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Structure paper

TitleOvercoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.
Journal, issue, pagesNature, Vol. 534, Page 129-132, Year 2016
Publish dateAug 7, 2015 (structure data deposition date)
AuthorsJia, Y. / Yun, C.H. / Park, E. / Ercan, D. / Manuia, M. / Juarez, J. / Xu, C. / Rhee, K. / Chen, T. / Zhang, H. ...Jia, Y. / Yun, C.H. / Park, E. / Ercan, D. / Manuia, M. / Juarez, J. / Xu, C. / Rhee, K. / Chen, T. / Zhang, H. / Palakurthi, S. / Jang, J. / Lelais, G. / DiDonato, M. / Bursulaya, B. / Michellys, P.Y. / Epple, R. / Marsilje, T.H. / McNeill, M. / Lu, W. / Harris, J. / Bender, S. / Wong, K.K. / Janne, P.A. / Eck, M.J.
External linksNature / PubMed:27251290
MethodsX-ray diffraction
Resolution2.31 Å
Structure data

PDB-5d41:
EGFR kinase domain in complex with mutant selective allosteric inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.31 Å

Chemicals

ChemComp-MG:
Unknown entry

ChemComp-ANP:
PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER / AMP-PNP, energy-carrying molecule analogue*YM

ChemComp-57N:
(2R)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-2-phenyl-N-(1,3-thiazol-2-yl)acetamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Allosteric inhibitor / EGFR / TRANSFERASE-TRANSFERASE INHIBITOR complex

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