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Structure paper

TitleStructural insights into how irreversible inhibitors can overcome drug resistance in EGFR.
Journal, issue, pagesBioorg. Med. Chem., Vol. 16, Page 3482-3488, Year 2008
Publish dateJul 3, 2007 (structure data deposition date)
AuthorsMichalczyk, A. / Kluter, S. / Rode, H.B. / Simard, J.R. / Grutter, C. / Rabiller, M. / Rauh, D.
External linksBioorg. Med. Chem. / PubMed:18316192
MethodsX-ray diffraction
Resolution2.32 - 2.38 Å
Structure data

PDB-2qi8:
Crystal structure of drug resistant SRC kinase domain
Method: X-RAY DIFFRACTION / Resolution: 2.32 Å

PDB-2qlq:
Crystal structure of SRC kinase domain with covalent inhibitor RL3
Method: X-RAY DIFFRACTION / Resolution: 2.33 Å

PDB-2qq7:
Crystal structure of drug resistant SRC kinase domain with irreversible inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.38 Å

Chemicals

ChemComp-GOL:
GLYCEROL

ChemComp-HOH:
WATER

ChemComp-SR2:
(2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide

Source
  • gallus gallus (chicken)
KeywordsSIGNALING PROTEIN / TRANSFERASE / Src kinase domain; drug resistance / Src kinase domain / drug resistance / irreversible inhibitor / kovalent inhibitor / Alternative splicing / ATP-binding / Lipoprotein / Myristate / Nucleotide-binding / Phosphorylation / Proto-oncogene / SH2 domain / SH3 domain / Tyrosine-protein kinase

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