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TitleGSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Journal, issue, pagesAcs Med. Chem. Lett., Vol. 11, Page 1581-1587, Year 2020
Publish dateJun 2, 2020 (structure data deposition date)
AuthorsPreston, A. / Atkinson, S.J. / Bamborough, P. / Chung, C.W. / Gordon, L.J. / Grandi, P. / Gray, J.R.J. / Harrison, L.A. / Lewis, A.J. / Lugo, D. ...Preston, A. / Atkinson, S.J. / Bamborough, P. / Chung, C.W. / Gordon, L.J. / Grandi, P. / Gray, J.R.J. / Harrison, L.A. / Lewis, A.J. / Lugo, D. / Messenger, C. / Michon, A.M. / Mitchell, D.J. / Prinjha, R.K. / Rioja, I. / Seal, J. / Taylor, S. / Thesmar, P. / Wall, I.D. / Watson, R.J. / Woolven, J.M. / Demont, E.H.
External linksAcs Med. Chem. Lett. / PubMed:32832027
MethodsX-ray diffraction
Resolution1.55 Å
Structure data

PDB-6z8p:
C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH GSK973
Method: X-RAY DIFFRACTION / Resolution: 1.55 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-1PG:
2-(2-{2-[2-(2-METHOXY-ETHOXY)-ETHOXY]-ETHOXY}-ETHOXY)-ETHANOL

ChemComp-QC8:
(2~{S},3~{S})-2-(fluoranylmethyl)-~{N}7-methyl-~{N}5-[(1~{R},5~{S})-3-oxabicyclo[3.1.0]hexan-6-yl]-3-phenyl-2,3-dihydro-1-benzofuran-5,7-dicarboxamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / INHIBITOR / HISTONE / EPIGENETIC READER / BROMODOMAIN / BRD2 / BROMODOMAIN CONTAINING PROTEIN 2 / ANTAGONIST

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