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Small molecule integrin antagonists in cancer therapy

Mayra Paolillo1, Marika A Russo, Massimo Serra

  • 1Dipartimento di Farmacologia Sperimentale ed Applicata, Università di Pavia, Italy. mayra.paolillo@unipv.it

Mini Reviews in Medicinal Chemistry
|November 26, 2009
PubMed

Insights

Small molecule antagonists targeting integrins, like alphavbeta3 and alphavbeta5, show promise in blocking tumor growth and metastasis. Cilengitide is a key cyclic peptidic antagonist in clinical trials for cancer therapy.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Oncology

Background:

  • Integrins are dimeric receptors mediating cell-ECM interactions, regulating crucial cellular processes.
  • Integrin activation is implicated in pathological conditions, including tumor growth and metastasis.
  • Understanding integrin structure is key to developing targeted therapies.

Purpose of the Study:

  • To review small molecule antagonists targeting alphavbeta3 and alphavbeta5 integrins for cancer therapy.
  • To highlight the therapeutic potential of blocking integrin-ECM interactions.
  • To discuss the role of integrin antagonists in combination therapies.

Main Methods:

  • Focus on small molecule antagonists, particularly for alphavbeta3 and alphavbeta5 integrins.
  • Review of recent advances in crystallographic structures of integrins.
  • Analysis of cilengitide as a cyclic peptidic antagonist in clinical trials.

Main Results:

  • Small molecule antagonists can block integrin binding to ECM proteins.
  • Inhibition of integrin biological effects can impede tumor growth and metastasis.
  • Cilengitide demonstrates potential as an anti-cancer therapeutic.

Conclusions:

  • Small molecule antagonists of alphavbeta3 and alphavbeta5 integrins are valuable tools for cancer therapy.
  • Combination therapies involving integrin antagonists may offer enhanced strategies against cancer.
  • Further research into integrin-targeted therapies holds significant promise for oncology.

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