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TitleDiscovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs.
Journal, issue, pagesAngew. Chem. Int. Ed. Engl., Vol. 60, Page 23327-23334, Year 2021
Publish dateAug 19, 2021 (structure data deposition date)
AuthorsLaw, R.P. / Nunes, J. / Chung, C.W. / Bantscheff, M. / Buda, K. / Dai, H. / Evans, J.P. / Flinders, A. / Klimaszewska, D. / Lewis, A.J. ...Law, R.P. / Nunes, J. / Chung, C.W. / Bantscheff, M. / Buda, K. / Dai, H. / Evans, J.P. / Flinders, A. / Klimaszewska, D. / Lewis, A.J. / Muelbaier, M. / Scott-Stevens, P. / Stacey, P. / Tame, C.J. / Watt, G.F. / Zinn, N. / Queisser, M.A. / Harling, J.D. / Benowitz, A.B.
External linksAngew. Chem. Int. Ed. Engl. / PubMed:34416073
MethodsX-ray diffraction
Resolution2.24 Å
Structure data

PDB-7pi4:
FAK Protac GSK215 in complex with FAK and pVHL:ElonginC:ElonginB
Method: X-RAY DIFFRACTION / Resolution: 2.24 Å

Chemicals

ChemComp-7QB:
(2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

ChemComp-PEG:
DI(HYDROXYETHYL)ETHER

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-CA:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / PROTAC

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