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TitleFrom DNA-Encoded Library Screening to AM-9747 - an MTA-Cooperative PRMT5 Inhibitor with Potent Oral in vivo Efficacy
Journal, issue, pagesTo Be Published
Publish dateMar 24, 2025 (structure data deposition date)
AuthorsAnderson, J. / Cowland, S. / Vestergaard, M. / Yang, Y. / Liu, S. / Fang, X. / Mukund, S. / GhimireRijal, S. / Carter, C. / Jasco, T. ...Anderson, J. / Cowland, S. / Vestergaard, M. / Yang, Y. / Liu, S. / Fang, X. / Mukund, S. / GhimireRijal, S. / Carter, C. / Jasco, T. / Savary, I. / Hughes, P.E. / Gouliaev, A. / Belmontes, B. / Caenepeel, S. / Franch, T. / Glad, S. / Husemoen, B. / Nielson, S.J.
External linksSearch PubMed
MethodsX-ray diffraction
Resolution3.1 Å
Structure data

PDB-9nwy:
Discovery of MTA-cooperative PRMT5 Inhibitors from Co-factor directed DNA-Encoded Library Screens
Method: X-RAY DIFFRACTION / Resolution: 3.1 Å

Chemicals

PDB-1b6y:
3,N4-ETHENO-2'-DEOXYCYTIDINE OPPOSITE ADENINE IN AN 11-MER DUPLEX, SOLUTION STRUCTURE FROM NMR AND MOLECULAR DYNAMICS, 2 STRUCTURES

ChemComp-MTA:
5'-DEOXY-5'-METHYLTHIOADENOSINE

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/INHIBITOR / PRMT5 / MTA-cooperative inhibitor / TRANSFERASE / TRANSFERASE-INHIBITOR complex

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