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Updated: Aug 12, 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

Recent advances and new directions in the discovery and development of cyclin-dependent kinase inhibitors

P M Fischer1

  • 1Cyclacel Ltd., James Lindsay Place, Dundee, DD1 5JJ, Scotland, UK. pfischer@cyclacel.com

Current Opinion in Drug Discovery & Development
|June 27, 2003
PubMed

Insights

Cyclin-dependent kinases (CDKs) regulate cell division. Inhibiting CDKs halts cancer cell proliferation, offering a therapeutic strategy. This review covers CDK inhibitor development and applications beyond oncology.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Oncology

Background:

  • The eukaryotic cell cycle is controlled by cyclin-dependent kinases (CDKs) and cyclins.
  • Dysregulation of CDKs and cyclins is a hallmark of cancer, leading to uncontrolled cell proliferation.
  • Targeting CDK activity is a key strategy for developing mechanism-based anticancer therapeutics.

Purpose of the Study:

  • To critically review advances in the development of cyclin-dependent kinase (CDK) inhibitors.
  • To discuss alternative approaches to CDK inhibition.
  • To explore therapeutic applications of CDK inhibitors beyond oncology.

Main Methods:

  • Review of recent scientific literature on CDK inhibitors.
  • Critical analysis of medicinal chemistry endeavors in selective kinase inhibition.
  • Discussion of therapeutic strategies targeting cell cycle regulation.

Main Results:

  • Significant progress has been made in developing inhibitors selective for the ATP binding sites of CDKs.
  • Various alternative strategies for CDK inhibition are being explored.
  • CDK inhibitors show potential therapeutic applications in non-oncology fields.

Conclusions:

  • Inhibiting CDK enzymatic activity is a promising strategy to halt malignant cellular proliferation.
  • Medicinal chemistry is advancing the development of selective CDK inhibitors.
  • The therapeutic potential of CDK inhibitors extends to diseases beyond cancer.

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