HDAC5–LSD1 axis regulates antineoplastic effect of natural HDAC inhibitor sulforaphane in human breast cancer cells
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Cancer"
DOI: 10.1002/ijc.31419
Abstract: Our recent studies have shown that cross‐talk between histone deacetylase 5 (HDAC5) and lysine‐specific demethylase 1 (LSD1) facilitates breast cancer progression. In this work, we demonstrated that regulatory activity at −356 to −100 bp promoter… read more here.
Keywords: sulforaphane; lsd1; hdac5 lsd1; breast cancer ... See more keywords
Probing the interaction of the p53 C-terminal domain to the histone demethylase LSD1.
Sign Up to like & getrecommendations! Published in 2017 at "Archives of biochemistry and biophysics"
DOI: 10.1016/j.abb.2017.07.021
Abstract: The p53 transcription factor plays a central role in the regulation of the expression of several genes, and itself is post-translationally regulated through its different domains. Of particular relevance for p53 function is its intrinsically… read more here.
Keywords: terminal domain; demethylase; lsd1; p53 ... See more keywords
Oncogene LSD1 is epigenetically suppressed by miR-137 overexpression in human non-small cell lung cancer.
Sign Up to like & getrecommendations! Published in 2017 at "Biochimie"
DOI: 10.1016/j.biochi.2017.02.010
Abstract: PURPOSE We examined the epigenetic regulation of microRNA-137 (miR-137) on lysine-specific demethylase 1 (KDM1A, or LSD1) induced oncogenic effects in NSCLC. METHODS NSCLC cell lines, A549 and H460 cells were transfected with a mammalian LSD1 overexpression… read more here.
Keywords: mir 137; overexpression; mir; proliferation ... See more keywords
New tranylcypromine derivatives containing sulfonamide motif as potent LSD1 inhibitors to target acute myeloid leukemia: Design, synthesis and biological evaluation.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103808
Abstract: Lysine-specific demethylase 1 (LSD1) is frequently elevated in acute myeloid leukemia (AML) and often leads to tumorigenesis. In recent years, numerous LSD1 inhibitors based on tranylcypromine (TCP) scaffolding have reached clinical trials. Most TCP derivatives… read more here.
Keywords: myeloid leukemia; lsd1 inhibitors; acute myeloid; lsd1 ... See more keywords
LSD1 Controls Timely MyoD Expression via MyoD Core Enhancer Transcription.
Sign Up to like & getrecommendations! Published in 2017 at "Cell reports"
DOI: 10.1016/j.celrep.2017.01.078
Abstract: MyoD is a master regulator of myogenesis. Chromatin modifications required to trigger MyoD expression are still poorly described. Here, we demonstrate that the histone demethylase LSD1/KDM1a is recruited on the MyoD core enhancer upon muscle… read more here.
Keywords: transcription; expression; myod expression; lsd1 ... See more keywords
Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.10.021
Abstract: A new series of [1,2,4]triazolo[1,5-a]pyrimidine-based LSD1 inhibitors were designed, synthesized, and further evaluated for their cytotoxicity against MGC-803, EC109, A549 and PC-9 cells as well as the ability of inhibiting LSD1. Some of these compounds showed… read more here.
Keywords: a549 cells; design synthesis; triazolo; biological evaluation ... See more keywords
Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.01.075
Abstract: Phenelzine was first employed to design new aryl hydrazine-based LSD1 inhibitors based on the experience-based discovery (EBD) strategy. Among these compounds, D8 potently inhibited LSD1 (IC50 = 882.30 nM) in a reversible manner. Compound D8 was selective to… read more here.
Keywords: based discovery; aryl hydrazines; experience based; hydrazines new ... See more keywords
Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c02156
Abstract: LSD1 is identified as an essential drug target, which is closely correlated to the development of several tumor types. In this work, on the basis of comprehensive analysis of the binding site of LSD1 and… read more here.
Keywords: structure activity; study indolin; relationship study; lsd1 inhibitors ... See more keywords
YAP/TAZ drives cell proliferation and tumour growth via a polyamine-eIF5A hypusination-LSD1 axis.
Sign Up to like & getrecommendations! Published in 2022 at "Nature cell biology"
DOI: 10.1038/s41556-022-00848-5
Abstract: Metabolic reprogramming is central to oncogene-induced tumorigenesis by providing the necessary building blocks and energy sources, but how oncogenic signalling controls metabolites that play regulatory roles in driving cell proliferation and tumour growth is less… read more here.
Keywords: polyamine; cell proliferation; yap taz; lsd1 ... See more keywords
Loss of NR2E3 represses AHR by LSD1 reprogramming, is associated with poor prognosis in liver cancer
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-11106-2
Abstract: The aryl hydrocarbon receptor (AHR) plays crucial roles in inflammation, metabolic disorder, and cancer. However, the molecular mechanisms regulating AHR expression remain unknown. Here, we found that an orphan nuclear NR2E3 maintains AHR expression, and… read more here.
Keywords: ahr expression; cancer; lsd1; liver cancer ... See more keywords
The inhibition of LSD1 via sequestration contributes to tau-mediated neurodegeneration
Sign Up to like & getrecommendations! Published in 2020 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2013552117
Abstract: Significance We have made the discovery that pathological tau functions through the histone demethylase LSD1 in the Alzheimer’s disease pathway. Thus, we have identified a mechanism that links tau to the downstream neuronal dysfunction pathways.… read more here.
Keywords: tau mediated; tau; neurodegeneration; pathological tau ... See more keywords