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TitleDiscovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases.
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 39, Page 127854-127854, Year 2021
Publish dateJan 29, 2021 (structure data deposition date)
AuthorsJi, Z. / Clark, R.F. / Bhat, V. / Matthew Hansen, T. / Lasko, L.M. / Bromberg, K.D. / Manaves, V. / Algire, M. / Martin, R. / Qiu, W. ...Ji, Z. / Clark, R.F. / Bhat, V. / Matthew Hansen, T. / Lasko, L.M. / Bromberg, K.D. / Manaves, V. / Algire, M. / Martin, R. / Qiu, W. / Torrent, M. / Jakob, C.G. / Liu, H. / Cole, P.A. / Marmorstein, R. / Kesicki, E.A. / Lai, A. / Michaelides, M.R.
External linksBioorg. Med. Chem. Lett. / PubMed:33631370
MethodsX-ray diffraction
Resolution2.607 Å
Structure data

PDB-7lje:
Discovery of Spirohydantoins as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases
Method: X-RAY DIFFRACTION / Resolution: 2.607 Å

Chemicals

ChemComp-Y2P:
2-[4-[(3'R,4S)-3'-fluoro-1-[2-[(4-fluorophenyl)methyl-[(1S)-2,2,2-trifluoro-1-methyl-ethyl]amino]-2-oxo-ethyl]-2,5-dioxo-spiro[imidazolidine-4,1'-indane]-5'-yl]pyrazol-1-yl]-N-methyl-acetamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / histone acetylation / TRANSFERASE-TRANSFERASE INHIBITOR complex

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