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Small-molecule modulators of 14-3-3 protein-protein interactions

机译:14-3-3蛋白质-蛋白质相互作用的小分子调节剂

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14-3-3 Proteins are eukaryotic adapter proteins that regulate a plethora of physiological processes by binding to several hundred partner proteins. They play a role in biological activities as diverse as signal transduction, cell cycle regulation, apoptosis, host-pathogen interactions and metabolic control. As such, 14-3-3s are implicated in disease areas like cancer, neurodegeneration, diabetes, pulmonary disease, and obesity. Targeted modulation of 14-3-3 protein-protein interactions (PPIs) by small molecules is therefore an attractive concept for disease intervention. In recent years a number of examples of inhibitors and stabilizers of 14-3-3 PPIs have been reported promising a vivid future in chemical biology and drug development for this remarkable class of proteins.
机译:14-3-3蛋白是真核衔接蛋白,通过结合数百种伴侣蛋白来调节过多的生理过程。它们在生物活动中起着重要作用,例如信号转导,细胞周期调节,凋亡,宿主-病原体相互作用和代谢控制。因此,14-3-3与癌症,神经变性,糖尿病,肺部疾病和肥胖症等疾病领域有关。因此,小分子对14-3-3蛋白质-蛋白质相互作用(PPI)的靶向调节是一种有吸引力的疾病干预概念。近年来,已经报道了许多14-3-3 PPI抑制剂和稳定剂的例子,这些蛋白质对于化学生物学和药物开发的前景广阔。

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