Results 1 to 10 of about 11,397 (98)
LSD1: Biologic Roles and Therapeutic Targeting [PDF]
Epigenomics, 2016 LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase activity and has since been shown to have multiple essential roles in mammalian biology. Given its enzymatic activity and its high-level expression in many human malignancies, a significant recent focus has been the development of pharmacologic inhibitors.
Maiques-Diaz, Alba, Somervaille, Tim Cp
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Histone Demethylase LSD1 Regulates Adipogenesis [PDF]
Journal of Biological Chemistry, 2010 Epigenetic mechanisms, in particular the enzymatic modification of histones, are a crucial element of cell differentiation, a regulated process that allows a precursor cell basically to turn into a different cell type while maintaining the same genetic equipment.
Melina M, Musri +5 more
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LSD1/KDM1 isoform LSD1+8a contributes to neural differentiation in small cell lung cancer [PDF]
Biochemistry and Biophysics Reports, 2017 Small cell lung cancer (SCLC) is an aggressive neuroendocrine tumor characterized by rapid progression. The mechanisms that lead to a shift from initial therapeutic sensitivity to ultimate therapeutic resistance are poorly understood. Although the SCLC genomic landscape led to the discovery of promising agents targeting genetic alterations that were ...
Takanobu Jotatsu +18 more
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Visualizing the Histone Code on LSD1 [PDF]
Cell, 2007 In this issue, Garcia-Bassets et al. (2007) show that spurious transcriptional activation by unliganded nuclear receptors is inhibited by histone lysine methylation. This inhibitory histone modification code is efficiently countered by the ligand-dependent recruitment of histone lysine demethylases, including lysine-specific demethylase 1 (LSD1), which
Gamble, Matthew J., Kraus, W. Lee
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Science-Business eXchange, 2012 Two teams have independently provided preclinical proof of concept for using lysine-specific histone demethylase 1 inhibitors to treat acute myelogenous leukemia. One of the teams is now running a clinical trial of a generic monoamine oxidase inhibitor that counts the demethylase among its many targets, whereas at least four biotechs are advancing ...
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Trends of LSD1 Inhibitors in Viral Infections [PDF]
Future Medicinal Chemistry, 2018 .
Zwergel, Clemens +3 more
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LSD1: Expanding Functions in Stem Cells and Differentiation [PDF]
Cells, 2021 Embryonic stem cells (ESCs) and induced pluripotent stem cells (iPSC) provide a powerful model system to uncover fundamental mechanisms that control cellular identity during mammalian development. Histone methylation governs gene expression programs that play a key role in the regulation of the balance between self-renewal and differentiation of ESCs ...
Carlos Martinez-Gamero +2 more
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LSD1 Histone Demethylase Assays and Inhibition [PDF]
, 2016 The lysine-specific demethylase (LSD1) is a flavin-dependent amine oxidase that selectively removes one or two methyl groups from histone H3 at the Lys4 position. Along with histone deacetylases 1 and 2, LSD1 is involved in epigenetically silencing gene expression. LSD1 has been implicated as a potential therapeutic target in cancer and other diseases.
D, Hayward, P A, Cole
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SYNTHESIS, LSD1 INHIBITORY ACTIVITY, AND LSD1 BINDING MODEL OF OPTICALLY PURE LYSINE-PCPA CONJUGATES
Computational and Structural Biotechnology Journal, 2014 Compounds that inhibit the catalytic function of lysine-specific demethylase 1 (LSD1) are interesting as therapeutic agents. Recently, we identified three lysine-phenylcyclopropylamine conjugates, NCD18, NCD25, and NCD41, which are potent LSD1 inactivators.
Yukihiro Itoh +4 more
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Defective heart development in hypomorphic LSD1 mice [PDF]
Cell Research, 2011 Lysine-specific demethylase 1 (LSD1/AOF2/KDM1A), the first enzyme with specific lysine demethylase activity to be described, demethylates histone and non-histone proteins and is essential for mouse embryogenesis. LSD1 interacts with numerous proteins through several different domains, most notably the tower domain, an extended helical structure that ...
Thomas B, Nicholson +12 more
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