Mori Mattia, Vignaroli Giulia, Botta Maurizio
Drug Discov Today Technol. 2013 Dec;10(4):e541-7. doi: 10.1016/j.ddtec.2012.10.001.
14-3-3 is a family of highly conserved regulatory proteins which is attracting a significant interest due to its potential role as target for pharmacological intervention against cancer and neurodegenerative disorders. Although modulating protein-protein interactions (PPI) is still conceived as a challenging task in drug discovery, in past few years peptide inhibitors and small molecular modulators of 14-3-3 PPI have been described. Here we examine structural and biological features of 14-3-3 and propose an overview on techniques used for discovering small molecular inhibitors and stabilizers of 14-3-3 PPI.
14-3-3是一类高度保守的调节蛋白家族，由于其作为抗癌和神经退行性疾病药物干预靶点的潜在作用而备受关注。尽管在药物发现中调节蛋白质-蛋白质相互作用（PPI）仍然被认为是一项具有挑战性的任务，但在过去几年中，已经报道了14-3-3 PPI的肽抑制剂和小分子调节剂。在这里，我们研究了14-3-3的结构和生物学特性，并概述了用于发现14-3-3 PPI小分子抑制剂和稳定剂的技术。
