4RZV

Crystal structure of the BRAF (R509H) kinase domain monomer bound to Vemurafenib

Summary for 4RZV

• Entry DOI: 10.2210/pdb4rzv/pdb
• Related: 4RZW
• Descriptor: Serine/threonine-protein kinase B-raf, N-(3-{[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)propane-1-sulfonamide (2 entities in total)
• Functional Keywords: transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Nucleus : P15056
• Total number of polymer chains: 2
• Total formula weight: 65007.19

Authors

Wu, Y.,Gavathiotis, E. (deposition date: 2014-12-24, release date: 2016-08-10, Last modification date: 2023-09-20)

• Primary citation: Karoulia, Z.,Wu, Y.,Ahmed, T.A.,Qisheng, X.,Bollard, J.,Krepler, C.,Wu, X.,Zhang, C.,Bollag, G.,Herlym, M.,Fagin, J.A.,Lujambio, A.,Gavathiotis, E.,Poulikakos, P.I.; An integrated model of RAF inhibitor action predicts inhibitor activity against oncogenic BRAF signaling; Cancer Cell, 30:1-14, 2016

Experimental method

X-RAY DIFFRACTION (2.994 Å)