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Ligands
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03P N-{2-[4-({3-chloro-4-[3-(trifluoromethyl)phenoxy]phenyl}amino)-5h-pyrrolo[3,2-D]pyrimidin-5-yl]ethyl}-3-hydroxy-3-methylbutanamide
SO4 Sulfate ion
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Code : 3POZ   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : EGFR Kinase domain complexed with tak-285
Release Data : 2011-03-30
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: Residues 606-1022
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7118)
gene: EGFR, ERBB1
expression_system_strain: Sf9
expression_system_vector_type: BACULOVIRUS
expression_system_plasmid: pFastBacHT
Authors : Aertgeerts, K., Skene, R., Sogabe, S.
Keywords : KINASE DOMAIN, ANTI-ONCOGENE, ATP-BINDING, CELL CYCLE, DISEASE MUTATION, GLYCOPROTEIN, MEMBRANE, NUCLEOTIDE-BINDING, PHOSPHOPROTEIN, RECEPTOR, SECRETED, TRANSFERASE, TRANSMEMBRANE, TYROSINE-PROTEIN KINASE, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 1.50 Å )
Citation :

Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein.

Aertgeerts, K.,Skene, R.,Yano, J.  et al.
(2011)  J.Biol.Chem.  286 : 18756 - 18765

PubMed: 21454582
DOI: 10.1074/jbc.M110.206193

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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