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Structure paper

TitleMolecular glues that facilitate RAS binding to PI3K alpha promote glucose uptake without insulin.
Journal, issue, pagesScience, Vol. 389, Page 402-408, Year 2025
Publish dateJul 15, 2024 (structure data deposition date)
AuthorsTerayama, K. / Furuzono, S. / Fer, N. / Yan, W. / Young, L.C. / Czyzyk, D.J. / Goldstein de Salazar, R. / Sasaki, M. / Uozumi, A. / Konishi, M. ...Terayama, K. / Furuzono, S. / Fer, N. / Yan, W. / Young, L.C. / Czyzyk, D.J. / Goldstein de Salazar, R. / Sasaki, M. / Uozumi, A. / Konishi, M. / Kanda, S. / Sogawa, Y. / Yamaguchi, M. / Tsuji, T. / Kuroyanagi, J. / Hayashi, M. / Ogura, Y. / Simanshu, D.K. / Kubota, K. / Tanaka, J. / McCormick, F.
External linksScience / PubMed:40705882
MethodsX-ray diffraction
Resolution1.75 - 3.01 Å
Structure data

PDB-9cmk:
Crystal structure of p110alpha-RAS binding domain (RBD) in complex with molecular glue D927
Method: X-RAY DIFFRACTION / Resolution: 1.75 Å

PDB-9cml:
Crystal structure of p110alpha-RAS binding domain (RBD) in complex with molecular glue D223
Method: X-RAY DIFFRACTION / Resolution: 2.01 Å

PDB-9cmv:
Crystal structure of the KRAS-p110alpha complex in the presence of molecular glue D223
Method: X-RAY DIFFRACTION / Resolution: 3.01 Å

Chemicals

PDB-1atf:
Unknown entry

ChemComp-MG:
Unknown entry

ChemComp-MRD:
(4R)-2-METHYLPENTANE-2,4-DIOL / precipitant*YM

ChemComp-MPD:
(4S)-2-METHYL-2,4-PENTANEDIOL / precipitant*YM

ChemComp-HOH:
WATER

PDB-1azd:
CONCANAVALIN FROM CANAVALIA BRASILIENSIS

ChemComp-GOL:
GLYCEROL

ChemComp-GNP:
PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER / GppNHp, GMPPNP, energy-carrying molecule analogue*YM

Source
  • homo sapiens (human)
KeywordsSIGNALING PROTEIN / RAS / PI3Kalpha / p110alpha / PIK3CA / RBD / glue / D927 / D223 / oncoprotein / KRAS / inducer compound

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