Results 61 to 70 of about 19,155 (194)

Hitting histone demethylases [PDF]

Science-Business eXchange, 2012
A GSK–Structural Genomics Consortium team has identified the first potent and selective histone demethylase inhibitor and shown that the molecule dampens the macrophage inflammatory response. The pharma now is focusing on internal efforts and external approaches to exploring potential therapeutic applications of the inhibitor.
openaire   +1 more source

Histone lysine demethylases in breast cancer [PDF]

Critical Reviews in Oncology/Hematology, 2013
Histone lysine demethylases (KDMs) have been recently discovered in mammals and have been nicknamed "erasers" for their ability to remove methyl groups from histone substrates. In cancer cells, KDMs can activate or repress gene transcription, behaving as oncogenes or tumor suppressors depending upon the cellular context.
PAOLICCHI, ELISA, F. Crea, W. L. Farrar, J. E. Green, DANESI, ROMANO   +4 more
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Master Regulator SMC1A, Stabilized by N6‐Methyladenosine Reader IGF2BP1, Promotes HCC Progression Through Facilitating Enhancer–Promoter Interaction of Nestin

Advanced Science, EarlyView.
IGF2BP1‐mediated m6A stabilization sustains SMC1A expression, enabling cohesin‐associated chromatin regulation of Nestin in hepatocellular carcinoma. This work reveals an epitranscriptomic‐chromatin‐cytoskeletal regulatory axis linked to malignant phenotypes and identifies SMC1A as a biologically relevant vulnerability in HCC.
Zhenxiang Peng, Diguang Wen, Lu Zeng, Lin Lv, Shengtao Liao, Wenguang Zhang, Zhechuan Mei, Chuanfei Li   +7 more
wiley   +1 more source

Targeting KDM3B Elicits Anti‐tumor Immunity by Alleviating SHP1–mediated STING Suppression in Triple–Negative Breast Cancer

Advanced Science, EarlyView.
P3FI–90 treatment targets KDM3B, reshapes the epigenetic landscape, and suppresses SHP1 expression, thereby activating STING–TBK1–IRF3–type I IFN signaling pathway. Consequently, CD8+ T cells are recruited to the tumor site and activated to produce IFN–γ and GZMB, leading to the killing of TNBC cells.
Xiaolong Wang, Wenhao Li, Yifei Wang, Ning Zhang, Bing Chen, Wenjing Zhao, Lijuan Wang, Dan Luo, Qifeng Yang   +8 more
wiley   +1 more source

Posttranslational modifications of the histone 3 tail and their impact on the activity of histone lysine demethylases in vitro. [PDF]

PLoS ONE, 2013
Posttranslational modifications (PTMs) of the histone H3 tail such as methylation, acetylation and phosphorylation play important roles in epigenetic signaling.
Brian Lohse, Charlotte Helgstrand, Jan B L Kristensen, Ulrike Leurs, Paul A C Cloos, Jesper L Kristensen, Rasmus P Clausen   +6 more
doaj   +1 more source

Tumor suppression by the histone demethylase UTX [PDF]

Cell Cycle, 2010
Aberrant epigenetic regulation can alter cell fates and result in unrestrained cell growth, leading to cancer development. Understanding the complex epigenetic pathways may point the way for advanced cancer therapy. Several recent studies identified mutations in components of the chromatin modification machinery in different types of cancer 1-3 ...
Miao-Chih, Tsai, Jordon K, Wang, Howard Y, Chang   +2 more
openaire   +2 more sources

Histone Modification Complex JMJ704‐HDA709 Negatively Regulates Salinity Tolerance in Rice

Advanced Science, EarlyView.
This study reveals that the rice histone demethylase JMJ704 interacts with HDA709―a H3K9ac deacetylase characterized herein―to form a chromatin‐modifying complex. Under salt stress, OsWRKY72 recruits this complex through interaction with JMJ704 to target loci, repressing the expression of oxidative stress and salt‐responsive genes via removal of ...
Jing Wang, Zhengting Chen, Pengxiang Bai, Biao Liu, Lingling Meng, Jian Zhang, Xu Li, Dao‐Xiu Zhou, Xuan Ma, Yu Zhao   +9 more
wiley   +1 more source

A scintillation proximity assay for histone demethylases

Analytical Biochemistry, 2014
Covalent modifications, such as methylation and demethylation of lysine residues in histones, play important roles in chromatin dynamics and the regulation of gene expression. The lysine demethylases (KDMs) catalyze the demethylation of lysine residues on histone tails and are associated with diverse human diseases, including cancer, and are therefore ...
Wenyu Yu, Mohammad S. Eram, Taraneh Hajian, Aleksandra Szykowska, Nicola Burgess-Brown, Masoud Vedadi, Peter J. Brown   +6 more
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Histone demethylases in chromatin cross‐talks [PDF]

Biology of the Cell, 2011
The ‘histone code’ hypothesis states that chromatin‐based regulation of nuclear processes such as transcription is brought about by the combination of distinct modifications (histone marks) at specific loci. Its correct establishment involves chromatin cross‐talks, ensuring an ordered and concerted deposition/removal of a particular set of ...
Laure, Verrier, Marie, Vandromme, Didier, Trouche   +2 more
openaire   +2 more sources

Mechanical Activation of Piezo1 Drives Osteoarthritis Through Kdm5c‐Mediated Epigenetic Silencing

Advanced Science, EarlyView.
Excessive mechanical stress activates Piezo1, triggering Ca2+‐dependent cytoskeletal forces that deform the nucleus and reduce H3K4me3. Kdm5c demethylates H3K4me3 at Col2a1 and Runx3 promoters. Kdm5c knockout rescues degradation. Repurposed telmisartan directly inhibits Kdm5c, blocking this axis and showing disease‐modifying efficacy in mouse OA models
Tianyou Kan, Xuran Li, Han Wang, Lin Sun, Yao Wang, Jiangdong Wu, Junqi Cui, Yiqi Yang, Kai Yuan, Linyang Chu, Liao Wang, Hanjun Li, Mengning Yan, Zhifeng Yu   +13 more
wiley   +1 more source