Jin-Lian Ma

TL;DR: Five series of 1,2,3-triazole-dithiocarbamate hybrids were designed and synthesized and screened their inhibitory activity toward LSD1 and it was found that some of these compounds exhibited the most specific and robust inhibition of LSD1.

TL;DR: A review of recent studies about LSD1 focuses on the basic physiological function of LSD1 and its involved mechanisms in pathophysiologic conditions, as well as the development of LSD 1 inhibitors as potential anticancer therapeutic agents.

TL;DR: Compound 8k showed potent and reversible inhibition against lysine specific demethylase 1 with an IC50 value of 0.39 μM, which was 74-fold more potent than that of tranylcypromine (2-PCPA) and further investigation revealed that compound 8k was active at both recombinant and cell levels by upregulating the expression of H3K4me1, H3 k4me2 and H3k9me2.

TL;DR: The [1,2,3]triazolo[4,5-d]pyrimidine scaffold can be used as the template for designing new LSD1 inhibitors and docking studies indicated that the hydrogen interaction between the nitrogen atom in the pyridine ring and Met332 could be responsible for the improved activity of 2-thiopyridine series.

TL;DR: Baicalin was first characterized as a LSD1 inhibitor with an IC50 of 3.01μM and showed strong LSD1 inhibitory effect in cells, and may serve as a template for designing flavone-based LSD1 inhibitors.