Macrocyclic peptides as regulators of protein-protein interactions

作者：Jiang, Yang^*; Long, Hongyi; Zhu, Yujie; Zeng, Yi

来源：Chinese Chemical Letters, 2018, 29(7): 1067-1073.

DOI：10.1016/j.cclet.2018.05.028

• Macrocycle
• Macrocyclic peptide
• Protein-protein interaction
• Inhibitor
• Cell-penetrating peptide

Protein-protein interactions (PPIs) are recognized as attractive therapeutic targets. However targeting PPIs especially intracellular ones has been proven extremely difficult for conventional drug-like small molecules, and biological drugs such as monoclonal antibodies have difficulty in reaching intracellular targets. Macrocyclic peptides are promising candidates of PPI regulators for their potential in combining high potency and biological stability together. Cell permeability of macrocyclic peptides may also be achieved by structural modifications or conjugation to a cell-penetrating sequence. Significant progress has been made in this research area in recent years. Important technology progress and recent examples of macrocyclic peptide PPI modulators are reviewed.

• 出版日期2018-7
• 单位成都大学; 西华大学