Jiangkun Yan

TL;DR: The design, synthesis and biochemical evaluation of novel tetrahydroquinoline-based reversible LSD1 inhibitors are reported, and it is suggested that tetrahYDroquinolin-based LSD1 inhibitor deserve further investigation for the treatment of LSD1 overexpressing cancer.

TL;DR: In this paper, a series of benzofuran derivatives were designed, synthesized and biochemical evaluated as novel LSD1 inhibitors based on scaffold hopping and conformational restriction strategy, and the representative compound 17i exhibited excellent LSD1 inhibition at the molecular levels with IC50 = 0.065μM, as well as anti-proliferation against MCF-7, MGC-803, H460, A549 and THP-1 tumor cells with IC 50 values of 2.90−±−0.32, 5.85−±-0.35

TL;DR: Wang et al. as mentioned in this paper made an extensive review of the research obtained from the literature retrieval of electronic databases, such as PubMed, Web of Science, RCSB PDB, ClinicalTrials.gov, and EU clinical trials register, covering January 2015 to June 2021.

TL;DR: It is suggested that compounds WA20 and WB07 are the first curcumin analogue-based LSD1 inhibitor with remarkable A549 suppressive activity, providing a novel scaffold for the development of LSD1 inhibitors.

TL;DR: A molecular modeling study on a set of 43 thieno[3,2-b]pyrrole competitive inhibitors of LSD1 using three-dimensional quantitative structure-activity relationship (3D-QSAR), molecular docking and molecular dynamics simulations indicated the good predictive power and statistical reliability of this model.