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Structure paper

TitleA first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance.
Journal, issue, pagesNat Cancer, Vol. 5, Page 1250-1266, Year 2024
Publish dateApr 5, 2023 (structure data deposition date)
AuthorsWhitehead, C.E. / Ziemke, E.K. / Frankowski-McGregor, C.L. / Mumby, R.A. / Chung, J. / Li, J. / Osher, N. / Coker, O. / Baladandayuthapani, V. / Kopetz, S. / Sebolt-Leopold, J.S.
External linksNat Cancer / PubMed:38992135
MethodsX-ray diffraction
Resolution1.855 - 2.687 Å
Structure data

PDB-8sc7:
Structure of EGFR in complex with MTX-531
Method: X-RAY DIFFRACTION / Resolution: 1.984 Å

PDB-8sc8:
Structure of PI3KG in complex with MTX-531
Method: X-RAY DIFFRACTION / Resolution: 2.687 Å

PDB-8sc9:
Structure of PPARG in complex with MTX-531
Method: X-RAY DIFFRACTION / Resolution: 1.855 Å

Chemicals

ChemComp-GOL:
GLYCEROL

ChemComp-CL:
Unknown entry


ChemComp, No image

ChemComp-D0D:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-SO4:
SULFATE ION

ChemComp-TAM:
TRIS(HYDROXYETHYL)AMINOMETHANE / pH buffer*YM

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/INHIBITOR / EGFR / dual EGFR/PI3K inhibitor / TRANSFERASE / TRANSFERASE-INHIBITOR complex / PI3KG / TRANSCRIPTION/INHIBITOR / TRANSCRIPTION / TRANSCRIPTION-INHIBITOR complex

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