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Inhibition of histone demethylases by 4-carboxy-2,2′-bipyridyl compounds
DOI:
10.1002/cmdc.201100026
PMID:
21412984
Authors:
Kai-Hsuan
Chang
(University of Oxford)
,
Oliver N, F.
King
(University of Oxford)
,
Antony
Tumber
(University of Oxford)
,
Esther C. Y.
Woon
(University of Oxford)
,
Tom D.
Heightman
(University of Oxford)
,
Michael A.
Mcdonough
(University of Oxford)
,
Christopher J.
Schofield
(University of Oxford)
,
Nathan R.
Rose
(University of Oxford)
Co-authored by industrial partner:
No
Type:
Journal Paper
Journal:
Chemmedchem
, VOL 6 (5)
, PAGES 759 - 764
State:
Published (Approved)
Published:
March 2011
Abstract: Exploiting epigenetics: 2-Oxoglutarate (2OG)-dependent histone lysine demethylases, such as JMJD2E, are potential therapeutic targets in a range of diseases. Through structure–activity relationship studies and analyses, we identified a potent 4-carboxy-2,2′-bipyridyl compound, which inhibits JMJD2E with an IC50 value of 110 nM, representing a 66-fold improvement over the lead compound. These bipyridyl derivatives bind in the 2-oxoglutarate binding site.
Journal Keywords: bipyridyl derivatives; epigenetics; histone; demethylases; inhibitors; 2-oxoglutarate
Diamond Keywords: Epigenetics
Subject Areas:
Chemistry,
Biology and Bio-materials,
Medicine
Instruments:
I02-Macromolecular Crystallography
Added On:
06/04/2011 10:38
Discipline Tags:
Health & Wellbeing
Biochemistry
Chemistry
Structural biology
Organic Chemistry
Drug Discovery
Life Sciences & Biotech
Technical Tags:
Diffraction
Macromolecular Crystallography (MX)