Target intelligence / Profile preview

Integrin (cell surface receptor) (Integrin)

Target
Integrin
Molecular classification
Receptor, Cell-adhesion molecule, Transmembrane glycoprotein, Heterodimeric protein complex
01

Overview

Integrins are heterodimeric transmembrane receptors consisting of α and β subunits that connect cells to the extracellular matrix by binding ECM proteins such as collagen, fibronectin, and laminin. They function as structural anchors and as major signal transducers, enabling cells to sense and respond to biochemical and mechanical properties of their environment. Integrins are vital for cell survival, migration, proliferation, and tissue integrity, and play roles in normal development, wound healing, immune responses, and a wide variety of diseases including cancer, fibrosis, cardiovascular disease, and inflammation. Multiple integrin subtypes exist, and their biological effects depend on their specific α/β combinations and tissue context. Integrin-targeting drugs exploit their roles in cell migration and adhesion, but clinical use is sometimes limited by infection and bleeding risks.

Other names
IntegrinsCell-surface integrin receptorECM receptorsα/β integrin heterodimers (e.g., α5β1, αVβ3, etc.)
02

Mechanism of action

Inhibition of integrin-ligand binding prevents cell adhesion, migration, or immune cell trafficking; Antagonism disrupts platelet aggregation (for anti-thrombotic drugs); Direct modulation of intracellular signaling pathways (FAK, PI3K/Akt, MAPK)

03

Biological functions

Cell adhesion (to ECM)Signal transduction (mechanotransduction and chemical signaling)Cell migrationCell proliferation and survivalTissue architecture and organizationMatrix assembly
04

Disease associations

Cancer (metastasis, invasion)Inflammation (autoimmune diseases)Cardiovascular diseaseFibrosisInfection
05

Safety considerations

Infection risk (due to immunosuppression with anti-integrin therapies)Bleeding risk (with platelet integrin inhibitors)Impaired wound healingProgressive multifocal leukoencephalopathy (PML) for certain anti-integrin drugs (natalizumab)
06

Interacting drugs

Natalizumab (targets α4-integrins, used in multiple sclerosis)

4 more in the full profile.

07

Biomarkers

Integrin expression profiles (β1, β3, αV, α4, α5) in tumors or tissuesSoluble integrin levels in blood (rare, under investigation)Matrix metalloprotease activity (for ECM remodeling)

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