Design, synthesis and biological activity of 3-oxoamino-benzenesulfonamides as selective and reversible LSD1 inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2017.04.006
Abstract: Lysine specific demethylase 1 (LSD1) is a flavin-dependent amine oxidase that selectively removes one or two methyl groups from H3 at Lys4 and is recognized as a promising therapeutic target for cancer and other diseases.… read more here.
Keywords: design synthesis; oxoamino benzenesulfonamides; reversible lsd1; lsd1 inhibitors ... 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
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
LSD1 inhibitors from the roots of Pueraria lobata.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Asian natural products research"
DOI: 10.1080/10286020.2022.2032677
Abstract: One new 6a,11a-dehydropterocarpan derivative, 6-O-methyl-anhydrotuberosin (1), one new 6a-hydroxypterocarpan, (6aR,11aR,11bR)-hydroxytuberosone (7), and seven known compounds including two 6a,11a-dehydropterocarpans (2 and 4), two coumestans (3 and 5), one isoflavonoid (6) and two other phenolic compounds (8… read more here.
Keywords: pueraria lobata; lsd1 inhibitors; roots pueraria; inhibitors roots ... See more keywords
An Overview on Screening Methods for Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Current medicinal chemistry"
DOI: 10.2174/0929867324666170509114321
Abstract: BACKGROUND In the past few years, great of attention has been paid to the identification and characterization of selective and potent inhibitors of the first identified histone demethylase LSD1, which may erase mono- and di-methylated… read more here.
Keywords: lsd1 inhibitor; lsd1 inhibitors; chemistry; demethylase lsd1 ... See more keywords
QSAR Modeling, Molecular Docking and Molecular Dynamics Simulations Studies of Lysine-Specific Demethylase 1 (LSD1) Inhibitors as Anticancer Agents.
Sign Up to like & getrecommendations! Published in 2020 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520620666200721134010
Abstract: BACKGROUND Histone lysine demetylases1 (LSD1) is a promising medication to treat cancer, which plays a crucial role in epigenetic modulation of gene expression. Inhibition of LSD1with small molecules has emerged as a vital mechanism to… read more here.
Keywords: molecular dynamics; docking molecular; lsd1 inhibitors; cancer ... See more keywords
LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2023.1120911
Abstract: Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely H3K4me1/2 and H3K9me1/2, using FAD as the cofactor. It is ubiquitously… read more here.
Keywords: clinical trials; lsd1 inhibitors; covalent; cancer ... See more keywords