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Structure paper

TitleMake the right measurement: Discovery of an allosteric inhibition site for p300-HAT.
Journal, issue, pagesStruct Dyn., Vol. 6, Page 054702-054702, Year 2019
Publish dateJun 21, 2019 (structure data deposition date)
AuthorsGardberg, A.S. / Huhn, A.J. / Cummings, R. / Bommi-Reddy, A. / Poy, F. / Setser, J. / Vivat, V. / Brucelle, F. / Wilson, J.
External linksStruct Dyn. / PubMed:31649965
MethodsX-ray diffraction
Resolution1.72 - 2.32 Å
Structure data

PDB-6pf1:
Crystal structure of the p300 acetyltransferase domain with allosteric inhibitor CPI-090 and CoA
Method: X-RAY DIFFRACTION / Resolution: 2.32 Å

PDB-6pgu:
Crystal structure of the p300 acetyltransferase domain with allosteric inhibitor CPI-076 and CoA
Method: X-RAY DIFFRACTION / Resolution: 1.72 Å

Chemicals

ChemComp-COA:
COENZYME A

ChemComp-OJ7:
3-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]-2-methyl-1H-indole

ChemComp-HOH:
WATER

ChemComp-OK7:
N-(thiophen-2-yl)acetamide

Source
  • homo sapiens (human)
  • synthetic construct (others)
KeywordsTRANSFERASE/INHIBITOR / EP300 / p300 acetyltransferase / chromatin modification / epigenetics / inhibitor / allosteric / TRANSFERASE / TRANSFERASE-INHIBITOR complex

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