Abstract:
The present invention features a method for determining the methyltransferase activity of a polypeptide and screening for modulators of methyltransferase activity, more particularly for modulators of the methylation of retinoblastoma by SMYD3. The invention further provides a method or pharmaceutical composition for prevention or treating of colorectal cancer, hepatocellular carcinoma, bladder cancer and/or breast cancer using a modulator so identified.
Abstract:
The present invention provides a reconstituted complex including EED, EZH2 and SUZ12 wherein the reconstituted complex has histone methyltransferase (HMTase) activity for lysine 27 of histone H3 (H3-K27). The reconstituted complex may further include RbAp48, AEBP2 or both. Also disclosed are methods of producing the reconstituted complex, methods of identifying compounds that inhibit the HTMase activity of the reconstituted complex and methods of identifying candidate compounds for treating cancer. Reagents and kits including the reconstituted complex are further provided.
Abstract:
The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
Abstract:
Objective methods for detecting or diagnosing cancer, or determining a predisposition for developing cancer, particularly lung cancer, cervical cancer, bladder cancer, esophageal cancer, osteosarcoma, prostate cancer and soft tissue tumor, are described herein. In one embodiment, the diagnostic method involves determining an expression level of the SUV39H2 gene. The present invention further provides methods of screening for candidate substances useful in the treatment and/or prevention of an SUV39H2-associated cancer, such as lung cancer, cervical cancer, bladder cancer, esophageal cancer, osteosarcoma, prostate cancer and soft tissue tumor. The present invention further provides methods of inhibiting the cell growth and thereby treating or alleviating symptoms of an SUV39H2 associated cancer. The present invention also features double-stranded molecules against the SUV39H2 gene and vectors encoding thereof as well as compositions containing such components and their utility in connection with the treatment and prevention of an SUV39H2-associated cancer.
Abstract:
The present invention relates to methods of suppressing the transcriptional expression of one or more genes by methylating the chromatin histone proteins of the one or more genes. Specifically, a viral SET domain histone lysine mehtyltransferase (vSET or vSET-like protein) methylates lysine 27 of a gene's histone protein 3 (H3- K27) thereby suppressing the transcription of the gene.
Abstract:
The invention features a method for inhibiting growth of a cancer cell by contacting the cell with a composition of a ZNFN3A1 siRNA. Methods of treating cancer are also within the invention. The invention also features products, including nucleic acid sequences and vectors as well as to compositions comprising them, useful in the provided methods. The invention also provides a method for inhibiting of tumer cell, for example liver or colon cancer cell, particularly HCC or colorectal adenocarcinoma.
Abstract:
This invention relates to long non-coding RNAs (IncRNAs), libraries of those ncRNAs that bind chromatin modifiers, such as Polycomb Repressive Complex 2, inhibitory nucleic acids and methods and compositions for targeting IncRNAs. d
Abstract:
A method for promoting the reprogramming of a non-cardiomyocytic cell or tissue into cardiomyocytic cell or tissue comprising is carried out by contacting a non-cardiomyocytic cell or tissue with a modulator of histone methyltransferase activity or expression.
Abstract:
The present invention relates to a pharmaceutical composition comprising a histone-lysine N-methyltransferase EZH2 (enhancer of zeste homolog 2) inhibitor and an enhancer of interferon-gamma receptor activity. The invention also relates to method of treating a patient having cancer, comprising administration of the pharmaceutical composition.