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METHOD OF ASSAYING COMPOUNDS WHICH AFFECT THE ACTIVITY OF G PROTEIN-COUPLED RECEPTORS BASED ON MEASUREMENT OF RECEPTOR OLIGOMERIZATION

机译:基于受体寡聚化测量影响G蛋白偶联受体活性的化合物的方法

摘要

This invention is a new method of assaying compounds that modulate the activity of G protein-coupled receptors based on measurement of changes in the relative proportions of monomeric to multimeric receptor polypeptides. More specifically, techniques are described herein which permit the prediction of the pharmacological efficacy of drug candidates based solely on the ability of the candidate compounds to alter the ratio of receptor monomer to homo-oligomeric forms of the receptor. This method provides a novel means of assaying compounds as potential therapeutic drugs at G protein-coupled receptors which is greatly simplified and more generally applicable than existing methods.
机译:本发明是基于测量单体对多聚体受体多肽的相对比例变化来测定调节G蛋白偶联受体活性的化合物的新方法。更具体地,本文描述了仅基于候选化合物改变受体的单体与同型寡聚体之比的能力来预测候选药物的药理功效的技术。该方法提供了一种在G蛋白偶联受体处测定化合物作为潜在治疗药物的新方法,与现有方法相比,该方法大大简化并且更普遍适用。

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