Results 201 to 210 of about 12,929 (212)
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Discovery of acridine-based LSD1 inhibitors as immune activators targeting LSD1 in gastric cancer
European Journal of Medicinal Chemistry, 2023LSD1 is overexpressed in various cancers and promotes tumor cell proliferation, tumor expansion, and suppresses immune cells infiltration and is closely associated with immune checkpoint inhibitors therapy. Therefore, the inhibition of LSD1 has been recognized as a promising strategy for cancer therapy.
Hui-Min Liu +8 more
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Trends in Endocrinology & Metabolism, 2017
The histone lysine-specific demethylase 1 (LSD1) is a new and important player in the regulation of brown fat identity and function. In a recent Cell Reports article, Duteil et al. show that LSD1 exerts its effects via regulation of specific histone marks as well as through association with co-repressor complexes.
Leon G. Straub, Christian Wolfrum
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The histone lysine-specific demethylase 1 (LSD1) is a new and important player in the regulation of brown fat identity and function. In a recent Cell Reports article, Duteil et al. show that LSD1 exerts its effects via regulation of specific histone marks as well as through association with co-repressor complexes.
Leon G. Straub, Christian Wolfrum
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Modeling LSD1-Mediated Tumor Stagnation
Bulletin of Mathematical Biology, 2021LSD1 (KDMA1) has gained attention in the last decade as a cancer biomarker and drug target. In particular, recent work suggests that LSD1 inhibition alone reduces tumor growth, increases T cell tumor infiltration, and complements PD1/PDL1 checkpoint inhibitor therapy.
Jesse Milzman +2 more
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Baicalin, a natural LSD1 inhibitor
Bioorganic Chemistry, 2016Baicalin is one of the active ingredients in the skullcap, with a variety of pharmacological effects, such as blood pressure reduction, sedation, liver-protection, gallbladder-protection, anti-bacteria, and anti-inflammation. In our study, baicalin was first characterized as a LSD1 inhibitor with an IC50 of 3.01μM and showed strong LSD1 inhibitory ...
Xue-Qi Liu +12 more
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LSD1 inhibition: a therapeutic strategy in cancer?
Expert Opinion on Therapeutic Targets, 2012The role of epigenetic dysfunction in cancer is increasingly appreciated. This has raised the question as to whether enzymes that regulate the structure and function of chromatin might represent novel therapeutic targets. The histone demethylase LSD1 is one such candidate and novel, potent inhibitors are under development.The literature on LSD1 (also ...
Lynch, James T. +2 more
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p53 is regulated by the lysine demethylase LSD1
Nature, 2007p53, the tumour suppressor and transcriptional activator, is regulated by numerous post-translational modifications, including lysine methylation. Histone lysine methylation has recently been shown to be reversible; however, it is not known whether non-histone proteins are substrates for demethylation.
Ramin Shiekhattar +10 more
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B cells turn on, tune in with LSD1
Nature Immunology, 2018The histone demethylase LSD1 partners with the transcription factor BCL6 to initiate the formation of germinal centers.
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Histone demethylase LSD1 and its biological functions
Hereditas (Beijing), 2010Discovery of histone lysine specific demethylase 1 (LSD1) indicates that even histone methylation is reversible. Structural analysis shows that LSD1 is a flavin-dependent amine oxidase, which is able to catalyze the specific removal of methyl groups from mono- and dimethylated Lys4 and Lys9 of histone H3.
Sang +5 more
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LSD1 inhibitors: a patent review (2010-2015)
Expert Opinion on Therapeutic Patents, 2016Lysine demethylase 1 (LSD1) plays an important role in mediating the expression of genes involved in cancer and non-cancer diseases such as viral infections, cardiovascular and neurodegenerative disorders. It is involved in a number of processes from adipogenesis to cell adhesion to viral latency, regulating several cell pathways related with ...
STAZI, Giulia +3 more
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A Mechanism-Based Inactivator for Histone Demethylase LSD1
Journal of the American Chemical Society, 2006Histone demethylase LSD1 is a flavin-dependent amine oxidase that catalyzes the oxidative removal of one or two methyl groups from the methyl-lysine-4 side chain of histone H3. We have designed and synthesized two peptide-based inhibitor analogues that block LSD1.
Xin Liu +5 more
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