نتایج جستجو برای: آنزیم g9a

تعداد نتایج: 12176  

Journal: :Genes & development 2014
Bernhard Lehnertz Caroline Pabst Le Su Michelle Miller Feng Liu Lin Yi Regan Zhang Jana Krosl Eric Yung Jeanette Kirschner Patty Rosten T Michael Underhill Jian Jin Josée Hébert Guy Sauvageau R Keith Humphries Fabio M Rossi

Chromatin modulators are emerging as attractive drug targets, given their widespread implication in human cancers and susceptibility to pharmacological inhibition. Here we establish the histone methyltransferase G9a/EHMT2 as a selective regulator of fast proliferating myeloid progenitors with no discernible function in hematopoietic stem cells (HSCs). In mouse models of acute myeloid leukemia (...

Journal: :Molecular bioSystems 2010
Mariana D Plazas-Mayorca Joshua S Bloom Ulrike Zeissler Gary Leroy Nicolas L Young Peter A DiMaggio Leonid Krugylak Robert Schneider Benjamin A Garcia

Histones are highly conserved proteins that organize cellular DNA. These proteins, especially their N-terminal domains, are adorned with many post-translational modifications (PTMs) such as lysine methylation, which are associated with active or repressed transcriptional states. The lysine methyltransferase G9a and its interaction partner Glp1 can mono- or dimethylate histone H3 on lysine (H3K9...

2016
Nan Wang Xiaofeng Shen Senzhu Bao Shan-Wu Feng Wei Wang Yusheng Liu Yiquan Wang Xian Wang Xirong Guo Rong Shen Haibo Wu Liming Lei Shiqin Xu Fuzhou Wang

The neural balance between facilitation and inhibition determines the final tendency of central sensitization. Nerve injury-induced hypersensitivity was considered as the results from the enhanced ascending facilitation and the diminished descending inhibition. The role of dopaminergic transmission in the descending inhibition has been well documented, but its underlying molecular mechanisms ar...

Journal: :Genes & development 2011
Yoichi Shinkai Makoto Tachibana

The discovery of Suv39h1, the first SET domain-containing histone lysine methyltransferase (HKMT), was reported in 2000. Since then, research on histone methylation has progressed rapidly. Among the identified HKMTs in mammals, G9a and GLP are the primary enzymes for mono- and dimethylation at Lys 9 of histone H3 (H3K9me1 and H3K9me2), and exist predominantly as a G9a-GLP heteromeric complex th...

2017
Jolene Caifeng Ho Lissa Nurrul Abdullah Qing You Pang Sudhakar Jha Edward Kai-Hua Chow Henry Yang Hiroyuki Kato Lorenz Poellinger Jun Ueda Kian Leong Lee

Epigenetic mechanisms play important roles in the regulation of tumorigenesis, and hypoxia-induced epigenetic changes may be critical for the adaptation of cancer cells to the hypoxic microenvironment of solid tumors. Previously, we showed that loss-of-function of the hypoxia-regulated H3K9 methyltransferase G9A attenuates tumor growth. However, the mechanisms by which blockade of G9A leads to ...

Journal: :Nature chemical biology 2011
Masoud Vedadi Dalia Barsyte-Lovejoy Feng Liu Sylvie Rival-Gervier Abdellah Allali-Hassani Viviane Labrie Tim J Wigle Peter A Dimaggio Gregory A Wasney Alena Siarheyeva Aiping Dong Wolfram Tempel Sun-Chong Wang Xin Chen Irene Chau Thomas J Mangano Xi-Ping Huang Catherine D Simpson Samantha G Pattenden Jacqueline L Norris Dmitri B Kireev Ashutosh Tripathy Aled Edwards Bryan L Roth William P Janzen Benjamin A Garcia Arturas Petronis James Ellis Peter J Brown Stephen V Frye Cheryl H Arrowsmith Jian Jin

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 targets. Here we report the discovery of UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 treatment of a...

Journal: :Nature communications 2016
Xi Zhang Danni Peng Yuanxin Xi Chao Yuan Cari A Sagum Brianna J Klein Kaori Tanaka Hong Wen Tatiana G Kutateladze Wei Li Mark T Bedford Xiaobing Shi

The euchromatin histone methyltransferase 2 (also known as G9a) methylates histone H3K9 to repress gene expression, but it also acts as a coactivator for some nuclear receptors. The molecular mechanisms underlying this activation remain elusive. Here we show that G9a functions as a coactivator of the endogenous oestrogen receptor α (ERα) in breast cancer cells in a histone methylation-independe...

2016
Frann Antignano Mitchell Braam Michael R Hughes Alistair L Chenery Kyle Burrows Matthew J Gold Menno J Oudhoff David Rattray Timotheus Y Halim Alissa Cait Fumio Takei Fabio M Rossi Kelly M McNagny Colby Zaph

Innate lymphoid cells (ILCs) are emerging as important regulators of homeostatic and disease-associated immune processes. Despite recent advances in defining the molecular pathways that control development and function of ILCs, the epigenetic mechanisms that regulate ILC biology are unknown. Here, we identify a role for the lysine methyltransferase G9a in regulating ILC2 development and functio...

2010
Bernhard Lehnertz Jeffrey P. Northrop Frann Antignano Kyle Burrows Sima Hadidi Sarah C. Mullaly Fabio M.V. Rossi Colby Zaph

Accumulating evidence suggests that the regulation of gene expression by histone lysine methylation is crucial for several biological processes. The histone lysine methyltransferase G9a is responsible for the majority of dimethylation of histone H3 at lysine 9 (H3K9me2) and is required for the efficient repression of developmentally regulated genes during embryonic stem cell differentiation. Ho...

Journal: :Nucleic Acids Research 2005
Pierre-Olivier Estève Debasis Patnaik Hang Gyeong Chin Jack Benner Michael A. Teitell Sriharsa Pradhan

Methylation of lysine 9 (K9) in the N-terminus tail of histone H3 (H3) in chromatin is associated with transcriptionally silenced genes and is mediated by histone methyltransferases. Murine G9a is a 1263 amino acid H3-K9 methyltransferase that possesses characteristic SET domain and ANK repeats. In this paper, we have used a series of green fluorescent protein-tagged deletion constructs to iden...

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