Target intelligence / Profile preview

Integrin Alpha 5 Beta 1 (α5β1)

Target
α5β1
Molecular classification
Receptor, Integrin, Cell adhesion molecule
01

Overview

Integrin alpha 5 beta 1 (α5β1), also known as the fibronectin receptor, is a heterodimeric cell surface receptor composed of two subunits: α5 (ITGA5/CD49e) and β1 (ITGB1/CD29). It mediates cell-extracellular matrix (ECM) adhesion and plays critical roles in cellular signaling, migration, proliferation, survival, and differentiation. It primarily binds fibronectin via the RGD motif and is implicated in cancer metastasis, angiogenesis, and wound healing. It functions by triggering downstream signalling cascades involving kinases, leading to cytoskeletal reorganisation.

Other names
Fibronectin receptorITGA5/ITGB1CD49e/CD29
02

Mechanism of action

Inhibition of α5β1 binding to fibronectin, disruption of focal adhesion signaling, modulation of downstream kinase activity (e.g., FAK/Src), interference with actin cytoskeleton reorganization

03

Biological functions

Cell adhesionCell migrationFocal adhesion formationAngiogenesisCell signalingECM interaction
04

Disease associations

Cancer progressionCancer metastasisWound healingTissue repair
05

Safety considerations

Potential for off-target effects due to integrin family homologyRisk of disrupting normal cell adhesion and tissue homeostasisPotential for immune-related adverse events
06

Biomarkers

α5β1 expression levels in tumor tissueα5β1 expression levels in tumor vasculatureSoluble α5β1 levels in serum

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