Research ArticleArticle
Probing the CB1 Cannabinoid Receptor Binding Pocket with AM6538, a High-Affinity Irreversible Antagonist
Robert B. Laprairie, Kiran Vemuri, Edward L. Stahl, Anisha Korde, Jo-Hao Ho, Travis W. Grim, Tian Hua, Yiran Wu, Raymond C. Stevens, Zhi-Jie Liu, Alexandros Makriyannis and Laura M. Bohn
Molecular Pharmacology November 2019, 96 (5) 619-628; DOI: https://doi.org/10.1124/mol.119.116483
Robert B. Laprairie
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Kiran Vemuri
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Edward L. Stahl
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Anisha Korde
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Jo-Hao Ho
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Travis W. Grim
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Tian Hua
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Yiran Wu
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Raymond C. Stevens
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Zhi-Jie Liu
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Alexandros Makriyannis
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
Laura M. Bohn
Departments of Molecular Medicine and Neuroscience, The Scripps Research Institute, Jupiter, Florida (R.B.L., E.L.S., J.-H.H., T.W.G., L.M.B.); Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts (K.V., A.K., A.M.); iHuman Institute, ShanghaiTech University, Shanghai, China (T.H., Y.W., Z.-J.L.); and Departments of Biological Sciences and Chemistry, Bridge Institute, Michelson Center for Convergent Bioscience, University of Southern California, Los Angeles, California (R.C.S.)
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Research ArticleArticle
AM6538: An Irreversible CB1 Antagonist
Robert B. Laprairie, Kiran Vemuri, Edward L. Stahl, Anisha Korde, Jo-Hao Ho, Travis W. Grim, Tian Hua, Yiran Wu, Raymond C. Stevens, Zhi-Jie Liu, Alexandros Makriyannis and Laura M. Bohn
Molecular Pharmacology November 1, 2019, 96 (5) 619-628; DOI: https://doi.org/10.1124/mol.119.116483
Research ArticleArticle
AM6538: An Irreversible CB1 Antagonist
Robert B. Laprairie, Kiran Vemuri, Edward L. Stahl, Anisha Korde, Jo-Hao Ho, Travis W. Grim, Tian Hua, Yiran Wu, Raymond C. Stevens, Zhi-Jie Liu, Alexandros Makriyannis and Laura M. Bohn
Molecular Pharmacology November 1, 2019, 96 (5) 619-628; DOI: https://doi.org/10.1124/mol.119.116483
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