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- Publications
- Influence
Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.
- H. Xu, M. H. Lambert, +9 authors M. Milburn
- Biology, Medicine
- Molecular cell
- 11 March 2000
The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors for fatty acids (FAs) that regulate glucose and lipid homeostasis. We report the crystal structure of the PPAR delta… Expand
The PPARs: from orphan receptors to drug discovery.
- T. Willson, P. Brown, D. Sternbach, B. Henke
- Chemistry, Medicine
- Journal of medicinal chemistry
- 24 February 2000
Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma.
- S. Kliewer, S. S. Sundseth, +8 authors J. Lehmann
- Medicine
- Proceedings of the National Academy of Sciences…
- 1997
Peroxisome proliferator-activated receptors (PPARs) alpha and gamma are key regulators of lipid homeostasis and are activated by a structurally diverse group of compounds including fatty acids,… Expand
Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors α and γ
- S. A. Kliewer, S. S. Sundseth, +8 authors J. Lehmann
- Biology
- 29 April 1997
Peroxisome proliferator-activated receptors (PPARs) α and γ are key regulators of lipid homeostasis and are activated by a structurally diverse group of compounds including fatty acids, eicosanoids,… Expand
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
- Kyle D. Konze, A. Ma, +20 authors J. Jin
- Medicine, Biology
- ACS chemical biology
- 24 April 2013
EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a transcriptionally… Expand
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
- M. Vedadi, D. Barsyte-Lovejoy, +29 authors J. Jin
- Biology, Medicine
- Nature chemical biology
- 1 August 2011
Protein lysine methyltransferases G9a and GLP modulate the transcriptional repression of a variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as dimethylation of non-histone… Expand
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
- Wenyu Yu, Emma J. Chory, +25 authors M. Schapira
- Chemistry, Medicine
- Nature communications
- 18 December 2012
Selective inhibition of protein methyltransferases is a promising new approach to drug discovery. An attractive strategy towards this goal is the development of compounds that selectively inhibit… Expand
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
- F. Liu, D. Barsyte-Lovejoy, +11 authors J. Jin
- Chemistry, Medicine
- Journal of medicinal chemistry
- 31 October 2013
Among epigenetic "writers", "readers", and "erasers", the lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9me2) and nonhistone proteins, have… Expand
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia
- F. Grebien, M. Vedadi, +28 authors G. Superti-Furga
- Biology, Medicine
- Nature chemical biology
- 29 May 2015
The CEBPA gene is mutated in 9% of patients with acute myeloid leukemia (AML). Selective expression of a short 30 kDa C/EBPα translational isoform, termed p30, represents the most common type of… Expand
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.
- F. Liu, X. Chen, +17 authors J. Jin
- Chemistry, Medicine
- Journal of medicinal chemistry
- 24 December 2009
SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to the discovery of 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal structure of the… Expand