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个人简介
I am a medicinal chemist with interests in the structure and pharmacology of receptors and in developing drugs that act as agonists or antagonists of G protein-coupled receptors (GPCRs). My current focus is on receptors for purines, encompassing both adenosine receptors and P2 receptors, which are activated by ATP, UTP and other extracellular nucleotides. My lab has taken an interdisciplinary approach to studying the chemical and biological aspects of these receptors. We have used convergent modeling, mutagenesis and structure activity approaches to gather information about the three-dimensional structure of the receptors and its relationship to binding and activation functions. The determination of the X-ray crystallographic structures of the P2Y1 receptor and an agonist bound A2A adenosine receptor by our lab in collaboration with Ray Stevens of Scripps Research Institute is providing a new path to designing drugs that act at these receptors. We have developed a functionalized congener approach to drug design that permits inclusion of reporter groups such as fluorophores. Novel ligands (small molecules) for these receptors are developed using classical synthetic approaches and also by semirational methods based on molecular modeling and template design. Receptors are computer-modeled by homology to GPCRs of known structure, and the models for ligand recognition are tested and refined using site-directed mutagenesis of the receptor proteins. Recently, the involvement of extracellular loops of GPCRs have been implicated in the receptor binding of small molecules. We are interested in correlating structure of receptors and small molecular drugs with pharmacological properties.
研究兴趣
论文共 1139 篇作者统计合作学者相似作者
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Ana C. Puhl,Sarah A. Lewicki,Zhan-Guo Gao, Asmita Pramanik,Vadim Makarov,Sean Ekins,Kenneth A. Jacobson
Purinergic Signallingpp.1-11, (2024)
Naveen Thakur,Arka Prabha Ray,Beining Jin, Nessa Pesaran Afsharian,Edward Lyman,Zhan-Guo Gao,Kenneth A. Jacobson,Matthew T. Eddy
Structure (2024)
Ana C. Puhl, Sarah A. Lewicki,Zhan-Guo Gao, Asmita Pramanik, Vadim Makarov,Sean Ekins,Kenneth A. Jacobson
Purinergic Signallingpp.1-11, (2024)
Stephanie A. Michalski, Karen Galen, Paula Sureda I Gibert,Kenneth A. Jacobson,Simon Akerman,Daniela Salvemini
The Journal of Painno. 4 (2024): 8
Kenneth Jacobson,Dilip K. Tosh,Chunxia Cronin, Matteo Pavan,Eline Pottie,Tina C. Wan,Eric Chen,Sarah A. Lewicki,Ryan G. Campbell,Zhan-Guo Gao, John A. Auchampach,Christophe P. Stove,
ASPET 2024 Annual Meeting Abstract - Drug Discovery and Development (2024)
Zhan-Guo Gao, Weiping Chen, Ray R. Gao, Jonathan Li,Dilip K. Tosh,John A. Hanover,Kenneth A. Jacobson
Purinergic Signallingpp.1-12, (2024)
ASPET 2024 Annual Meeting Abstract - Cellular and Molecular Pharmacology (2024)
Hai-Jun Zhang,Michał Ociepa,Molhm Nassir,Bin Zheng,Sarah A. Lewicki,Veronica Salmaso, Helay Baburi,Jessica Nagel,Salahuddin Mirza,Beatriz Bueschbell,Haneen Al-Hroub, Olga Perzanowska,
Nature Chemistryno. 2 (2024): 249-258
Matthew R Sapio, Ellen S Staedtler, Diana M King,Dragan Maric,Jahandar Jahanipour, Andre Ghetti,Kenneth A Jacobson,Andrew J Mannes,Michael J Iadarola
Pain (2024)
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