Grillo-Bosch Dolors, Choquet Daniel, Sainlos Matthieu
Drug Discov Today Technol. 2013 Dec;10(4):e531-40. doi: 10.1016/j.ddtec.2012.10.003.
Modulating protein-protein interactions constitutes a promising strategy both for the investigation of biological mechanisms and for developing new therapeutic approaches. Among the many types of inter-actions, PDZ domain-mediated interactions (PDMIs) have emerged over the last decade as attractive targets in the drug discovery field. Indeed, these small domains are involved in the regulation of many signaling pathways and possess structural properties which are favorable for the design of competing ligands. Herein, we describe the recent approaches developed to inhibit this class of protein-protein interactions.
调节蛋白质-蛋白质相互作用对于研究生物学机制和开发新的治疗方法而言都是一种很有前景的策略。在众多类型的相互作用中，PDZ结构域介导的相互作用（PDMIs）在过去十年中已成为药物发现领域颇具吸引力的靶点。事实上，这些小结构域参与了许多信号通路的调节，并且具有有利于设计竞争性配体的结构特性。在此，我们描述了为抑制这类蛋白质-蛋白质相互作用而开发的最新方法。
