7KIE
Crystal structure of FGFR2 kinase domain gatekeeper mutant V564F in complex with covalent compound 3
Summary for 7KIE
Entry DOI | 10.2210/pdb7kie/pdb |
Related | 7KIA |
Descriptor | Fibroblast growth factor receptor 2, N-{4-[(E)-2-{4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}ethenyl]phenyl}prop-2-enamide, CITRATE ANION, ... (5 entities in total) |
Functional Keywords | fgfr kinase domain, fgfr, fgfr2, fgfr3, kinase inhibitor, covalent inhibitor, gatekeeper mutant, rtk, signaling protein, tumor growth, cholangiocarcinoma |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 2 |
Total formula weight | 72106.76 |
Authors | Ke, J.,Wibowo, A.S.,Carter, J.J.,Larsen, N.A. (deposition date: 2020-10-23, release date: 2021-02-10, Last modification date: 2023-10-18) |
Primary citation | Brawn, R.A.,Cook, A.,Omoto, K.,Ke, J.,Karr, C.,Colombo, F.,Virrankoski, M.,Prajapati, S.,Reynolds, D.,Bolduc, D.M.,Nguyen, T.V.,Gee, P.,Borrelli, D.,Caleb, B.,Yao, S.,Irwin, S.,Larsen, N.A.,Selvaraj, A.,Zhao, X.,Ioannidis, S. Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3. Acs Med.Chem.Lett., 12:93-98, 2021 Cited by PubMed: 33488969DOI: 10.1021/acsmedchemlett.0c00517 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.47 Å) |
Structure validation
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