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TitleA biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders.
Journal, issue, pagesEur. J. Med. Chem., Vol. 219, Page 113435-113435, Year 2021
Publish dateApr 7, 2021 (structure data deposition date)
AuthorsFischer, P.D. / Papadopoulos, E. / Dempersmier, J.M. / Wang, Z.F. / Nowak, R.P. / Donovan, K.A. / Kalabathula, J. / Gorgulla, C. / Junghanns, P.P.M. / Kabha, E. ...Fischer, P.D. / Papadopoulos, E. / Dempersmier, J.M. / Wang, Z.F. / Nowak, R.P. / Donovan, K.A. / Kalabathula, J. / Gorgulla, C. / Junghanns, P.P.M. / Kabha, E. / Dimitrakakis, N. / Petrov, O.I. / Mitsiades, C. / Ducho, C. / Gelev, V. / Fischer, E.S. / Wagner, G. / Arthanari, H.
External linksEur. J. Med. Chem. / PubMed:33892272
MethodsX-ray diffraction
Resolution1.91 Å
Structure data

PDB-7meu:
A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders
Method: X-RAY DIFFRACTION / Resolution: 1.91 Å

Chemicals

ChemComp-MGP:
7-METHYL-GUANOSINE-5'-TRIPHOSPHATE

ChemComp-Z5D:
(2E)-2-{2-[4-([1,1'-biphenyl]-4-yl)-1,3-thiazol-2-yl]hydrazinylidene}-3-(2-nitrophenyl)propanoic acid

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsPROTEIN BINDING / Inhibitor / Complex / eIF4E

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