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Strategies that regulate LSD1 for novel therapeutics
Histone methylation plays crucial roles in regulating chromatin structure and gene transcription in epigenetic modifications. Lysine-specific demethylase 1 (LSD1), the first identified histone demethylase, is universally overexpressed in various diseases.
Meng Li +7 more
doaj +3 more sources
LSD1: Biologic Roles and Therapeutic Targeting [PDF]
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
openaire +3 more sources
LSD1-mediated enhancer silencing attenuates retinoic acid signalling during pancreatic endocrine cell development. [PDF]
Developmental progression depends on temporally defined changes in gene expression mediated by transient exposure of lineage intermediates to signals in the progenitor niche.
Benner, Christopher W +14 more
core +2 more sources
Histone Demethylase LSD1 Regulates Adipogenesis [PDF]
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
openaire +2 more sources
Alternative splicing of LSD1+8a in neuroendocrine prostate cancer is mediated by SRRM4
Neuroendocrine prostate cancer (NEPC) is the most virulent form of prostate cancer. Importantly, our recent work examining metastatic biopsy samples demonstrates NEPC is increasing in frequency.
Daniel J. Coleman +16 more
doaj +1 more source
Summary: Targeting lysine-specific histone demethylase 1A (LSD1) can improve tumor immunogenicity of poorly immunogenic tumors, such as non-small cell lung cancer (NSCLC), with elevated T cell infiltration and sensitize tumors to anti-PD-1 therapy ...
Feiyu Tang +9 more
doaj +1 more source
LSD1/KDM1 isoform LSD1+8a contributes to neural differentiation in small cell lung cancer [PDF]
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
openaire +5 more sources
Sanguinarine, identified as a natural alkaloid LSD1 inhibitor, suppresses lung cancer cell growth and migration [PDF]
Objective(s): Lysine-specific demethylase1 (LSD1), an important class of histone demethylases, plays a crucial role in regulation of mammalian biology. The up-regulated LSD1 expression was frequently associated with progress and oncogenesis of multiple ...
Ting-ting Qin +7 more
doaj +1 more source
Visualizing the Histone Code on LSD1 [PDF]
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
openaire +2 more sources
LSD1 is essential for oocyte meiotic progression by regulating CDC25B expression in mice [PDF]
Mammalian oocytes are arrested at prophase I until puberty when hormonal signals induce the resumption of meiosis I and progression to meiosis II.
Chen, T +8 more
core +1 more source

