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TitleInsights into the Aberrant Activity of Mutant EGFR Kinase Domain and Drug Recognition.
Journal, issue, pagesStructure, Vol. 21, Page 209-219, Year 2013
Publish dateNov 21, 2012 (structure data deposition date)
AuthorsGajiwala, K.S. / Feng, J. / Ferre, R. / Ryan, K. / Brodsky, O. / Weinrich, S. / Kath, J.C. / Stewart, A.
External linksStructure / PubMed:23273428
MethodsX-ray diffraction
Resolution1.71 - 3.37 Å
Structure data

PDB-4i1z:
Crystal structure of the monomeric (V948R) form of the gefitinib/erlotinib resistant EGFR kinase domain L858R+T790M
Method: X-RAY DIFFRACTION / Resolution: 3 Å

PDB-4i20:
Crystal structure of monomeric (V948R) primary oncogenic mutant L858R EGFR kinase domain
Method: X-RAY DIFFRACTION / Resolution: 3.34 Å

PDB-4i21:
Crystal structure of L858R + T790M EGFR kinase domain in complex with MIG6 peptide
Method: X-RAY DIFFRACTION / Resolution: 3.37 Å

PDB-4i22:
Structure of the monomeric (V948R)gefitinib/erlotinib resistant double mutant (L858R+T790M) EGFR kinase domain co-crystallized with gefitinib
Method: X-RAY DIFFRACTION / Resolution: 1.71 Å

PDB-4i23:
Crystal structure of the wild-type EGFR kinase domain in complex with dacomitinib (soaked)
Method: X-RAY DIFFRACTION / Resolution: 2.8 Å

PDB-4i24:
Structure of T790M EGFR kinase domain co-crystallized with dacomitinib
Method: X-RAY DIFFRACTION / Resolution: 1.8 Å

Chemicals

ChemComp-HOH:
WATER

ChemComp-IRE:
Gefitinib / medication, inhibitor*YM

ChemComp-SO4:
SULFATE ION

ChemComp-1C9:
(2E)-N-{4-[(3-chloro-4-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}-4-(piperidin-1-yl)but-2-enamide / medication, inhibitor*YM

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Kinase domain / Phosphotransfer / ATP binding / Transferase/Transferase Inhibitor / EGFR kinase domain / MIG6 peptide / Transferase-Transferase Inhibitor complex / Phosphotrasfer

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