pharmacia-ASPET Award from the American Soc. for Pharmacology and Experimental Therapeutics. Dr. Jacobson was recently included in a listing of the ten most cited researchers in the field of pharmacology.

ACS Division of Medicinal Chemistry

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