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Protein-protein Interfaces02:04

Protein-protein Interfaces

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 polypeptide...
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Interfacial Electrochemical Methods: Overview01:06

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Updated: May 26, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Interfacial inhibitors: targeting macromolecular complexes.

Yves Pommier1, Christophe Marchand

  • 1Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, US National Institutes of Health, Bethesda, Maryland 20892, USA. pommier@nih.gov

Nature Reviews. Drug Discovery
|December 17, 2011
PubMed
Summary
This summary is machine-generated.

Interfacial inhibitors target molecular machines in diseases like cancer and infections. This review explores five key examples and strategies for discovering new inhibitors.

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Microtensiometer for Confocal Microscopy Visualization of Dynamic Interfaces
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Last Updated: May 26, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Microtensiometer for Confocal Microscopy Visualization of Dynamic Interfaces
08:05

Microtensiometer for Confocal Microscopy Visualization of Dynamic Interfaces

Published on: September 9, 2022

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Interfacial inhibitors are natural products and synthetic drugs used in cancer, bacterial, and HIV treatments.
  • These drugs bind to interfaces during macromolecular machine assembly, arresting their function.
  • This arrest can trigger allosteric effects or desynchronize coordinated molecular machines.

Purpose of the Study:

  • To review archetypal examples of interfacial inhibitors.
  • To discuss similarities and differences between interfacial and allosteric inhibitors.
  • To provide a perspective on discovering novel interfacial inhibitors.

Main Methods:

  • Review of five archetypal interfacial inhibitors: camptothecins, etoposide, quinolone antibiotics, vinca alkaloids, and raltegravir.
  • Comparative analysis of interfacial and allosteric inhibitor mechanisms.
  • Discussion of discovery rationale and methodologies.

Main Results:

  • Interfacial inhibitors represent a significant class of therapeutic agents.
  • Understanding their mechanism of action provides insights into molecular machine regulation.
  • The review highlights key examples and their therapeutic applications.

Conclusions:

  • Interfacial inhibitors offer a unique therapeutic strategy by targeting molecular machine assembly.
  • Further research into their discovery and application holds promise for treating various diseases.
  • This class of inhibitors warrants continued investigation for novel drug development.