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Small molecule kinase inhibitors as anti-cancer therapeutics

O Chahrour1, D Cairns, Z Omran

  • 1School of Pharmacy, University of Damascus, Damascus, Syria.

Mini Reviews in Medicinal Chemistry
|February 7, 2012
PubMed

Insights

Protein kinase inhibitors are crucial in cancer drug discovery. This review classifies inhibitors by binding site and mechanism, exploring their impact on selectivity and resistance, with a focus on clinical trials.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Protein kinases are key regulators of cellular processes and significant targets in cancer drug discovery.
  • Several kinase inhibitors are FDA-approved, with ongoing research to develop new therapies.
  • Understanding inhibitor mechanisms is vital for improving cancer treatment efficacy.

Purpose of the Study:

  • To review and classify protein kinase inhibitors based on their mechanisms of action and binding sites.
  • To explore the relationship between inhibitor mechanisms, target selectivity, and drug resistance.
  • To highlight kinase inhibitors currently undergoing clinical trials for cancer treatment.

Main Methods:

  • Literature review and classification of kinase inhibitors.
  • Analysis of different inhibitor mechanisms: ATP-competitive, allosteric, substrate-competitive, and covalent inhibitors.
  • Examination of clinical trial data for kinase inhibitors.

Main Results:

  • Kinase inhibitors can act through various mechanisms, including ATP-competitive and allosteric inhibition.
  • Inhibitor classification aids in understanding target selectivity and resistance patterns.
  • A significant number of kinase inhibitors are in various phases of clinical trials.

Conclusions:

  • The mechanism of action is critical for kinase inhibitor efficacy, selectivity, and overcoming resistance.
  • Further research into diverse inhibitor classes and their clinical applications is warranted.
  • Targeting protein kinases remains a promising strategy in oncology drug development.

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