5 results about "Transferase inhibitor" patented technology

This invention discloses a high-throughput screening method for monkeypox virus (MPXV) N7-methyltransferase (N7-MTase) inhibitors based on fluorescence polarization technology and its application. This method uses MPXV E1... CTD Using the / E12 protein complex as a target, and leveraging the specific binding characteristic of the fluorescent probe FL-NAH to the target catalytic center, small molecule inhibitors that competitively bind to the SAM binding site are screened by monitoring changes in fluorescence polarization signals. This invention yielded a series of candidate compounds with significant inhibitory activity. Experiments demonstrated that these inhibitors exhibit strong inhibitory effects on MPXV N7-MTase, with a biochemical IC50 level of [missing information]. 50 Preferably, the concentration can reach 4.65 μM; at the cellular level, the compound exhibits a clear attenuation effect against poxviruses, with an EC50 value of [missing value]. 50 The range is up to 46.75 μM, and it has low cytotoxicity (CC). 50 >200 μM).

The present invention relates to an amide derivative compound, which exhibits the activity of a diacylglycerol acyltransferase (DGAT) 2 inhibitor and is represented by chemical formula (1), a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

This invention discloses an NK cell-like inducer and its application. The NK cell-like inducer comprises a DNA methyltransferase inhibitor, a histone deacetase inhibitor, a histone methyltransferase inhibitor, and vitamin C or a derivative thereof; the final concentration of the DNA methyltransferase inhibitor is 0.05~0.45 μM; the final concentration of the histone deacetase inhibitor is 0.05~1 μM; and the final concentration of vitamin C or a derivative thereof is 1~1000 μM. The inducer combination of this invention can activate the synthesis of intracellular cryoprotective substances such as glutathione, effectively reducing cell damage during cryopreservation, and increasing the survival rate of NK cell-like cells after 7 days of liquid nitrogen cryopreservation to over 90%, thus achieving long-term storage of NK cell-like cells.

A metal complex comprising: (a) a pharmaceutically acceptable central metal; (b) a DNA methyltransferase (DNMT) inhibitor; and (c) 2,5-dihydroxyterephthalic acid (DTA) and / or syringic acid (SA).

The present invention relates to a method of treating RAS-dependent cancer in a subject by use of a farnesyltransferase inhibitor. Also described are compositions comprising a farnesyltransferase inhibitor; and an agent that increases the amount of geranylgeranyl pyrophosphate (GGPP). Lastly, the use of farnesyltransferase inhibitor for transdifferentiating a cell into a fibroblast-like stage is described herein.