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TitleTilting the Scales toward EGFR Mutant Selectivity: Expanding the Scope of Bivalent "Type V" Kinase Inhibitors.
Journal, issue, pagesJ. Med. Chem., Vol. 67, Page 21438-21469, Year 2024
Publish dateAug 2, 2023 (structure data deposition date)
AuthorsWittlinger, F. / Chitnis, S.P. / Pham, C.D. / Damghani, T. / Patel, K.B. / Mollers, M. / Schaeffner, I.K. / Abidakun, O.A. / Deng, M.Q. / Ogboo, B.C. ...Wittlinger, F. / Chitnis, S.P. / Pham, C.D. / Damghani, T. / Patel, K.B. / Mollers, M. / Schaeffner, I.K. / Abidakun, O.A. / Deng, M.Q. / Ogboo, B.C. / Rasch, A. / Beyett, T.S. / Buckley, B. / Feru, F. / Shaurova, T. / Knappe, C. / Eck, M.J. / Hershberger, P.A. / Scott, D.A. / Brandt, A.L. / Laufer, S.A. / Heppner, D.E.
External linksJ. Med. Chem. / PubMed:39626019
MethodsX-ray diffraction
Resolution2.49 - 2.99 Å
Structure data

PDB-8to3:
EGFR(T790M/V948R) in complex with LN5461
Method: X-RAY DIFFRACTION / Resolution: 2.49 Å

PDB-8to4:
EGFR(T790M/V948R) in complex with the allosteric inhibitor FRF-06-057
Method: X-RAY DIFFRACTION / Resolution: 2.99 Å

Chemicals

ChemComp-MG:
Unknown entry

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


ChemComp, No image

ChemComp-IXC:
Unknown entry

ChemComp-HOH:
WATER


ChemComp, No image

ChemComp-IXR:
Unknown entry

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Cancer / Inhibitor / Kinase

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