4R7I

Crystal structure of FMS kinase domain with a small molecular inhibitor, GLEEVEC

Summary for 4R7I

• Entry DOI: 10.2210/pdb4r7i/pdb
• Descriptor: Macrophage colony-stimulating factor 1 receptor, 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE (3 entities in total)
• Functional Keywords: csf-1-r, fms proto-oncogene, c-fms, cd115 antigen, kinase, atp-binding, gleevec, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cell membrane; Single-pass type I membrane protein: P07333
• Total number of polymer chains: 1
• Total formula weight: 39133.78

Authors

Zhang, Y.,Zhang, C. (deposition date: 2014-08-27, release date: 2015-08-12, Last modification date: 2023-09-20)

• Primary citation: Tap, W.D.,Wainberg, Z.A.,Anthony, S.P.,Ibrahim, P.N.,Zhang, C.,Healey, J.H.,Chmielowski, B.,Staddon, A.P.,Cohn, A.L.,Shapiro, G.I.,Keedy, V.L.,Singh, A.S.,Puzanov, I.,Kwak, E.L.,Wagner, A.J.,Von Hoff, D.D.,Weiss, G.J.,Ramanathan, R.K.,Zhang, J.,Habets, G.,Zhang, Y.,Burton, E.A.,Visor, G.,Sanftner, L.,Severson, P.,Nguyen, H.,Kim, M.J.,Marimuthu, A.,Tsang, G.,Shellooe, R.,Gee, C.,West, B.L.,Hirth, P.,Nolop, K.,van de Rijn, M.,Hsu, H.H.,Peterfy, C.,Lin, P.S.,Tong-Starksen, S.,Bollag, G.; Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.; N Engl J Med, 373:428-437, 2015; PubMed: 26222558; DOI: 10.1056/NEJMoa1411366

Experimental method

X-RAY DIFFRACTION (2.75 Å)