3RKZ
Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.
Summary for 3RKZ
Entry DOI | 10.2210/pdb3rkz/pdb |
Descriptor | Heat shock protein HSP 90-alpha, (5R,6S)-3-(L-alanyl)-5,6,15,15,18-pentamethyl-17-oxo-2,3,4,5,6,7,14,15,16,17-decahydro-1H-12,8-(metheno)[1,5,9]triazacyclotetradecino[1,2-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 | 25906.21 |
Authors | Zapf, C.W.,Bloom, J.D.,Li, Z.,Dushin, R.G.,Nittoli, T.,Otteng, M.,Nikitenko, A.,Golas, J.M.,Liu, H.,Lucas, J.,Boschelli, F.,Vogan, E.,Olland, A.,Johnson, M.,Levin, J.I. (deposition date: 2011-04-18, release date: 2011-07-13, Last modification date: 2023-09-13) |
Primary citation | Zapf, C.W.,Bloom, J.D.,Li, Z.,Dushin, R.G.,Nittoli, T.,Otteng, M.,Nikitenko, A.,Golas, J.M.,Liu, H.,Lucas, J.,Boschelli, F.,Vogan, E.,Olland, A.,Johnson, M.,Levin, J.I. Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model. Bioorg.Med.Chem.Lett., 21:4602-4607, 2011 Cited by PubMed: 21715165DOI: 10.1016/j.bmcl.2011.05.102 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.5693 Å) |
Structure validation
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