HORMONALLY UP-REGULATED, NEU-TUMOR-ASSOCIATED KINASE
    92.
    发明申请
    HORMONALLY UP-REGULATED, NEU-TUMOR-ASSOCIATED KINASE 有权
    异常上调,与肿瘤相关的激素

    公开(公告)号:US20050186668A1

    公开(公告)日:2005-08-25

    申请号:US10032256

    申请日:2001-12-21

    摘要: This invention relates generally to a novel serine/threonine protein kinase, specifically to hormonally up-regulated, neu-tumor-associated kinase (HUNK); and to the nucleotide sequence encoding it. The kinase is temporally expressed during postnatal mammary development in a spatially heterogeneous manner in certain subsets of cells, and overexpressed in a subset of primary breast cancers. The invention further relates to an analysis of a correlation between carcinogenesis and postnatal development, particularly mammary development, especially associated with parity; to methods of using the kinase, or gene encoding it, as markers, prognostic tools, screening tools and therapies, in vitro and in vivo, that are based upon that correlation; and to the regulation of pregnancy-induced changes in the mammary tissue that occur in response to estrogen and progesterone.

    摘要翻译: 本发明一般涉及一种新的丝氨酸/苏氨酸蛋白激酶,特别是激素上调的神经肿瘤相关激酶(HUNK); 和编码它的核苷酸序列。 该激酶在产后乳腺发育中在某些细胞亚群中以空间异质的方式在时间上表达,并且在原发性乳腺癌的一个子集中过表达。 本发明还涉及癌发生与产后发育之间的相关性的分析,特别是与平等相关的乳腺发育; 使用基于该相关性的在体外和体内使用激酶或编码它的基因作为标记物,预后工具,筛选工具和疗法的方法; 以及针对雌激素和孕激素反应发生的怀孕引起的乳腺组织变化的调节。

    Methods and compositions for derepression of IAP-inhibited caspase
    93.
    发明申请
    Methods and compositions for derepression of IAP-inhibited caspase 审中-公开
    用于抑制IAP抑制半胱天冬酶的方法和组合物

    公开(公告)号:US20050159359A1

    公开(公告)日:2005-07-21

    申请号:US11021517

    申请日:2004-12-23

    摘要: The invention provides isolated agents having a core peptide selected from the group consisting of Core peptides 5 through 39 and 42 through 55, wherein the agent derepresses an IAP-inhibited caspase. Also provided is an isolated agent having a core structure selected from any of the structures shown in FIGS. 5, 9, 10, 14B, and 21-24 wherein said agent derepresses an IAP-inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The method consists of contacting an IAP-inhibited caspase with an effective amount of an agent to derepress an IAP-inhibited caspase, the agent having a core motif selected from the group consisting of a core peptide having a sequence set forth in any of Core peptides 4 through 39 and 42 through 55, and a core structure selected from the group consisting of TPI759, TPI882, TPI914 or TPI927. The methods of the invention also can be used for promoting apoptosis in a cell and for reducing the severity of a pathology characterized by reduced levels of apoptosis. Methods for identifying agents that derepress an IAP-inhibited caspase are also provided.

    摘要翻译: 本发明提供了具有选自核心肽5至39和42至55的核心肽的分离的试剂,其中所述试剂减阻IAP抑制的半胱天冬酶。 还提供了一种隔离剂,其具有选自图1和图2所示的任何结构的芯结构。 5,9,10,14B和21-24,其中所述药物抑制IAP抑制的半胱天冬酶。 本发明还提供了一种去抑制IAP抑制的半胱天冬酶的方法。 该方法包括使IAP抑制的半胱天冬酶与有效量的试剂接触以对抑制IAP-抑制的半胱天冬酶进行脱保护,该试剂具有选自核心肽的核心基序,所述核心基序具有核心肽 4至39和42至55,以及选自TPI759,TPI882,TPI914或TPI927的核心结构。 本发明的方法还可用于促进细胞凋亡和降低以凋亡水平降低为特征的病理学的严重性。 还提供了用于鉴定抑制IAP抑制的半胱天冬酶的药剂的方法。