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TitleA Degron Blocking Strategy Towards Improved CRL4 CRBN Recruiting PROTAC Selectivity.
Journal, issue, pagesChembiochem, Vol. 24, Page e202300351-e202300351, Year 2023
Publish dateMar 23, 2023 (structure data deposition date)
AuthorsBouguenina, H. / Scarpino, A. / O'Hanlon, J.A. / Warne, J. / Wang, H.Z. / Wah Hak, L.C. / Sadok, A. / McAndrew, P.C. / Stubbs, M. / Pierrat, O.A. ...Bouguenina, H. / Scarpino, A. / O'Hanlon, J.A. / Warne, J. / Wang, H.Z. / Wah Hak, L.C. / Sadok, A. / McAndrew, P.C. / Stubbs, M. / Pierrat, O.A. / Hahner, T. / Cabry, M.P. / Le Bihan, Y.V. / Mitsopoulos, C. / Sialana, F.J. / Roumeliotis, T.I. / Burke, R. / van Montfort, R.L.M. / Choudhari, J. / Chopra, R. / Caldwell, J.J. / Collins, I.
External linksChembiochem / PubMed:37418539
MethodsX-ray diffraction
Resolution2.5 - 2.72 Å
Structure data

PDB-8oiz:
Crystal structure of human CRBN-DDB1 in complex with Pomalidomide
Method: X-RAY DIFFRACTION / Resolution: 2.5 Å

PDB-8ojh:
Crystal structure of human CRBN-DDB1 in complex with compound 4
Method: X-RAY DIFFRACTION / Resolution: 2.72 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-ZN:
Unknown entry

ChemComp-Y70:
S-Pomalidomide

ChemComp-HOH:
WATER

ChemComp-VP9:
4-azanyl-2-[(3~{S})-2,6-bis(oxidanylidene)piperidin-3-yl]-7-methoxy-isoindole-1,3-dione

Source
  • homo sapiens (human)
KeywordsPROTEIN BINDING / E3-ligase / Degradation / Glue / Protac

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