首页> 外国专利> SCREENING ASSAYS, MODULATORS AND MODULATION OF ACTIVATION OF RECEPTOR FOR ADVANCED GLYCATION END-PRODUCTS (RAGE)

SCREENING ASSAYS, MODULATORS AND MODULATION OF ACTIVATION OF RECEPTOR FOR ADVANCED GLYCATION END-PRODUCTS (RAGE)

机译:先进的糖化终产物(残渣)的筛查方法,调节剂和激活受体的调节剂

摘要

A method of screening candidate agents for their ability to modulate RAGE activity where such RAGE activity is induced by an active co-located GPCR, the method comprising the steps of: contacting a RAGE polypeptide with a GPCR polypeptide in the presence of a candidate agent where the GPCR polypeptide is constitutively active and/or is activated by addition of an agonist, partial agonist or allosteric modulator of that GPCR; and detecting whether the candidate agent is a modulator of RAGE ligand-independent activation of RAGE by activated co-located GPCR by detecting an effect indicative of modulation of RAGE activation by the presence of the candidate agent and/or by detecting RAGE-dependent signalling that is modulated by the presence of the candidate agent.
机译:一种筛选候选试剂调节RAGE活性的能力的方法,其中这种RAGE活性是通过活性共位GPCR诱导的,该方法包括以下步骤:在候选试剂存在下使RAGE多肽与GPCR多肽接触,其中GPCR多肽是组成性活性的和/或通过添加该GPCR的激动剂,部分激动剂或变构调节剂而被激活的;以及通过检测指示候选药物的存在指示RAGE激活的调节作用的作用和/或通过检测RAGE依赖的信号传导,通过激活的共位GPCR检测候选药物是否为RAGE配体非依赖性RAGE激活的调节剂。通过候选试剂的存在来调节。

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