Brand  (β version)

PDB ID: 3IKA

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Ligands
Code Name Style Show Link
0UN N-{3-[(5-chloro-2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)oxy]phenyl}prop-2-enamide PoSSuM
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Structure summary

Code : 3IKA   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Crystal Structure of EGFR 696-1022 T790M Mutant Covalently Binding to WZ4002
Release Data : 2010-01-12
Compound :
mol_id molecule chains synonym
1 Epidermal growth factor receptor A,B Receptor tyrosine-protein kinase ErbB-1
ec: 2.7.10.1
fragment: 694-1022
mutation: T790M
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: EGFR, ERBB1
expression_system_strain: sf9
expression_system_vector_type: Baculovirus
expression_system_plasmid: pAcG2T
Authors : Yun, C.-H., Eck, M.J.
Keywords : EGFR, T790M, WZ4002, WZ-4002, Alternative splicing, ATP-binding, Cell membrane, Disease mutation, Disulfide bond, Glycoprotein, Isopeptide bond, Kinase, Membrane, Nucleotide-binding, Phosphoprotein, Polymorphism, Receptor, Secreted, Transferase, Transmembrane, Tumor suppressor, Tyrosine-protein kinase, Ubl conjugation
Exp. method : X-RAY DIFFRACTION ( 2.90 Å )
Citation :

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.

Zhou, W.,Ercan, D.,Chen, L.  et al.
(2009)  Nature  462 : 1070 - 1074

PubMed: 20033049
DOI: 10.1038/nature08622

Reaction

Chain : A, B
UniProt : P00533 (EGFR_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) 2.7.10.1 PROSITE-ProRule:PRU10028, PubMed:15374980, PubMed:17349580, PubMed:18046415, PubMed:18227510, PubMed:19560417, PubMed:19563760
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