Methods and compositions for characterization of HSD1 inhibitors
    4.
    发明申请
    Methods and compositions for characterization of HSD1 inhibitors 审中-公开
    表征HSD1抑制剂的方法和组成

    公开(公告)号:US20100292085A1

    公开(公告)日:2010-11-18

    申请号:US12584317

    申请日:2009-09-03

    IPC分类号: C40B30/00 C12Q1/68 G01N33/574

    摘要: One aspect of the present invention relates to methods of identifying cortisone response signature gene sets and methods of using the identified gene sets to identify compounds that modulate HSD1 activity. In some embodiments, methods are provided to use cortisone response gene sets to estimate the HSD1 activity. Another aspect of the present inventive relates to methods for identification of off-target signature gene sets that can be used to estimate HSD1 compound induced off-target activity and methods for classification of compounds that modulate HSD1 activity. Another aspect of the present invention relates to cell lines that over-expresses HSD1 and methods of use thereof. Additional embodiments of the of the invention are described in the specification provided herein. The contents of this ABSTRACT are not intended to in anyway limit the scope of the invention claimed herein.

    摘要翻译: 本发明的一个方面涉及鉴定可的松反应特征基因组的方法以及使用鉴定的基因组鉴定调节HSD1活性的化合物的方法。 在一些实施方案中,提供了使用可的松反应基因组估计HSD1活性的方法。 本发明的另一方面涉及用于鉴定可用于估计HSD1化合物诱导的脱靶活性的离靶标签基因组的方法以及调节HSD1活性的化合物的分类方法。 本发明的另一方面涉及过表达HSD1的细胞系及其使用方法。 在本文提供的说明书中描述了本发明的另外的实施例。 本摘要的内容并不旨在限制本文所要求保护的发明的范围。

    Methods for determining whether a chemical agent modulates enzymatic activity of an L-2-hydroxy acid oxidase
    5.
    发明授权
    Methods for determining whether a chemical agent modulates enzymatic activity of an L-2-hydroxy acid oxidase 失效
    用于确定化学试剂是否调节L-2-羟基酸氧化酶的酶活性的方法

    公开(公告)号:US07727740B1

    公开(公告)日:2010-06-01

    申请号:US11490840

    申请日:2006-07-21

    IPC分类号: C12Q1/26 A61K49/00

    摘要: The present invention provides methods for screening for one or more chemical agents that modulate the enzymatic activity of an L-2-hydroxy acid oxidase. The methods comprise the steps of (a) contacting an L-2-hydroxy acid oxidase, in a solution in vitro, with one or more chemical agents in the presence of a substrate that is capable of being oxidized by the L-2-hydroxy acid oxidase; (b) measuring the enzymatic activity of the L-2-hydroxy acid oxidase in the presence of the chemical agent to identify one or more candidate chemical agents that modulate L-2-hydroxy acid oxidase activity in vitro; and (c) administering the one or more identified candidate chemical agents to a test animal and measuring one or more physiological parameters.

    摘要翻译: 本发明提供了筛选调节L-2-羟基酸氧化酶的酶活性的一种或多种化学试剂的方法。 所述方法包括以下步骤:(a)将体外溶液中的L-2-羟基酸氧化酶与一种或多种化学试剂在基质存在下接触,所述底物能够被L-2-羟基 酸性氧化酶; (b)在化学试剂存在下测定L-2-羟基酸氧化酶的酶活性,以鉴定一种或多种在体外调节L-2-羟基酸氧化酶活性的候选化学试剂; 和(c)将一种或多种鉴定的候选化学试剂施用于测试动物并测量一种或多种生理参数。