Target intelligence / Profile preview

Integrin alpha-6 beta-1 (α6β1 integrin or VLA-6)

Target
α6β1 integrin or VLA-6
Molecular classification
Receptor, Adhesion receptor, Integrin family, Catalytic receptor (per some databases; integrins transduce signals but do not catalyze chemical reactions directly)[4][7][8]
01

Overview

Integrin alpha-6 beta-1 (α6β1 integrin) is a heterodimeric cell surface receptor formed by the non-covalent association of the α6 (ITGA6/CD49f) and β1 (ITGB1/CD29) subunits. It is a prototypical laminin receptor highly expressed on epithelial cells, stem cells, endothelial cells, and various cell types in adult tissues and during development. α6β1 mediates adhesion to basement membrane laminins, regulates key aspects of cell proliferation, stem cell maintenance, migration, and survival via bi-directional signaling. In cancer, α6β1 plays important roles in tumor progression, metastasis, and cancer stem cell regulation, making it a target of interest for therapeutic and diagnostic development. As with other integrins, α6β1 can transduce mechanical and chemical signals and is critical for tissue organization and response to injury[1][2][4][5][7][9].

Other names
CD49f/CD29 complexVLA-6Laminin receptor (when referring specifically to α6β1)ITGA6/ITGB1Platelet glycoprotein GPIc-IIa[1][4][5][9]
02

Mechanism of action

Inhibition of α6β1 blocks cell adhesion to laminin, affects stem cell function, can inhibit migration/metastasis in models. Activating antibodies increase ligand binding affinity and can modulate integrin conformation/activation[2][3][9].

03

Biological functions

Cell adhesion to extracellular matrix (basement membrane)Signal transduction (bidirectional, outside-in and inside-out)Stem cell self-renewal and maintenanceRegulation of cell proliferation and migrationCell differentiationCell survival[2][3][4][5][7]
04

Disease associations

Cancer (notably cancer stem cell biology and metastasis)Inflammation (e.g., colitis)Tissue regenerationPotential involvement in infection (e.g., viral entry or tissue tropism)Other (angiogenesis, tissue development)[2][3][7]
05

Safety considerations

Targeting integrins broadly (not only α6β1) can cause impaired wound healing, bleeding risk, and immune system dysregulationPotential for unintended disruption of normal stem cell or epithelial maintenanceRedundancy and compensation by other integrins complicate therapeutic targeting[7]
06

Interacting drugs

No small-molecule drugs are currently approved that specifically target α6β1 integrin, but research antibodies (e.g., GoH3, TS2/16) and some experimental agents modulate this integrin in preclinical/clinical research[2][5][9]
07

Biomarkers

CD49f (α6) is used as a biomarker for human and mouse pluripotent stem cells and for cancer stem cells[2][5]Expression of α6β1 is used as a marker in some tumor tissues and stem cell isolation protocols[2][4][5]

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