5UUU
Design, Synthesis, and Evaluation of the First Selective and Potent G-protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure
Summary for 5UUU
Entry DOI | 10.2210/pdb5uuu/pdb |
Related | 5UVC |
Descriptor | Beta-adrenergic receptor kinase 1, 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, SULFATE ION, ... (5 entities in total) |
Functional Keywords | kinase, inhibitor, heart failure, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Cytoplasm : P25098 |
Total number of polymer chains | 1 |
Total formula weight | 64089.92 |
Authors | Hoffman, I.D.,Lawson, J.D. (deposition date: 2017-02-17, release date: 2017-07-26, Last modification date: 2024-03-06) |
Primary citation | Okawa, T.,Aramaki, Y.,Yamamoto, M.,Kobayashi, T.,Fukumoto, S.,Toyoda, Y.,Henta, T.,Hata, A.,Ikeda, S.,Kaneko, M.,Hoffman, I.D.,Sang, B.C.,Zou, H.,Kawamoto, T. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J. Med. Chem., 60:6942-6990, 2017 Cited by PubMed: 28699740DOI: 10.1021/acs.jmedchem.7b00443 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.7 Å) |
Structure validation
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