8W3B
TAS-120 covalent structure with FGFR2 molecular brake mutant
Summary for 8W3B
| Entry DOI | 10.2210/pdb8w3b/pdb |
| Descriptor | Fibroblast growth factor receptor 2, 1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en-1-one, SULFATE ION, ... (4 entities in total) |
| Functional Keywords | fgfr2, tas-120, inhibitor, complex, transferase, transferase-inhibitor complex, kinase, molecular brake, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 4 |
| Total formula weight | 150564.92 |
| Authors | Hoffman, I.D.,Nelson, K.J.,Bensen, D.C.,Bailey, J.B. (deposition date: 2024-02-22, release date: 2025-01-01) |
| Primary citation | Goyal, L.,DiToro, D.,Facchinetti, F.,Martin, E.E.,Peng, P.,Baiev, I.,Iyer, R.,Maurer, J.,Reyes, S.,Zhang, K.,Majeed, U.,Berchuck, J.E.,Chen, C.T.,Walmsley, C.,Pinto, C.,Vasseur, D.,Gordan, J.D.,Mody, K.,Borad, M.,Karasic, T.,Damjanov, N.,Danysh, B.P.,Wehrenberg-Klee, E.,Kambadakone, A.R.,Saha, S.K.,Hoffman, I.D.,Nelson, K.J.,Iyer, S.,Qiang, X.,Sun, C.,Wang, H.,Li, L.,Javle, M.,Lin, B.,Harris, W.,Zhu, A.X.,Cleary, J.M.,Flaherty, K.T.,Harris, T.,Shroff, R.T.,Leshchiner, I.,Parida, L.,Kelley, R.K.,Fan, J.,Stone, J.R.,Uboha, N.V.,Hirai, H.,Sootome, H.,Wu, F.,Bensen, D.C.,Hollebecque, A.,Friboulet, L.,Lennerz, J.K.,Getz, G.,Juric, D. A Model for Decoding Resistance in Precision Oncology: Acquired Resistance to FGFR inhibitors in Cholangiocarcinoma. Ann Oncol, 2024 Cited by PubMed Abstract: Fibroblast growth factor receptor (FGFR) inhibitors have significantly improved outcomes for patients with FGFR-altered cholangiocarcinoma, leading to their regulatory approval in multiple countries. However, as with many targeted therapies, acquired resistance limits their efficacy. A comprehensive, multimodal approach is crucial to characterizing resistance patterns to FGFR inhibitors. PubMed: 39706336DOI: 10.1016/j.annonc.2024.12.011 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.23 Å) |
Structure validation
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