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TitleDiscovery of a Series of Covalent Ligands That Bind to Cys77 of the Von Hippel-Lindau Tumor Suppressor Protein (VHL).
Journal, issue, pagesAcs Med. Chem. Lett., Vol. 16, Page 693-699, Year 2025
Publish dateAug 19, 2024 (structure data deposition date)
AuthorsLucas, S.C.C. / Xu, Y. / Hewitt, S. / Collie, G.W. / Fusani, L. / Kadamur, G. / Hadfield, T.E. / Su, N. / Truman, C. / Demanze, S. ...Lucas, S.C.C. / Xu, Y. / Hewitt, S. / Collie, G.W. / Fusani, L. / Kadamur, G. / Hadfield, T.E. / Su, N. / Truman, C. / Demanze, S. / Hao, H. / Phillips, C.
External linksAcs Med. Chem. Lett. / PubMed:40236540
MethodsX-ray diffraction
Resolution1.486 Å
Structure data

PDB-9gio:
Crystal structure of the VHL-EloC-EloB complex with a covalent compound bound to C77 of VHL.
Method: X-RAY DIFFRACTION / Resolution: 1.486 Å

Chemicals

ChemComp-3JF:
N-acetyl-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide

PDB-1imd:
STRUCTURAL STUDIES OF METAL BINDING BY INOSITOL MONOPHOSPHATASE: EVIDENCE FOR TWO-METAL ION CATALYSIS

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsLIGASE / VHL / covalent / fragment / E3 ligase

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