Summary for 5AM7
| Entry DOI | 10.2210/pdb5am7/pdb |
| Related | 5AM6 |
| Descriptor | FIBROBLAST GROWTH FACTOR RECEPTOR 1, 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, CHLORIDE ION, ... (4 entities in total) |
| Functional Keywords | transferase, fgfr, cancer, dovitinib, tki258, gatekeeper, gate keeper |
| Biological source | HOMO SAPIENS (HUMAN) |
| Cellular location | Cell membrane; Single-pass type I membrane protein: P11362 |
| Total number of polymer chains | 2 |
| Total formula weight | 71572.58 |
| Authors | Bunney, T.D.,Wan, S.,Thiyagarajan, N.,Sutto, L.,Williams, S.V.,Ashford, P.,Koss, H.,Knowles, M.A.,Gervasio, F.L.,Coveney, P.V.,Katan, M. (deposition date: 2015-03-10, release date: 2015-03-18, Last modification date: 2024-01-10) |
| Primary citation | Bunney, T.,Wan, S.,Thiyagarajan, N.,Sutto, L.,Williams, S.V.,Ashford, P.,Koss, H.,Knowles, M.A.,Gervasio, F.L.,Coveney, P.V.,Katan, M. The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study Ebiomedicine, 2:194-, 2015 Cited by PubMed Abstract: Fibroblast growth factor receptors (FGFRs) are recognized therapeutic targets in cancer. We here describe insights underpinning the impact of mutations on FGFR1 and FGFR3 kinase activity and drug efficacy, using a combination of computational calculations and experimental approaches including cellular studies, X-ray crystallography and biophysical and biochemical measurements. Our findings reveal that some of the tested compounds, in particular TKI258, could provide therapeutic opportunity not only for patients with primary alterations in but also for acquired resistance due to the gatekeeper mutation. The accuracy of the computational methodologies applied here shows a potential for their wider application in studies of drug binding and in assessments of functional and mechanistic impacts of mutations, thus assisting efforts in precision medicine. PubMed: 26097890DOI: 10.1016/J.EBIOM.2015.02.009 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.957 Å) |
Structure validation
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