9 results about "Histone methyltransferase" patented technology

This invention belongs to the field of pharmaceutical technology, specifically relating to novel substituted benzoylpyridinone compounds and their applications. These novel substituted benzoylpyridinone compounds have the general structural formulas shown in (Ⅰ), (Ⅱ), (Ⅲ), (Ⅳ), (Ⅴ), (Ⅵ), (Ⅶ), (Ⅷ), or (Ⅸ), and as antitumor drugs, they exhibit significant EZH2 histone methyltransferase inhibitory activity. This invention provides methods for preparing these compounds, as well as pharmaceutical compositions containing them and their uses. The novel substituted benzoylpyridinone compounds obtained by this invention possess more significant antitumor activity and safety, and are of great value, particularly as antitumor agents, in EZH2, PRC2, and EZH2 / PRC2-mediated diseases.

This invention relates to methods for treating cancer, providing methods for treating solid tumors, B-cell lymphomas, or cancers with abnormal H3-K27 methylation, the method comprising orally administering a dosage form of EPZ-6438 in a therapeutically effective amount to a subject in need. This invention also relates to pharmaceutical compositions comprising one or more inhibitors of the human histone methyltransferase EZH2, and methods for treating cancer using such one or more EZH2 inhibitors.

The present invention relates to novel therapeutic compositions and methods for treating cancer. In particular, the use of proteinaceous inhibitors, including novel bicyclic peptide inhibitors, for use in treating cancer.

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.

This invention relates to a small molecule inhibitor of NSD2, its preparation method, and its applications. The NSD2 small molecule inhibitor is a compound with the structure shown in Formula (I) or a salt thereof: Formula (I). This NSD2 small molecule inhibitor exhibits high selectivity and potent efficacy against histone methyltransferase NDS2, and can be used to prepare drugs that inhibit NSD2, and drugs for the prevention and / or treatment of tumors or cancer.

The invention relates to the technical field of stem cell engineering and anti-aging biology, in particular to a histone modification regulation method based on placenta amnion sub-totipotent stem cells and an anti-aging preparation thereof. The regulation and control method comprises the following steps: separating and purifying healthy full-month caesarean section placenta amniotic membrane tissues, carrying out composite enzymolysis and flow cytometry screening to obtain CD105 < + >, CD73 < + > and CD45 <-> stem cells, and primarily culturing the CD105 < + >, CD73 < + > and CD45 <-> stem cells; the method comprises the following steps: determining histone methyltransferase MLL3 and demethylase JMJD3 as target spots through ChIP-seq, and determining H3K4me3 and H3K27me3 as target modification sites; an MLL3 activator CM-272 with the final concentration of 15 [mu] M and a JMJD3 inhibitor GSK-J4 with the final concentration of 10 [mu] M form a composite regulator, and induction culture is performed for 84 h under the conditions of 37 DEG C and 5% CO2; and carrying out Western Blot verification and screening on the stem cells meeting the standard. According to the anti-aging preparation, regulated stem cells are used as active ingredients, a sodium alginate-gelatin (2: 1) composite carrier, 5% mannitol and 1% human serum albumin protective agent are used as auxiliary materials, and the injection with the pH of 7.2-7.4 is prepared. The method is accurate in regulation and control, and the preparation is remarkable in anti-aging effect and low in immunological rejection risk.

The application provides an application of vascular endothelial cell histone methyltransferase Ezh2 in preparation of a medicine for preventing and treating sepsis-associated encephalopathy and model construction, relates to the field of biomedical technology, and has the primary purpose of providing a drug target for preventing and treating SAE, namely, EZH2 in vascular endothelial cells. The application also provides an endothelial cell specific Ezh2 gene conditional knockout mouse model, the model has a high sensitivity and a high stability of BBB damage phenotype, and can be used for SAE pathogenesis research and drug screening. The application further has the purpose of providing SAE treatment drugs, diagnostic markers and screening methods based on the new target and the new model. In the application, a mouse Ezh2 gene conditional knockout and an induced conditional knockout-CLP high-sensitivity SAE model are successfully constructed. The model not only overcomes the problem of systemic knockout lethality, but also has a BBB damage and neuroinflammation phenotype which is much more serious and stable than that of a traditional CLP model, thereby providing an irreplaceable tool for drug research and development.

The present invention provides a method for producing natural killer (NK) cells or precursor cells thereof from pluripotent stem cells, comprising a) a step of in vitro inducing hematopoietic progenitor cells (HPC) from pluripotent stem cells, b) a step of in vitro expanding HPC, and c) a step of in vitro inducing NK cells or precursor cells thereof from HPC and inhibiting histone methyltransferase and / or aromatic hydrocarbon receptors (AHR) in one or more of steps a) to c); and a method comprising (1) a step for forming pluripotent stem cell spheres having an average particle diameter of 200 [mu] m or more in a first culture medium, (2) a step for inducing the pluripotent stem cell spheres obtained in step (1) into a cell population containing HPC by three-dimensional culture using a second culture medium containing a histone methyltransferase inhibitor and / or an AHR antagonist, and (3) a step for inducing the pluripotent stem cell spheres obtained in step (2) into a cell population containing HPC. And (3) a step in which the cell population containing HPC obtained in step (2) is induced into a cell population containing NK cells or precursor cells thereof by three-dimensional culture using a third culture medium containing a histone methyltransferase inhibitor and / or an AHR antagonist, and one or more of steps (1) to (3) are performed by a perfusion culture method. Steps (1) to (3) are preferably performed by a continuous perfusion culture method.

The invention discloses application of a histone methyltransferase inhibitor BIX-01294 in preparation of a medicine for treating alveolar echinococcosis, and belongs to the field of biomedicine. The technical problem to be solved by the invention is how to treat and / or prevent alveolar echinococcosis. The invention finds that the BIX-01294 can be used for treating and / or preventing alveolar echinococcosis, has a remarkable killing effect on the protoscolex of echinococcus multilocularis and the vesicle stage in the continuous period in vitro, and can destroy tissue structures such as a head hook, a suction cup, microvillus and the like of the protoscolex so as to cause collapse of the vesicle in the continuous period. In addition, BIX-01294 treatment can inhibit the ability of echinococcus multilocularis protoscolex to develop towards cysts in a mouse secondary infection model body, and the infection rate and the liver transfer rate are both reduced. Therefore, the BIX-01294 can be used as the medicine for treating the alveolar echinococcosis.