Target intelligence / Profile preview

Integrin alpha-V beta-3 receptor and Integrin alpha-V beta-5 receptor (α_Vβ_3 (for Integrin alpha-V beta-3 receptor) α_Vβ_5 (for Integrin alpha-V beta-5 receptor))

Target
α_Vβ_3 (for Integrin alpha-V beta-3 receptor) α_Vβ_5 (for Integrin alpha-V beta-5 receptor)
Molecular classification
Receptor (Transmembrane adhesion receptor), Integrin family, Type I membrane protein
01

Overview

Integrin alpha-V beta-3 receptor and Integrin alpha-V beta-5 receptor are transmembrane receptors composed of an alpha and beta chain, classified within the integrin family. They mediate cell adhesion by binding to extracellular matrix proteins such as vitronectin and fibronectin, and facilitate processes including cell migration, signal transduction, and angiogenesis. Both receptors are widely expressed on endothelial cells, fibroblasts, epithelial cells, immune cells, and certain tumor cells. Their abnormal expression and function have been implicated in cancer progression, pathological angiogenesis, fibrosis, and inflammatory diseases. Therapeutically, these integrins are targeted to inhibit vascularization in tumors and modulate inflammation. Drugs targeting these receptors block ECM ligand binding or induce apoptosis, and have been studied as anti-cancer and anti-fibrotic agents. Safety concerns include the potential for delayed wound healing and immunological side effects due to their important roles in normal tissue homeostasis[2][3][4][5][6][7][9].

Other names
Vitronectin receptorIntegrin alpha-V beta-3Integrin alpha-V beta-5ITGAV/ITGB3ITGAV/ITGB5CD61
02

Mechanism of action

Blockade of ligand binding (especially inhibition of vitronectin/fibronectin interactions); Inhibition of angiogenesis; Induction of apoptosis (ProAgio recruits caspase 8 after binding); Interference with signal transduction required for cell migration, survival, proliferation.

03

Biological functions

Cell adhesionSignal transductionCell migration and motilityAngiogenesis (formation of new blood vessels)Phagocytosis (especially by macrophages)Tissue remodeling and wound healingMorphogenesis in pancreatic development
04

Disease associations

Cancer (particularly tumor angiogenesis and metastasis)InflammationFibrosisCardiovascular disease (due to effects on vascular remodeling)Muscle regenerationOrgan development
05

Safety considerations

Risk of impaired wound healing due to disrupted physiological angiogenesisPotential for thrombocytopeniaOff-target effects and lack of efficacy in certain solid tumorsImmune-mediated adverse reactions to therapeutic antibodies
06

Interacting drugs

Etaracizumab

4 more in the full profile.

07

Biomarkers

Expression levels of α_Vβ_3 and α_Vβ_5 on endothelial cells and tumor cells for patient selection in anti-angiogenic therapiesCirculating soluble fragments or activation state

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