8U1F

FGFR2 Kinase Domain Bound to Irreversible Inhibitor Cmpd 10

Summary for 8U1F

• Entry DOI: 10.2210/pdb8u1f/pdb
• Related: 8STG 8SWE
• Descriptor: Fibroblast growth factor receptor 2, GLYCEROL, N-[4-(4-amino-7-methyl-5-{4-[(4-methylpyrimidin-2-yl)oxy]phenyl}-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenyl]-2-methylpropanamide, ... (4 entities in total)
• Functional Keywords: inhibitor kinase, oncoprotein, transferase-inhibitor complex, transferase/inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 2
• Total formula weight: 73418.52

Authors

Valverde, R.,Foster, L. (deposition date: 2023-08-31, release date: 2024-02-14)

• Primary citation: Schonherr, H.,Ayaz, P.,Taylor, A.M.,Casaletto, J.B.,Toure, B.B.,Moustakas, D.T.,Hudson, B.M.,Valverde, R.,Zhao, S.,O'Hearn, P.J.,Foster, L.,Sharon, D.A.,Garfinkle, S.,Giordanetto, F.,Lescarbeau, A.,Kurukulasuriya, R.,Gerami-Moayed, N.,Maglic, D.,Bruderek, K.,Naik, G.,Gunaydin, H.,Mader, M.M.,Boezio, A.A.,McLean, T.H.,Chen, R.,Wang, Y.,Shaw, D.E.,Watters, J.,Bergstrom, D.A.; Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.; Proc.Natl.Acad.Sci.USA, 121:e2317756121-e2317756121, 2024; PubMed: 38300868; DOI: 10.1073/pnas.2317756121

Experimental method

X-RAY DIFFRACTION (3.33 Å)