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TitlePhenotype-Led Identification of IL-10 Upregulators in Human CD4 + T-cells and Elucidation of Their Pharmacology as Highly Selective CDK8/CDK19 Inhibitors.
Journal, issue, pagesJ. Med. Chem., Vol. 68, Page 1883-1900, Year 2025
Publish dateOct 29, 2024 (structure data deposition date)
AuthorsNicolle, S. / Barker, M. / Barrett, J. / Campbell, M. / Wojno-Picon, J. / Atkinson, S.J. / Aylott, H. / Kessedjian, H. / He, Y. / Messenger, C. ...Nicolle, S. / Barker, M. / Barrett, J. / Campbell, M. / Wojno-Picon, J. / Atkinson, S.J. / Aylott, H. / Kessedjian, H. / He, Y. / Messenger, C. / Roberts, E. / Spitzfaden, C. / Le, J. / Zinn, N. / Werner, T. / Dumpelfeld, B. / Bantscheff, M. / Somers, D.O. / Reid, H. / Thang, K. / Gobbetti, T. / Lewis, H.D.
External linksJ. Med. Chem. / PubMed:39780505
MethodsX-ray diffraction
Resolution2.157 - 2.573 Å
Structure data

PDB-9h8c:
Human CDK8/Cyclin-C complex with inhibitor 2-9
Method: X-RAY DIFFRACTION / Resolution: 2.573 Å

PDB-9h8s:
Human CDK8/Cyclin-C complex with inhibitor 3-7
Method: X-RAY DIFFRACTION / Resolution: 2.157 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-GOL:
GLYCEROL

PDB-1is8:
Crystal structure of rat GTPCHI/GFRP stimulatory complex plus Zn

ChemComp-DMS:
DIMETHYL SULFOXIDE / DMSO, precipitant*YM

ChemComp-HOH:
WATER

ChemComp-CL:
Unknown entry

PDB-1itf:
INTERFERON ALPHA-2A, NMR, 24 STRUCTURES

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / Kinase / Inhibitor / CDK8 / Cyclin Dependent Kinase / Cyclin / Transcription-Transferase-Inhibitor Complex

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