4R5Y

The complex structure of Braf V600E kinase domain with a novel Braf inhibitor

Summary for 4R5Y

• Entry DOI: 10.2210/pdb4r5y/pdb
• Descriptor: Serine/threonine-protein kinase B-raf, 5-({(1R,1aS,6bR)-1-[5-(trifluoromethyl)-1H-benzimidazol-2-yl]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-5-yl}oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one (2 entities in total)
• Functional Keywords: kinase, signal transduction, 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: 67607.11

Authors

Feng, Y.,Peng, H.,Zhang, Y.,Liu, Y.,Wei, M. (deposition date: 2014-08-22, release date: 2016-02-24, Last modification date: 2024-02-28)

• Primary citation: Tang, Z.,Yuan, X.,Du, R.,Cheung, S.H.,Zhang, G.,Wei, J.,Zhao, Y.,Feng, Y.,Peng, H.,Zhang, Y.,Du, Y.,Hu, X.,Gong, W.,Liu, Y.,Gao, Y.,Liu, Y.,Hao, R.,Li, S.,Wang, S.,Ji, J.,Zhang, L.,Li, S.,Sutton, D.,Wei, M.,Zhou, C.,Wang, L.,Luo, L.; BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers.; Mol.Cancer Ther., 14:2187-2197, 2015; PubMed: 26208524; DOI: 10.1158/1535-7163.MCT-15-0262

Experimental method

X-RAY DIFFRACTION (3.5 Å)