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Ligands
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FI3 N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide
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Code : 4R5S   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Crystal structure of EGFR 696-1022 L858R in complex with FIIN-3
Release Data : 2014-11-12
Compound :
mol_id molecule chains synonym
1 Epidermal growth factor receptor A Proto-oncogene c-ErbB-1, Receptor tyrosine-protein kinase erbB-1
ec: 2.7.10.1
fragment: UNP RESIDUES 696-1022
mutation: L858R
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: EGFR, ERBB, ERBB1, HER1
expression_system_common: Fall armyworm
expression_system_vector_type: Baculovirus
Authors : Zhu, S.J., Yun, C.H.
Keywords : EGFR, L858R, Kinase, FIIN-3, TRANSFERASE
Exp. method : X-RAY DIFFRACTION ( 3.001 Å )
Citation :

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.

Tan, L.,Wang, J.,Tanizaki, J.  et al.
(2014)  Proc.Natl.Acad.Sci.USA  111 : E4869 - E4877

PubMed: 25349422
DOI: 10.1073/pnas.1403438111

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