Target intelligence / Profile preview

Extracellular matrix adhesion receptor (ECM receptor)

Target
ECM receptor
Molecular classification
Receptor, Transmembrane protein, Cell adhesion molecule
01

Overview

Extracellular matrix (ECM) adhesion receptors are a diverse group of transmembrane proteins that mediate the physical attachment of cells to the surrounding matrix and facilitate bidirectional signaling between the intracellular and extracellular environments [Frontiers in Cell and Developmental Biology, 2021; NIH, 2011]. The most prominent members of this class are the integrins, which are heterodimeric receptors composed of alpha and beta subunits that recognize specific motifs, such as the Arg-Gly-Asp (RGD) sequence, in ECM proteins like collagen, fibronectin, and laminin [Frontiers in Cell and Developmental Biology, 2021; NIH, 2018]. Other important receptors include discoidin domain receptors (DDRs), syndecans, and CD44 [NIH, 2011; Tocris Bioscience]. These receptors play critical roles in regulating cell survival, proliferation, migration, and differentiation by integrating mechanical cues and biochemical signals [Frontiers in Cell and Developmental Biology, 2021; MDPI, 2024]. Dysregulation of ECM adhesion receptors is a hallmark of many diseases, including cancer metastasis, where they promote tumor cell invasion and angiogenesis, as well as inflammatory and fibrotic disorders [Frontiers in Cell and Developmental Biology, 2021; NIH, 2025; Tocris Bioscience]. Consequently, they have become significant therapeutic targets, with several approved drugs successfully modulating their activity to treat cardiovascular diseases, autoimmune conditions, and chronic inflammation [NIH, 2009; NIH, 1998].

Other names
Cell-matrix adhesion receptorECM receptorIntegrinCell adhesion molecule (CAM)
02

Mechanism of action

Competitive inhibition of ligand binding to the extracellular domain (e.g., RGD-mimetics), allosteric modulation of receptor conformation to prevent activation, and blocking of receptor-cytoskeleton interactions to inhibit downstream signaling pathways like FAK/Src [Frontiers in Cell and Developmental Biology, 2021; NIH, 2009].

03

Biological functions

Cell adhesionSignal transductionMechanotransductionCell migrationCell proliferationCell differentiationApoptosis regulationTissue homeostasis
04

Disease associations

CancerInflammationFibrosisCardiovascular diseaseAutoimmune disease
05

Safety considerations

Bleeding and thrombocytopenia (primarily with anti-platelet integrin inhibitors)Increased risk of opportunistic infections such as Progressive Multifocal Leukoencephalopathy (PML) with immunomodulatory agentsFunctional redundancy among receptor subtypes leading to limited clinical efficacyPotential for paradoxical activation of signaling pathways
06

Interacting drugs

Abciximab

7 more in the full profile.

07

Biomarkers

Integrin alphaV beta3 expressionSoluble CD44Collagen degradation products (e.g., CTX-I)Fibronectin levels

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