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Related Concept Videos

Protein-protein Interfaces02:04

Protein-protein Interfaces

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Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...
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Targeting protein-protein interfaces using macrocyclic peptides.

Meng Gao1, Kui Cheng1, Hang Yin1,2

  • 1Department of Chemistry, Center of Basic Molecular Science, Tsinghua University, Beijing, China , 100082.

Biopolymers
|February 10, 2015
PubMed
Summary
This summary is machine-generated.

Macrocyclic peptides are effective regulators of protein-protein interactions (PPIs), offering potent and selective inhibition. This review highlights recent advances in macrocyclic peptides for PPI regulation, sourced from nature, libraries, and rational design.

Keywords:
inhibitormacrocyclic peptideprotein−protein interfacerational design

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Area of Science:

  • Biochemistry and Molecular Biology
  • Drug Discovery and Development

Background:

  • Protein-protein interactions (PPIs) are fundamental to biological processes, including cell signaling and disease pathogenesis.
  • Regulating PPIs is challenging due to their dynamic nature and large interface areas.
  • Small molecules, peptides, and proteins have shown promise in targeting PPIs.

Purpose of the Study:

  • To review recent advancements in the development of macrocyclic peptides as regulators of protein-protein interactions (PPIs).
  • To focus on macrocyclic peptides derived from natural products, library screening, and structure-based rational design.

Main Methods:

  • Literature review of recent developments in macrocyclic peptide research for PPI regulation.
  • Categorization of macrocyclic peptides based on their origin: natural products, library screening, and rational design.

Main Results:

  • Macrocyclic peptides exhibit high potency, stability, and selectivity, making them valuable tools for inhibiting PPIs.
  • Diverse strategies, including isolation from natural sources, high-throughput screening, and structure-guided design, yield effective PPI-regulating macrocyclic peptides.

Conclusions:

  • Macrocyclic peptides represent a promising therapeutic strategy for modulating protein-protein interactions.
  • Continued research into natural products, library screening, and rational design will further advance the application of macrocyclic peptides in medicine.