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TitleDiscovery and Functional Characterization of a Potent, Selective, and Metabolically Stable PROTAC of the Protein Kinases DYRK1A and DYRK1B.
Journal, issue, pagesJ. Med. Chem., Vol. 67, Page 17259-17289, Year 2024
Publish dateJun 6, 2023 (structure data deposition date)
AuthorsWilms, G. / Schofield, K. / Maddern, S. / Foley, C. / Shaw, Y. / Smith, B. / Basantes, L.E. / Schwandt, K. / Babendreyer, A. / Chavez, T. ...Wilms, G. / Schofield, K. / Maddern, S. / Foley, C. / Shaw, Y. / Smith, B. / Basantes, L.E. / Schwandt, K. / Babendreyer, A. / Chavez, T. / McKee, N. / Gokhale, V. / Kallabis, S. / Meissner, F. / Rokey, S.N. / Dunckley, T. / Montfort, W.R. / Becker, W. / Hulme, C.
External linksJ. Med. Chem. / PubMed:39344427
MethodsX-ray diffraction
Resolution1.85 Å
Structure data

PDB-8t2h:
DYRK1A complex with DYR530
Method: X-RAY DIFFRACTION / Resolution: 1.85 Å

Chemicals


ChemComp, No image

ChemComp-XIR:
Unknown entry

ChemComp-PG4:
TETRAETHYLENE GLYCOL / precipitant*YM

ChemComp-GOL:
GLYCEROL

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsLIGASE/LIGASE INHIBITOR / Kinase / Inhibitor / Alzheimer's Disease / LIGASE / LIGASE-LIGASE INHIBITOR complex

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