72 results about "Histone methyltransferase" patented technology

Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

The invention relates to determining the presence of an EZH2 gene mutation in a sample from a subject and inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono-through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

The invention provides application of tetraphenyl ethylene derivatives in detecting activity of transmethylase, belonging to the technical field of biology. The detection method comprises the following steps: preparing quenching-molecule-modified double-chain nucleic acid; reacting the quenching-molecule-modified double-chain nucleic acid with S-adenosylmethionine, different concentrations of transmethylase and an enzyme reaction buffer solution to obtain a mixed solution; and finally, reacting the obtained mixed solution with a tetraphenyl ethylene derivative water solution, and detecting the activity of the transmethylase. The invention also provides application of the tetraphenyl ethylene derivatives in detecting the concentration of the transmethylase inhibitor. The detection method is simple and quick, and has high sensitivity.

The invention relates to the technical field of medical treatment. Theanine is a characteristic amino acid of tea, can be used for inhibiting cell growth and invasion of human pancreatic cancer, cervical cancer, gastric cancer, breast cancer and other cancers as well as remarkably inhibiting growth of tumors in a body, and has an inhibition effect superior to anti-cancer medicines such as cyclophosphamide. The action mechanism relates to down-regulation of receptors closely related to inhibition of tumor growth, invasion and transfer, signal transduction regulated protein, kinase level and combination of nuclear factors and DNA, as well as upper regulation of factors such as cancer-inhibiting protein and cell cycle inhibition protein; and the theanine can be used for directly inhibiting the activity of histone deacetylase and histone methyltransferase EZH2 and combination of inflammatory factor NF-kappa B and DNA. Furthermore, the theanine can be synergized with 6-fluoro-4-hydroxycoumarin (X) to improve inhibition on tumor cell growth and invasion by times, and has the activity superior to that of cyclophosphamide and the like. The theanine and synthesis with X can be applied to prevention and treatment of tumors, inflammations, cardiovascular diseases, immunodeficiency and other diseases.