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TitleDiscovery and Optimization of First-in-Class Molecular Glue Degraders of the WIZ Transcription Factor for Fetal Hemoglobin Induction to Treat Sickle Cell Disease.
Journal, issue, pagesJ. Med. Chem., Vol. 67, Page 20682-20694, Year 2024
Publish dateSep 6, 2024 (structure data deposition date)
AuthorsKerrigan, J.R. / Thomsen, N.M. / Cernijenko, A. / Kochanek, S.E. / Dewhurst, J. / O'Brien, G. / Ware, N.F. / Sanchez, C.C. / Manning, J.R. / Ma, X. ...Kerrigan, J.R. / Thomsen, N.M. / Cernijenko, A. / Kochanek, S.E. / Dewhurst, J. / O'Brien, G. / Ware, N.F. / Sanchez, C.C. / Manning, J.R. / Ma, X. / Ornelas, E. / Savage, N.A. / Partridge, J.R. / Patterson, A.W. / Lam, P. / Dales, N.A. / Bonazzi, S. / Borikar, S. / Hinman, A.E. / Ting, P.Y.
External linksJ. Med. Chem. / PubMed:39541509
MethodsX-ray diffraction
Resolution2.95 - 3.35 Å
Structure data

PDB-9djt:
Ternary complex structure of Cereblon-DDB1 bound to WIZ(ZF7) and the molecular glue WIZ-5
Method: X-RAY DIFFRACTION / Resolution: 2.95 Å

PDB-9djx:
Ternary complex structure of Cereblon-DDB1 bound to WIZ(ZF7) and the molecular glue WIZ-6
Method: X-RAY DIFFRACTION / Resolution: 3.35 Å

Chemicals

ChemComp-ZN:
Unknown entry

ChemComp-SO4:
SULFATE ION

PDB-1a5h:
CATALYTIC DOMAIN OF HUMAN TWO-CHAIN TISSUE PLASMINOGEN ACTIVATOR COMPLEX OF A BIS-BENZAMIDINE

ChemComp-HOH:
WATER

PDB-1a5i:
CATALYTIC DOMAIN OF VAMPIRE BAT (DESMODUS ROTUNDUS) SALIVA PLASMINOGEN ACTIVATOR IN COMPLEX WITH EGR-CMK (GLU-GLY-ARG CHLOROMETHYL KETONE)

Source
  • homo sapiens (human)
KeywordsLIGASE / Cereblon / Molecular Glue / degradation

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