Results 61 to 70 of about 22,216 (225)

Negative regulation of the androgen receptor gene through a primate specific androgen response element present in the 5' UTR [PDF]

, 2014
Open Access This article is distributed under the terms of the Creative Commons Attribution License which permits any use, distribution, and reproduction in any medium, provided the original author(s) and the source are credited.
Hay, Colin W, Hunter, Irene, Lavery, Derek N, MacKenzie, Alasdair, McEwan, Iain J, Watt, Kate   +5 more
core   +2 more sources

The kinase NEK6 positively regulates LSD1 activity and accumulation in local chromatin sub-compartments

Communications Biology
LSD1 plays a crucial role in mammalian biology, regulated through interactions with coregulators and post-translational modifications. Here we show that the kinase NEK6 stimulates LSD1 activity in cells and observe a strong colocalization of NEK6 and ...
Franziska Knodel, Jürgen Eirich, Sabine Pinter, Stephan A. Eisler, Iris Finkemeier, Philipp Rathert   +5 more
doaj   +1 more source

Reduced Maintenance DNA Methylation Thresholds Enable Sensitive Reporter Assays for UHRF1 and DNMT1 Inhibition

Advanced Science, EarlyView.
The authors engineer colorectal cancer cells with reduced redundancy of UHRF1 and DNMT1, key DNA methylation maintenance factors, lowering the maintenance threshold and sensitizing cells to inhibition. They develop reporter assays driven by endogenous tumor‐suppressor gene promoters with enhanced sensitivity and dynamic range to demethylating drugs ...
Cuicui Xia, Ying Cui, Jiongliang Wang, Wenjing Bai, Danyang Wang, Yao Chen, Huahui Guo, Liangyi Zong, Bing Qin, Xintong Cai, Jie Wang, Jing Huang, Scott B. Rothbart, Zufeng Guo, Stephen B. Baylin, Xiangqian Kong   +15 more
wiley   +1 more source

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

ACS Medicinal Chemistry Letters, 2020
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1.
Victor S. Gehling, John P. McGrath, Martin Duplessis, Avinash Khanna, Francois Brucelle, Rishi G. Vaswani, Alexandre Côté, Jacob Stuckey, Venita Watson, Richard T. Cummings, Srividya Balasubramanian, Priyadarshini Iyer, Priyanka Sawant, Andrew C. Good, Brian K. Albrecht, Jean-Christophe Harmange, James E. Audia, Steven F. Bellon, Patrick Trojer, Julian R. Levell   +19 more
openaire   +3 more sources

LSD1 demethylates histone and non-histone proteins [PDF]

Epigenetics, 2009
One of the key breakthroughs in the epigenetics/chromatin field in the last several years was the identification of enzymes capable of removing the methyl group from methylated lysines in histone proteins. Lysine-specific demethylase 1 (LSD1) was the first such enzyme identified, which has been shown to demethylate histone H3 on lysine 4 (H3K4) and ...
Thomas B, Nicholson, Taiping, Chen
openaire   +2 more sources

LSD1 inhibition suppresses the growth of clear cell renal cell carcinoma via upregulating P21 signaling

Acta Pharmaceutica Sinica B, 2019
Histone lysine-specific demethylase 1 (LSD1) has been implicated in the disease progression of several types of solid tumors. This study provides the first evidence showing that LSD1 overexpression occurred in 62.6% (224/358) of clear cell renal cell ...
Liangsong Zhu, Jianfeng Wang, Wen Kong, Jiwei Huang, Baijun Dong, Yiran Huang, Wei Xue, Jin Zhang   +7 more
doaj   +1 more source

T Cell Exhaustion in Cancer Immunotherapy: Heterogeneity, Mechanisms, and Therapeutic Opportunities

Advanced Science, EarlyView.
T cell exhaustion limits immunotherapy efficacy. This article delineates its progression from stem‐like to terminally exhausted states, governed by persistent antigen, transcription factors, epigenetics, and metabolism. It maps the exhaustion landscape in the TME and proposes integrated reversal strategies, providing a translational roadmap to overcome
Yang Yu, Xiaoyu Yao, Qingyang Wang, Mengrui Yang, Runze Li, Jiangjiang Qin, Jing Zhuang, Changgang Sun   +7 more
wiley   +1 more source

LSD1 protects against hippocampal and cortical neurodegeneration [PDF]

Nature Communications, 2017
AbstractTo investigate the mechanisms that maintain differentiated cells, here we inducibly delete the histone demethylase LSD1/KDM1A in adult mice. Loss of LSD1 leads to paralysis, along with widespread hippocampus and cortex neurodegeneration, and learning and memory defects.
Michael A. Christopher, Dexter A. Myrick, Benjamin G. Barwick, Amanda K. Engstrom, Kirsten A. Porter-Stransky, Jeremy M. Boss, David Weinshenker, Allan I. Levey, David J. Katz   +8 more
openaire   +3 more sources

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma [PDF]

, 2018
Medulloblastoma is one of the most frequent among pediatric brain tumors, and it has been classified in various subgroups. Some of them already benefit from quite good therapeutic options, whereas others urgently need novel therapeutic approaches ...
Annalisa Romanelli, Antonello Mai, Antonello Mai, Clemens Zwergel, Giulia Stazi, Giuseppina Catanzaro, Marco Tafani, Sergio Valente, Zein Mersini Besharat   +8 more
core   +2 more sources

Sensing and Filtering Environmental Fluctuations: The Case of Biomolecular Condensates in Plants

Advanced Science, EarlyView.
The diversity of plant condensates reflects constraints of sessile organisms to coordinate postembryonic development with environmental adaptation. This review examines how plants employ condensates to integrate temperature, light, redox, and nutrient signals.
Panagiotis N. Moschou, Dorothee Staiger
wiley   +1 more source