6JPJ

Crystal structure of FGF401 in complex of FGFR4

Summary for 6JPJ

• Entry DOI: 10.2210/pdb6jpj/pdb
• Descriptor: Fibroblast growth factor receptor 4, N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-methanoyl-6-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide, SULFATE ION, ... (4 entities in total)
• Functional Keywords: fgf401, reversible covalent inhibitor, fgfr4, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 35361.67

Authors

Zhou, Z.,Chen, X.,Chen, Y. (deposition date: 2019-03-27, release date: 2019-05-15, Last modification date: 2024-10-16)

Primary citation

Zhou, Z.,Chen, X.,Fu, Y.,Zhang, Y.,Dai, S.,Li, J.,Chen, L.,Xu, G.,Chen, Z.,Chen, Y.
Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4.
Chem.Commun.(Camb.), 55:5890-5893, 2019

PubMed Abstract: Biochemical and structural studies provide information on the mode of action of FGF401 as a selective, reversible covalent inhibitor of FGFR4. Kinase and proliferation assays reveal that FGF401 has the ability to overcome gatekeeper mutations in FGFR4.

PubMed: 31041948
DOI: 10.1039/c9cc02052g

Experimental method

X-RAY DIFFRACTION (2.638 Å)