Crystal structure of a deacetylase and inhibitors thereof
    1.
    发明申请
    Crystal structure of a deacetylase and inhibitors thereof 审中-公开
    脱乙酰酶的晶体结构及其抑制剂

    公开(公告)号:US20070087427A1

    公开(公告)日:2007-04-19

    申请号:US11505214

    申请日:2006-08-16

    IPC分类号: C12N9/18 G06F19/00

    CPC分类号: C12N9/16

    摘要: The present invention provides three-dimensional structural information from the hyperthermophilic bacterium Aquifex aeolicus which is a histone deacetylase-like protein (HDLP). HDLP shares 35.2% amino acid sequence identity with human histone deacetylase (HDAC1). The present invention further provides three-dimensional structural information of HDLP bound by inhibitor molecules. The three-dimensional structural information of the present invention is useful to design, isolate and screen deacetylase inhibitor compounds capable of inhibiting HDLP, HDAC family members and HDLP-related molecules. The invention also relates to nucleic acids encoding a mutant HDLP which facilitates the determination of the three-dimensional structure of HDLP in the presence of a zinc atom.

    摘要翻译: 本发明提供来自作为组蛋白脱乙酰酶样蛋白质(HDLP)的超嗜热菌Aquifex aeolicus的三维结构信息。 HDLP与人组蛋白脱乙酰酶(HDAC1)具有35.2%的氨基酸序列同一性。 本发明还提供了由抑制剂分子结合的HDLP的三维结构信息。 本发明的三维结构信息可用于设计,分离和筛选能够抑制HDLP,HDAC家族成员和HDLP相关分子的脱乙酰酶抑制剂化合物。 本发明还涉及编码突变型HDLP的核酸,其有助于在锌原子存在下测定HDLP的三维结构。