title: Targeting protein-protein interfaces using macrocyclic peptides.
abstract: 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.
authors: Department of Chemistry, Center of Basic Molecular Science, Tsinghua University, Beijing, China , 100082.
authors: Meng
authors: M
authors: Gao
authors: Department of Chemistry, Center of Basic Molecular Science, Tsinghua University, Beijing, China , 100082.
authors: Kui
authors: K
authors: Cheng
authors: 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.
authors: Hang
authors: H
authors: Yin
mesh_terms: D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D047028:Macrocyclic Compounds / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry*
chemical_list: D047028:Macrocyclic Compounds; D010455:Peptides
keywords: inhibitor; macrocyclic peptide; protein−protein interface; rational design