On March 15, 2019, Li, Zhong-Rui; Wang, Shuai; Yang, Linlin; Yuan, Xiao-Han; Suo, Feng-Zhi; Yu, Bin; Liu, Hong-Min published an article.Safety of Methyl 2-cyclopentanonecarboxylate The title of the article was Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors. And the article contained the following:
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 LSD1 over MAO-A/B and showed H3K4me2 competitive binding to LSD1. The interaction between H3K4me2 and LSD1 was also confirmed by the Co-IP assay. In LSD1 overexpressed A549 cells, compound D8 dose-dependently induced accumulation of LSD1 substrates H3K4me1/2 and H3K9me1/2, showed cellular target engagement to LSD1 and significantly inhibited cell migration of A549 cells. Docking studies suggested that compound D8 occupied the peptide binding region and therefore blocked the access of the peptide substrate to the FAD, finally leading to the demethylase activity inhibition of LSD1. The findings indicate that aryl hydrazines are new scaffolds for the design of LSD1 inhibitors, the identification of D8 provides further evidence for our previously proposed general principle that fused heterocycles with an amine group are potentially active toward LSD1 by competitive binding to LSD1 with H3 peptide substrates. The experimental process involved the reaction of Methyl 2-cyclopentanonecarboxylate(cas: 10472-24-9).Safety of Methyl 2-cyclopentanonecarboxylate
The Article related to lsd1 inhibitor experience discovery aryl hydrazine scaffolds, aryl hydrazines, epigenetic regulation, experience-based discovery, lsd1 inhibitors, [1, 2, 4] triazolo[1, 5- a] pyrimidine and other aspects.Safety of Methyl 2-cyclopentanonecarboxylate
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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics