Gao Meng, Cheng Kui, Yin Hang
Department of Chemistry, Center of Basic Molecular Science, Tsinghua University, Beijing, China , 100082.
Department of Chemistry and Biochemistry, the BioFrontiers Institute, University of Colorado Boulder, Boulder, CO, 80309-0596.
Biopolymers. 2015 Jul;104(4):310-6. doi: 10.1002/bip.22625.
Protein-protein interactions (PPIs) are critical in numerous biological processes including signaling transduction, function regulations, and disease development. To regulate PPIs has been thought to be challenging due to their highly dynamic and expansive interfacial areas. Nonetheless, successful examples have been reported of targeting PPIs using small molecules, peptides, and proteins. Peptides, especially macrocyclic peptides have proven to be a particularly useful tool to inhibit PPIs for their exquisite potency, stability and selectivity. Herein we review the recent developments of this area of research, focusing on the macrocyclic peptides isolated from natural products, identified from library screening, and rationally designed based on structures, as PPI regulators.
蛋白质-蛋白质相互作用（PPIs）在众多生物过程中至关重要，包括信号转导、功能调控和疾病发展。由于蛋白质-蛋白质相互作用具有高度动态和广阔的界面区域，因此调控它们一直被认为具有挑战性。尽管如此，已有报道称使用小分子、肽和蛋白质靶向蛋白质-蛋白质相互作用取得了成功。肽，尤其是大环肽，因其卓越的效力、稳定性和选择性，已被证明是抑制蛋白质-蛋白质相互作用的一种特别有用的工具。在此，我们综述该研究领域的最新进展，重点关注从天然产物中分离、通过文库筛选鉴定以及基于结构合理设计的大环肽作为蛋白质-蛋白质相互作用调节剂的情况。
