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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

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You never know: Cdk inhibitors as anti-cancer drugs

Tim Hunt1

  • 1Cancer Research UK, Clare Hall Laboratories, South Mimms, UK. tim.hunt@cancer.org.uk

Cell Cycle (Georgetown, Tex.)
|December 11, 2008
PubMed

Insights

Researchers explored kinase inhibitors for cancer therapy, inspired by cyclin-dependent kinases (CDKs) role in cell division. While the rationale is debated, testing these CDK inhibitors on tumors remains a viable research avenue.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Cyclin-dependent kinases (CDKs) regulate cell cycle transitions, leading to their investigation as anti-cancer drug targets.
  • Roscovitine, a potent CDK inhibitor discovered by Laurent Meijer and colleagues, has entered clinical trials (CYC202/Seliciclib).

Discussion:

  • The precise definition of cancer as a "disease of the cell cycle" and the therapeutic window for inhibiting cell division remain subjects of debate.
  • Permanent cell division blockade in humans is generally lethal, raising questions about the safety and efficacy of anti-CDK drugs.

Key Insights:

  • Despite uncertainties, the development of specific protein kinase inhibitors is relatively straightforward.
  • Investigating the selective effects of CDK inhibitors on tumors is a pragmatic approach given the incomplete understanding of cell cycle control.

Outlook:

  • Further research is needed to clarify the role of cell cycle dysregulation in cancer and to determine the potential of CDK inhibitors in cancer therapy.
  • Clinical trial outcomes for roscovitine (CYC202/Seliciclib) will provide crucial data on the efficacy and safety of targeting CDKs in cancer treatment.

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