Cinviz Zeynep Nur, Moroni Elisabetta, Sensoy Ozge, Morra Giulia, Gurevich Vsevolod V
Graduate School of Engineering and Natural Sciences, Istanbul Medipol University, Istanbul 34810, Turkey.
Institute of Chemical Sciences and Technologies (SCITEC)- National Research Council (CNR), Via Mario Bianco 9, 20131 Milano, Italy.
Biomol Ther (Seoul). 2025 Sep 1;33(5):758-769. doi: 10.4062/biomolther.2025.079. Epub 2025 Aug 6.
Out of at least 20,000 human proteins fewer than 700 are targeted by drugs. Arrestins regulate G protein-coupled receptors, the largest family of signaling proteins in animals, as well as many receptor-independent signaling pathways. Humans express four arrestin subtypes, two of which are ubiquitous and were already shown to serve as versatile hubs of cellular signaling. So far, arrestin proteins are not directly targeted by any drugs. Here we describe potential targets on arrestins and/or interacting proteins, possible approaches for the development of targeting compounds, expected biological outcomes, and possible research and therapeutic value of targeting the interactions of arrestins with receptors and other signaling and trafficking proteins.
在至少20000种人类蛋白质中，只有不到700种是药物的作用靶点。抑制蛋白调节G蛋白偶联受体（动物中最大的信号蛋白家族）以及许多不依赖受体的信号通路。人类表达四种抑制蛋白亚型，其中两种普遍存在，并且已被证明是细胞信号传导的多功能枢纽。到目前为止，尚无任何药物直接作用于抑制蛋白。在此，我们描述了抑制蛋白和/或相互作用蛋白上的潜在靶点、开发靶向化合物的可能方法、预期的生物学结果，以及靶向抑制蛋白与受体以及其他信号和转运蛋白相互作用的可能研究和治疗价值。
