Antiangiogenic drugs and tyrosine kinases

Research output: Contribution to journalArticle

25 Citations (Scopus)

Abstract

Various cancer types have different molecular and biological strategies for vascularization: neoangiogenesis, postnatal vasculogenesis, glomeruloid angiogenesis, intussusceptive microvascular growth, vessel cooption and vascular mimicry. The majority is still relatively obscure, which limits the development of more successful antivascular agents. It is not a surprise that, as our knowledge is deepest in case of tumor-induced neoangiogenesis, the first successful antiangiogenic drugs have been developed in this area. As neoangiogenesis involves growth factor receptors, most of them tyrosine kinases (KIT, Flt-3, VEGFRs, PDGFR, TIE2, FGFR1, EGFR and MET), several of these novel agents are tyrosine kinase inhibitors. This review summarizes our recent knowledge on various forms of cancer vascularization, the molecular mechanisms behind, depicting the "drugable" targets. In a short overview, we demonstrate the array of antiangiogenic approaches focusing on the tyrosine kinase inhibitors and summarize their preclinical activities. Finally we review the clinically available antiangiogenic tyrosine kinase inhibitors and demonstrate their current application and future perspectives. Further development in this field may depend on the identification of novel inhibitors targeting kinases that cannot be modulated yet by the available agents and on the development of vascularization strategy-specific design of these antivascular therapies.

Original languageEnglish
Pages (from-to)462-469
Number of pages8
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume8
Issue number5
DOIs
Publication statusPublished - Jun 2008

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Protein-Tyrosine Kinases
Pharmaceutical Preparations
Vascular Endothelial Growth Factor Receptor-3
Neoplasms
Growth Factor Receptors
Blood Vessels
Phosphotransferases
Growth
Therapeutics

Keywords

  • Antivascular therapy
  • Kinase inhibitors
  • Tumor vascularization
  • Tyrosine kinases

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Pharmacology

Cite this

Antiangiogenic drugs and tyrosine kinases. / Tímár, J.; Döme, B.

In: Anti-Cancer Agents in Medicinal Chemistry, Vol. 8, No. 5, 06.2008, p. 462-469.

Research output: Contribution to journalArticle

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