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 Abstract: Expression of the colony-stimulating factor 1 (CSF1) gene is elevated in most tenosynovial giant-cell tumors. This observation has led to the discovery and clinical development of therapy targeting the CSF1 receptor (CSF1R).

PubMed: 26222558
DOI: 10.1056/NEJMoa1411366

Experimental method

X-RAY DIFFRACTION (2.75 Å)