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Target intelligence / Profile preview
Integrin alpha-5 beta-1 receptor (α5β1-integrin)
- Target
- α5β1-integrin
- Molecular classification
- Receptor, Cell adhesion molecule, Integrin family (heterodimeric transmembrane glycoproteins)
01
Overview
Integrin alpha‑5 beta‑1 receptor (α5β1‑integrin) is a heterodimeric transmembrane protein composed of an alpha‑subunit (ITGA5/CD49e) and a beta‑subunit (ITGB1/CD29). It functions primarily as the main cellular receptor for fibronectin via recognition of the RGD sequence within its ligand. This integrin mediates cell-extracellular matrix interactions essential for cell adhesion, migration, proliferation, survival signaling pathways, and plays a pivotal role in physiological processes such as embryonic development and pathological conditions like cancer progression through promotion of angiogenesis. Its upregulation is associated with tumor neovascularization making it an attractive target for anti-cancer therapies[2][3][4][8].
- Other names
- Fibronectin receptorVLA-5 (Very Late Antigen 5)ITGA5/ITGB1CD49e/CD29
02
Mechanism of action
Drugs targeting α5β1-integrin typically act by inhibiting its interaction with fibronectin or other ligands, thereby blocking downstream signaling pathways involved in cell adhesion, migration, and angiogenesis. This can suppress tumor growth and metastasis by disrupting tumor vasculature formation[1].
03
Biological functions
Cell adhesion to the extracellular matrixSignal transduction across the plasma membraneRegulation of cell migration and activationMatrix fibrillogenesis (formation of fibrous extracellular matrix)Angiogenesis (formation of new blood vessels)[4][5]
04
Disease associations
Cancer (tumor angiogenesis, metastasis)[1][4][5]Inflammation[4]
05
Safety considerations
Potential safety concerns include impaired wound healing, bleeding risk due to effects on normal angiogenesis and tissue repair processes, as well as possible immune reactions to biologic agents such as monoclonal antibodies.
06
Interacting drugs
Specific drugs directly targeting α5β1-integrin are under investigation, including monoclonal antibodies and small molecules. Volociximab is a notable example—a chimeric antibody that targets α5β1-integrin for antiangiogenic therapy in cancer[1]. Other RGD-mimetic compounds may also interact with this integrin.
07
Biomarkers
Expression levels of α5β1-integrin on tumor vasculature or cancer cells can serve as biomarkers for patient selection or monitoring therapeutic efficacy in antiangiogenic therapies[4][5].
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