78 results about "Methyltransferase inhibitor" patented technology

There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.

The present invention relates to a pharmaceutical composition for treating a neoplasm, a preneoplasm, a proliferative disorder and / or a precancerous lesion, the use of such compositions for the treatment of the listed conditions, and methods of treating the listed conditions. The composition of the present invention comprises an inhibitor of eIF4E, a methltransferase inhibitor, and a pharmaceutically acceptable carrier.

Methods and compositions are provided for treating myelodysplastic syndrome and acute myeloid leukemia, wherein the composition comprises at least one compound according to Formula I:wherein R1 is selected from the group consisting of —NH2, —NH—CH2—CO2H, —NH—CH(CH3)—CO2H, and —NH—C(CH3)2—CO2H, or a pharmaceutically acceptable salt of such a compound; and a DNA methyltransferase inhibitor, or a pharmaceutically acceptable salt thereof.

Provided herein, in part, is a method of treating a neurological or movement disorder in a patient in need thereof, comprising subcutaneously administering to said patient a pharmaceutically acceptable composition comprising levodopa and optionally carbidopa and optionally entacapone or tolcapone, or pharmaceutically acceptable salts thereof, wherein said composition is administered substantially continuously, and compositions that can be used in the disclosed methods.

Provided herein, in part, is a method of treating a neurological or movement disorder in a patient in need thereof, comprising subcutaneously administering to said patient a pharmaceutically acceptable composition comprising levodopa and optionally carbidopa and optionally entacapone or tolcapone, or pharmaceutically acceptable salts thereof, wherein said composition is administered substantially continuously, and compositions that can be used in the disclosed methods.

The invention relates to a method for detecting DAN methyltransferase activity based on strand displacement amplification and DNAzyme amplification. A three-function double-stranded DNA probe is designed. Methylation happening to the three-function double-stranded DNA probe is specifically recognized through DAN methyltransferase. Remaining non-methylated double-stranded DNA is specifically cut through HpaII restriction enzymes, methylated double-stranded DNA triggers a strand displacement reaction, a large amount of 8-17 DNAzyme is released, the 8-17 DNAzyme catalyzes cutting of a large number of hairpin-line molecular beacon substrates, and remarkable fluorescent enhancement is triggered. The method can sensitively detect the DAN methyltransferase activity, and the detection limit is 0.0082 U / mL. The method has potential application in research of influences of anti-cancer drugs on DAN methyltransferase activity inhibition and screening of DAN methyltransferase inhibitors.

The invention discloses an umbilical cord blood Treg cell in-vitro amplification method based on trophoblastic cells and application. The specific technical method comprises the steps that firstly, umbilical cord Wharton's jelly mesenchymal stem cells are adopted as the trophoblastic cells to induce preliminary proliferation of Treg cells in umbilical cord blood mononuclear cells; then, pure Tregcells are obtained through magnetic bead sorting; and finally, the Treg cells are stimulated to be rapidly amplified by using optimized amplification factors. According to the amplification method, human AB plasma, IL-2, rapamycin, an RARA agonist and a DNA methyltransferase inhibitor are used as the optimized amplification factors, and a large number of umbilical cord blood Treg cells with high purity and high activity can be prepared within two weeks. Umbilical cord blood is used as a raw material for Treg cell amplification, batch preparation can be achieved, and Treg cell quality fluctuation caused by individual differences of samples can be reduced. The umbilical cord blood Treg cells have low immunogenicity and can be used as universal cells for clinical research, such as autoimmunediseases, graft-versus-host diseases and the like.

Methods and compositions are provided for treating myelodysplastic syndrome and acute myeloid leukemia, wherein the composition comprises at least one compound according to Formula I:wherein R1 is selected from the group consisting of —NH2, —NH—CH2—CO2H, —NH—CH(CH3)—CO2H, and —NH—C(CH3)2—CO2H, or a pharmaceutically acceptable salt of such a compound; and a DNA methyltransferase inhibitor, or a pharmaceutically acceptable salt thereof.

Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a cyclin-dependent kinase inhibitor and a DNA methyltransferase inhibitor to a mammal in need thereof.

The invention discloses a long-chain non-coding RNA marker for assisting diagnosis of esophageal squamous cell carcinoma (ESCC). The long-chain non-coding RNA is LINC01419, the expression amount of the long-chain non-coding RNA is detected and can be used for auxiliary diagnosis or prediction of the esophageal squamous cell carcinoma, and the methylation status of a GSTP1 gene is monitored to predict the sensitivity of the esophageal squamous cell carcinoma to 5-FU chemotherapy. The expression level of a LINC01419 gene can be detected by an RT-PCR, real-time quantitative PCR, immunoassay, in situ hybridization, a chip or a high-throughput sequencing platform. The invention further discloses application of a methyltransferase inhibitor 5-Aza-CdR to regulate the expression of the long-chainnon-coding RNA LINC01419 and response to the 5-FU, and application of an inhibitor medicine including the long-chain non-coding RNA LINC01419 in treatment of the esophageal squamous cell carcinoma. The molecular marker of the esophageal squamous cell carcinoma is provided, a theoretical basis for mechanism research and clinical individualized treatment of the esophageal squamous cell carcinoma isprovided, and by monitoring the overexpression of the LINC01419 in the ESCC, a new treatment strategy for the clinical treatment of the ESCC can be provided.

The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

A first aspect of the invention relates to a combination comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to 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.

Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a cyclin-dependent kinase inhibitor and a DNA methyltransferase inhibitor to a mammal in need thereof.

The invention provides an SET8 lysine methyltransferase inhibitor as well as a preparation method and application thereof. The inhibitor has a structural formula shown in the description. The inhibitor provided by the invention has a remarkable inhibition function on SET8 lysine methyltransferase, and in addition, has a remarkable inhibition effect on proliferation of tumor cells.