U.S. Department of Health and Human Services
Kenneth Jacobson

 Contact Info

Tel: 301-496-9024
Email: kajacobs@helix.nih.gov

 Select Experience

  • Bantrel FellowWeizmann Institute of Science, Department of Organic Chemistry1983
  • Ph.D.University of California, San Diego1981
  • M.S.University of California, San Diego1978
  • B.A.Reed College1975

 Related Links

  •   Molecular Pharmacology/Toxicology
  • Chemistry/Chemical Biology
  • Molecular Biology/Biochemistry


A selection of recent and significant publications can be viewed below.

Tosh DK, Paoletta S, Deflorian F, Phan K, Moss SM, Gao ZG, Jiang X, Jacobson KA. Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity. J. Med. Chem. 2012 Sep 27; 55:8075-90. [Full Text/Abstract]
Jacobson KA, Costanzi S. New insights for drug design from the X-ray crystallographic structures of G-protein-coupled receptors. Mol. Pharmacol. 2012 Sep; 82:361-71. [Full Text/Abstract]
Tosh DK, Phan K, Gao ZG, Gakh AA, Xu F, Deflorian F, Abagyan R, Stevens RC, Jacobson KA, Katritch V. Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening. J. Med. Chem. 2012 May 10; 55:4297-308. [Full Text/Abstract]
Chen Z, Janes K, Chen C, Doyle T, Bryant L, Tosh DK, Jacobson KA, Salvemini D. Controlling murine and rat chronic pain through A3 adenosine receptor activation. FASEB J. 2012 May; 26:1855-65. [Full Text/Abstract]
Fishman P, Bar-Yehuda S, Liang BT, Jacobson KA. Pharmacological and therapeutic effects of A3 adenosine receptor agonists. Drug Discov. Today. 2012 Apr; 17:359-66. [Full Text/Abstract]
Kecskés A, Tosh DK, Wei Q, Gao ZG, Jacobson KA. GPCR ligand dendrimer (GLiDe) conjugates: adenosine receptor interactions of a series of multivalent xanthine antagonists. Bioconjug. Chem. 2011 Jun 15; 22:1115-27. [Full Text/Abstract]
Xu F, Wu H, Katritch V, Han GW, Jacobson KA, Gao ZG, Cherezov V, Stevens RC. Structure of an agonist-bound human A2A adenosine receptor. Science. 2011 Apr 15; 332:322-7. [Full Text/Abstract]
Jacobson KA, Boeynaems JM. P2Y nucleotide receptors: promise of therapeutic applications. Drug Discov. Today. 2010 Jul; 15:570-8. [Full Text/Abstract]
Carlsson J, Yoo L, Gao ZG, Irwin JJ, Shoichet BK, Jacobson KA. Structure-based discovery of A2A adenosine receptor ligands. J. Med. Chem. 2010 May 13; 53:3748-55. [Full Text/Abstract]
Ivanov AA, Barak D, Jacobson KA. Evaluation of homology modeling of G-protein-coupled receptors in light of the A(2A) adenosine receptor crystallographic structure. J. Med. Chem. 2009 May 28; 52:3284-92. [Full Text/Abstract]
Klutz AM, Gao ZG, Lloyd J, Shainberg A, Jacobson KA. Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates. J Nanobiotechnology. 2008 Oct 23; 6:12. [Full Text/Abstract]
Ivanov AA, Jacobson KA. Molecular modeling of a PAMAM-CGS21680 dendrimer bound to an A2A adenosine receptor homodimer. Bioorg. Med. Chem. Lett. 2008 Aug 1; 18:4312-5. [Full Text/Abstract]
Kim Y, Klutz AM, Jacobson KA. Systematic investigation of polyamidoamine dendrimers surface-modified with poly(ethylene glycol) for drug delivery applications: synthesis, characterization, and evaluation of cytotoxicity. Bioconjug. Chem. 2008 Aug; 19:1660-72. [Full Text/Abstract]
Jeong LS, Lee HW, Kim HO, Tosh DK, Pal S, Choi WJ, Gao ZG, Patel AR, Williams W, Jacobson KA, Kim HD. Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists. Bioorg. Med. Chem. Lett. 2008 Mar 1; 18:1612-6. [Full Text/Abstract]
Gao ZG, Jacobson KA. Emerging adenosine receptor agonists. Expert Opin Emerg Drugs. 2007 Sep; 12:479-92. [Full Text/Abstract]
Ko H, Fricks I, Ivanov AA, Harden TK, Jacobson KA. Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor. J. Med. Chem. 2007 May 3; 50:2030-9. [Full Text/Abstract]
Koizumi S, Shigemoto-Mogami Y, Nasu-Tada K, Shinozaki Y, Ohsawa K, Tsuda M, Joshi BV, Jacobson KA, Kohsaka S, Inoue K. UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis. Nature. 2007 Apr 26; 446:1091-5. [Full Text/Abstract]
Jacobson KA, Gao ZG, Liang BT. Neoceptors: reengineering GPCRs to recognize tailored ligands. Trends Pharmacol. Sci. 2007 Mar; 28:111-6. [Full Text/Abstract]
Gao ZG, Jacobson KA. Keynote review: allosterism in membrane receptors. Drug Discov. Today. 2006 Mar; 11:191-202. [Full Text/Abstract]
Jacobson KA, Gao ZG. Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar; 5:247-64. [Full Text/Abstract]
Gao ZG, Kim SK, Ijzerman AP, Jacobson KA. Allosteric modulation of the adenosine family of receptors. Mini Rev Med Chem. 2005 Jun; 5:545-53. [Full Text/Abstract]
Jacobson KA, Ohno M, Duong HT, Kim SK, Tchilibon S, Cesnek M, Holý A, Gao ZG. A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists. Chem. Biol. 2005 Feb; 12:237-47. [Full Text/Abstract]
Joshi BV, Moon HR, Fettinger JC, Marquez VE, Jacobson KA. A new synthetic route to (North)-methanocarba nucleosides designed as A3 adenosine receptor agonists. J. Org. Chem. 2005 Jan 21; 70:439-47. [Full Text/Abstract]
Kim HS, Ohno M, Xu B, Kim HO, Choi Y, Ji XD, Maddileti S, Marquez VE, Harden TK, Jacobson KA. 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J. Med. Chem. 2003 Nov 6; 46:4974-87. [Full Text/Abstract]