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Published on: January 7, 2019

The alpha v integrin antagonists as novel anticancer agents: an update

Janet S Kerr1, Andrew M Slee, Shaker A Mousa

  • 1Enanta Pharmaceuticals Inc., 500 Arsenal Street, Watertown, MA 02472, USA.

Expert Opinion on Investigational Drugs
|November 30, 2002
PubMed

Insights

Integrins, like alpha(v)beta(3), are key in cancer growth and spread. Targeting alpha(v)beta(3) with small molecules shows promise for cancer therapies and diagnostics.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Integrins play crucial roles in cellular functions, including cancer progression.
  • The alpha(v)beta(3) integrin is implicated in solid tumors and metastases.
  • Its involvement in gene expression, proliferation, migration, survival, and angiogenesis makes it a therapeutic target.

Purpose of the Study:

  • To review the role of alpha(v)beta(3) integrin in cancer.
  • To discuss the rationale for developing alpha(v)beta(3) antagonists for cancer therapy and diagnostics.

Main Methods:

  • Literature review of published studies on alpha(v)beta(3) integrin in cancer.
  • Analysis of therapeutic candidates including antibodies, cyclic peptides, peptidomimetics, and small molecules.

Main Results:

  • Alpha(v)beta(3) integrin antagonists show potential in treating solid tumors and metastases.
  • These antagonists can inhibit tumor-associated angiogenesis.
  • Small-molecule antagonists are progressing in clinical trials for cancer treatment.

Conclusions:

  • Alpha(v)beta(3) integrin is a significant target for anti-cancer drug development.
  • Therapeutic and diagnostic strategies targeting alpha(v)beta(3) are advancing.
  • Small molecules offer a promising approach for cancer intervention.

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