METHOD FOR INHIBITING THE FORMATION OF SET1 FAMILY CORE COMPLEXES
    31.
    发明申请
    METHOD FOR INHIBITING THE FORMATION OF SET1 FAMILY CORE COMPLEXES 有权
    抑制SET1家族核心复合物形成的方法

    公开(公告)号:US20130203167A1

    公开(公告)日:2013-08-08

    申请号:US13415474

    申请日:2012-03-08

    CPC classification number: C12N9/99 C07K14/4702 C12Y201/01043

    Abstract: Disclosed in this specification is a method for inhibiting the formation of vertebrate SET1 family core complexes. A guanidinium-containing molecule is used to competitively inhibit the binding of the N-SET region of a SET1 protein to WDR5, thus inhibiting the formation of the SET1 family core complex. The guanidinium-containing molecule may be, for example, an arginine-containing peptide.

    Abstract translation: 在本说明书中公开的是抑制脊椎动物SET1家族核心复合物形成的方法。 使用含胍基分子竞争性地抑制SET1蛋白的N-SET区与WDR5的结合,从而抑制SET1家族核心复合物的形成。 含有胍基的分子可以是例如含精氨酸的肽。

    Methods of modulating SMYD3 for treatment of cancer
    32.
    发明授权
    Methods of modulating SMYD3 for treatment of cancer 有权
    调节SMYD3治疗癌症的方法

    公开(公告)号:US07968281B2

    公开(公告)日:2011-06-28

    申请号:US11912860

    申请日:2006-06-23

    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. N-terminal truncated forms of SMYD3 (alias ZNFN3A1) have higher methylating activity. Lys 824 is a preferred methylation site on the RB1 protein for SMYD3.

    Abstract translation: 本发明的特征在于确定多肽的甲基转移酶活性并筛选甲基转移酶活性的调节剂的方法,更特别是用于通过SMYD3进行视网膜母细胞瘤甲基化的调节剂。 本发明还提供了使用所鉴定的调节剂预防或治疗结肠直肠癌,肝细胞癌,膀胱癌和/或乳腺癌的方法或药物组合物。 SMYD3(别名ZNFN3A1)的N-末端截短形式具有较高的甲基化活性。 Lys 824是SMYD3的RB1蛋白上优选的甲基化位点。

    RECONSTITUTED HISTONE METHYLTRANSFERASE COMPLEX AND METHODS OF IDENTIFYI NG MODULATORS THEREOF
    33.
    发明申请
    RECONSTITUTED HISTONE METHYLTRANSFERASE COMPLEX AND METHODS OF IDENTIFYI NG MODULATORS THEREOF 审中-公开
    重组表达甲基转移酶复合物及其识别NG调节剂的方法

    公开(公告)号:US20090298105A1

    公开(公告)日:2009-12-03

    申请号:US12497211

    申请日:2009-07-02

    Applicant: Yi Zhang Ru Cao

    Inventor: Yi Zhang Ru Cao

    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 translation: 本发明提供了包含EED,EZH2和SUZ12的复原复合物,其中重构的复合物对组蛋白H3(H3-K27)的赖氨酸27具有组蛋白甲基转移酶(HMTase)活性。 重构的复合物还可以包括RbAp48,AEBP2或两者。 还公开了生产重建复合物的方法,鉴定抑制重构复合物的HTMase活性的化合物的方法和鉴定用于治疗癌症的候选化合物的方法。 还提供了试剂和试剂盒,包括重构的复合物。

Patent Agency Ranking