2JIV

Crystal structure of EGFR kinase domain T790M mutation in compex with HKI-272

Summary for 2JIV

• Entry DOI: 10.2210/pdb2jiv/pdb
• Related: 1DNQ 1DNR 1IVO 1M14 1M17 1MOX 1NQL 1XKK 1YY9 1Z9I 2GS2 2GS7 2ITN 2ITO 2ITP 2ITQ 2ITT 2ITU 2ITV 2ITW 2ITX 2ITY 2ITZ 2J5E 2J5F 2J6M 2JIT 2JIU
• Descriptor: EPIDERMAL GROWTH FACTOR RECEPTOR, N-(4-{[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino}-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)butanamide, CHLORIDE ION, ... (4 entities in total)
• Functional Keywords: hki272, hki-272, receptor, cell cycle, atp-binding, transferase, tyrosine-protein kinase, transmembrane, phosphorylation, disease mutation, nucleotide-binding, anti-oncogene, epidermal growth factor
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted: P00533
• Total number of polymer chains: 2
• Total formula weight: 76031.63

Authors

Yun, C.-H.,Mengwasser, K.E.,Toms, A.V.,Li, Y.,Woo, M.S.,Greulich, H.,Wong, K.-K.,Meyerson, M.,Eck, M.J. (deposition date: 2007-07-02, release date: 2008-01-22, Last modification date: 2023-12-13)

• Primary citation: Yun, C.-H.,Mengwasser, K.E.,Toms, A.V.,Woo, M.S.,Greulich, H.,Wong, K.-K.,Meyerson, M.,Eck, M.J.; The T790M Mutation in Egfr Kinase Causes Drug Resistance by Increasing the Affinity for ATP.; Proc.Natl.Acad.Sci.USA, 105:2070-, 2008; PubMed: 18227510; DOI: 10.1073/PNAS.0709662105

Experimental method

X-RAY DIFFRACTION (3.5 Å)