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Protein kinases as drug targets in cancer

Mehmet Alper Arslan1, Ozgur Kutuk, Huveyda Basaga

  • 1Biological Sciences and Bioengineering Program, Sabanci University, Orhanli-Tuzla 34956, Istanbul, Turkey.

Current Cancer Drug Targets
|November 15, 2006
PubMed

Insights

Targeted cancer therapies, including small molecule inhibitors and monoclonal antibodies, block cancer progression by inhibiting key protein kinases like mTOR and EGFR. This review details their mechanisms and discusses drug resistance.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Protein kinases are crucial in cancer signaling pathways.
  • Targeted therapies offer specific blockade of cancer progression.
  • Understanding kinase inhibitors is vital for effective cancer treatment.

Purpose of the Study:

  • To review targeted therapies focusing on protein kinase inhibitors.
  • To provide a technology-based perspective on ATP- and non-ATP-competitive inhibitors.
  • To discuss inhibitors of specific kinases (mTOR, BCR-ABL, MEK, etc.) and Hsp90.

Main Methods:

  • Literature review of structural, molecular, and clinical studies.
  • Analysis of small molecule inhibitors and monoclonal antibodies.
  • Examination of inhibitors targeting specific protein kinases and Hsp90.

Main Results:

  • Detailed molecular mechanisms of action for various kinase inhibitors.
  • Discussion on the emergence of drug resistance to targeted therapies.
  • Inclusion of inhibitors for mTOR, BCR-ABL, MEK, p38 MAPK, EGFR, PDGFR, VEGFR, HER2, Raf, and Hsp90.

Conclusions:

  • Targeted protein kinase inhibitors represent a significant advancement in cancer therapy.
  • Understanding inhibitor mechanisms and resistance is key to optimizing treatment strategies.
  • Further research into novel inhibitors and resistance circumvention is warranted.

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