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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
Summary
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.