Extrahelical Binding Site for a 1H-Imidazo[4,5-c]quinolin-4-amine A3 Adenosine Receptor Positive Allosteric Modulator on Helix 8 and Distal Portions of Transmembrane Domains 1 and 7.

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Title: Extrahelical Binding Site for a 1H-Imidazo[4,5-c]quinolin-4-amine A3 Adenosine Receptor Positive Allosteric Modulator on Helix 8 and Distal Portions of Transmembrane Domains 1 and 7.
Authors: Fisher CL; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Pavan M; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Salmaso V; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Keyes RF; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Wan TC; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Pradhan B; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Gao ZG; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Smith BC; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.)., Jacobson KA; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.) jauchamp@mcw.edu kennethj@niddk.nih.gov., Auchampach JA; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.) jauchamp@mcw.edu kennethj@niddk.nih.gov.
Source: Molecular pharmacology [Mol Pharmacol] 2024 Feb 15; Vol. 105 (3), pp. 213-223. Date of Electronic Publication: 2024 Feb 15.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Society for Pharmacology and Experimental Therapeutics Country of Publication: Netherlands NLM ID: 0035623 Publication Model: Electronic Cited Medium: Internet ISSN: 1521-0111 (Electronic) Linking ISSN: 0026895X NLM ISO Abbreviation: Mol Pharmacol Subsets: MEDLINE
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  Data: Extrahelical Binding Site for a 1H-Imidazo[4,5-c]quinolin-4-amine A<subscript>3</subscript> Adenosine Receptor Positive Allosteric Modulator on Helix 8 and Distal Portions of Transmembrane Domains 1 and 7.
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Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.).<br /><searchLink fieldCode="AU" term="%22Wan+TC%22">Wan TC</searchLink>; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.).<br /><searchLink fieldCode="AU" term="%22Pradhan+B%22">Pradhan B</searchLink>; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.).<br /><searchLink fieldCode="AU" term="%22Gao+ZG%22">Gao ZG</searchLink>; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.).<br /><searchLink fieldCode="AU" term="%22Smith+BC%22">Smith BC</searchLink>; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.).<br /><searchLink fieldCode="AU" term="%22Jacobson+KA%22">Jacobson KA</searchLink>; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.) jauchamp@mcw.edu kennethj@niddk.nih.gov.<br /><searchLink fieldCode="AU" term="%22Auchampach+JA%22">Auchampach JA</searchLink>; Departments of Pharmacology & Toxicology and the Cardiovascular Center (C.L.F., T.C.W., J.A.A.) and Biochemistry and the Program in Chemical Biology (R.F.K., B.C.S.), Medical College of Wisconsin, Milwaukee, Wisconsin; Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (M.P., V.S., B.P., Z.-G.G., K.A.J.); and Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy (V.S.) jauchamp@mcw.edu kennethj@niddk.nih.gov.
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