3R91
Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.
Summary for 3R91
Entry DOI | 10.2210/pdb3r91/pdb |
Descriptor | Heat shock protein HSP 90-alpha, (6S)-4,6,15,15,18-pentamethyl-5,17-dioxo-2,3,4,5,6,7,14,15,16,17-decahydro-1H-12,8-(metheno)[1,4,9]triazacyclotetradecino[9,8-a]indole-9-carboxamide (3 entities in total) |
Functional Keywords | chaperone, atp binding domain, atp-binding, nucleotide-binding, phosphoprotein, stress response, chaperone-chaperone inhibitor complex, chaperone/chaperone inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Cytoplasm: P07900 |
Total number of polymer chains | 1 |
Total formula weight | 25849.11 |
Authors | Zapf, C.W.,Bloom, J.D.,McBean, J.L.,Dushin, R.G.,Nittoli, T.,Otteng, M.,Ingalls, C.,Golas, J.M.,Liu, H.,Lucas, J.,Boschelli, F.,Vogan, E.,Hu, Y.,Levin, J.I. (deposition date: 2011-03-24, release date: 2011-05-11, Last modification date: 2023-09-13) |
Primary citation | Zapf, C.W.,Bloom, J.D.,McBean, J.L.,Dushin, R.G.,Nittoli, T.,Otteng, M.,Ingalls, C.,Golas, J.M.,Liu, H.,Lucas, J.,Boschelli, F.,Hu, Y.,Vogan, E.,Levin, J.I. Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity. Bioorg.Med.Chem.Lett., 21:3411-3416, 2011 Cited by PubMed: 21515049DOI: 10.1016/j.bmcl.2011.03.112 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.579 Å) |
Structure validation
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