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Integrin alpha v beta 3 antagonists for anti-angiogenic cancer treatment

Andrew R Hsu1, Anand Veeravagu, Weibo Cai

  • 1Department of Neurosurgery, Stanford University School of Medicine, Stanford, CA 94305, USA.

Recent Patents on Anti-Cancer Drug Discovery
|January 29, 2008
PubMed

Insights

Cell adhesion molecules like integrin alpha(v)beta(3) are key targets for novel anti-cancer therapies. This review examines patents for alpha(v)beta(3) antagonists, highlighting their potential in treating cancer by inhibiting tumor growth and angiogenesis.

Area of Science:

  • Molecular Biology
  • Oncology
  • Biochemistry

Background:

  • Cell adhesion molecules (CAMs) mediate essential physiological processes by facilitating direct contact between cells and the extracellular matrix (ECM).
  • Integrin signaling is critically involved in tumor progression, including angiogenesis and metastasis.
  • Integrin alpha(v)beta(3) is a specific CAM recognized for its role in cancer development.

Purpose of the Study:

  • To review and analyze patents detailing alpha(v)beta(3) antagonists for cancer treatment.
  • To highlight the therapeutic potential of targeting integrin alpha(v)beta(3) in oncology.
  • To differentiate various classes of alpha(v)beta(3) antagonists based on patent literature.

Main Methods:

  • Review of patent literature concerning alpha(v)beta(3) antagonists.
  • Categorization of antagonists into antibodies, RGD peptides, non-RGD peptides, peptidomimetics, and amine salts.
  • Analysis of pre-clinical anti-angiogenic and anti-tumor data associated with these antagonists.

Main Results:

  • Integrin alpha(v)beta(3) is highly expressed on tumor endothelial cells and tumor cells, making it a suitable target for anti-cancer therapies.
  • Numerous patents demonstrate the development of alpha(v)beta(3) antagonists with promising pre-clinical anti-angiogenic and anti-tumor activities.
  • Diverse strategies, including antibodies and various peptide-based molecules, are employed to antagonize alpha(v)beta(3).

Conclusions:

  • Integrin alpha(v)beta(3) represents a validated therapeutic target for anti-angiogenic and anti-tumor strategies.
  • The patent landscape reveals significant efforts in developing diverse alpha(v)beta(3) antagonists for cancer therapy.
  • Further clinical development of these antagonists holds promise for novel anti-cancer treatments.

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