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High-throughput screening for modulators of protein-protein interactions: use of photonic crystal biosensors and complementary technologies

机译:高通量筛选蛋白质-蛋白质相互作用的调节剂:使用光子晶体生物传感器和互补技术

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摘要

High-throughput screening (HTS) has played an integral role in the development of small molecule modulators of biological processes. These screens are typically developed for enzymes (such as kinases or proteases) or extracellular receptors, two classes of targets with well-established colorimetric or fluorimetric activity assays. In contrast, methods for detection of protein-protein interactions lack the simplicity inherent to enzyme and receptor assays. Technologies that facilitate the discovery of small molecule modulators of protein-protein interactions are essential to the exploitation of this important class of drug targets. As described in this critical review, photonic crystal (PC) biosensors and other emerging technologies can now be utilized in high-throughput screens for the identification of compounds that disrupt or enhance protein-protein interactions (167 references).
机译:高通量筛选(HTS)在生物过程的小分子调节剂的开发中起着不可或缺的作用。这些筛选通常针对酶(例如激酶或蛋白酶)或细胞外受体(具有公认的比色或荧光活性测定法的两类目标)而开发。相反,用于检测蛋白质-蛋白质相互作用的方法缺乏酶和受体测定法固有的简单性。促进发现蛋白质-蛋白质相互作用的小分子调节剂的技术对于开发这一重要类别的药物靶标至关重要。如本重要评论中所述,光子晶体(PC)生物传感器和其他新兴技术现在可以用于高通量筛选中,以鉴定破坏或增强蛋白质-蛋白质相互作用的化合物(167参考文献)。

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