Integrin α5β1 receptor (Integrin α5β1)

Integrin α5β1 receptor is a heterodimeric transmembrane cell adhesion receptor highly expressed on osteoblasts and progenitor cells, where it mediates interaction with extracellular matrix proteins, primarily fibronectin[2][4]. As a member of the integrin family, α5β1 facilitates adhesion, migration, differentiation, and proliferation of osteoblast lineage cells, participating in the regulation of bone formation and remodeling[2][1][5]. It also integrates mechanical force signals to upregulate osteogenic genes and plays a crucial role in the differentiation of mesenchymal stem cells into osteoblasts. Dysregulation of integrin α5β1 has been linked to diseases such as osteoporosis, osteoarthritis, and cancer metastasis to bone, making it a promising therapeutic target[2][1]. Drugs targeting integrin α5β1 act mainly by inhibiting cell-ECM binding, thereby influencing cell survival, migration, and pathological bone resorption[2]. Integrin α5β1 remains under investigation for biomarker-guided therapy and targeted therapy in skeletal and oncologic diseases.

Other names

Integrin alpha-5 beta-1Fibronectin receptorCD49e/CD29α5β1 integrinVery late antigen-5 (VLA-5)

Inhibition of integrin-ligand binding, Disruption of cell-extracellular matrix (ECM) adhesion, Blockade of downstream signaling like FAK/ERK pathway, Suppression of osteoclastogenesis and pathological cell migration