Target intelligence / Profile preview

Integrin αMβ2 (αMβ2)

Target
αMβ2
Molecular classification
Integrin (heterodimeric transmembrane receptor), Receptor (cell adhesion and signaling), Pattern recognition receptor (innate immune functions)
01

Overview

Integrin αMβ2 (Mac-1, CR3) is a leukocyte-specific receptor found on monocytes, macrophages, neutrophils, dendritic cells, and some lymphocytes. It consists of two subunits, αM (ITGAM/CD11b) and β2 (ITGB2/CD18), forming a heterodimer that mediates cell-to-cell and cell-to-matrix interactions essential for immune responses. αMβ2’s extracellular domains bind multiple ligands, including inactivated complement (iC3b), fibrinogen, and adhesion molecules on the endothelium, facilitating immune cell recruitment and phagocytosis. It is involved in the pathogenesis of several inflammatory and autoimmune diseases, notably systemic lupus erythematosus, through genetic associations. Therapies targeting αMβ2 are under investigation for their ability to reduce inappropriate immune activation, although modulation risks suppressing host defenses.

Other names
Macrophage-1 antigen (Mac-1)Complement receptor 3 (CR3)CD11b/CD18ITGAM/ITGB2CR3ACluster of differentiation molecule 11B (CD11B)Leukocyte beta-2 integrin
02

Mechanism of action

Inhibition of leukocyte adhesion and migration (blockade of integrin interactions); Blockade of phagocytosis (e.g. antibodies occupy ligand binding sites); Inhibition of complement binding (preventing iC3b interaction); Prevention of immune synapse stabilization (inhibition of cell-cell interactions).

03

Biological functions

Leukocyte adhesion and migrationPhagocytosis (especially of opsonized particles and pathogens)Cell-mediated cytotoxicityChemotaxisCellular activationRegulation of the complement system (binding to iC3b)Formation/stabilization of immunological synapsesRestriction of B cell signalingModulation of cytokine secretionImmune synapse formation (T cell, dendritic cell, platelet activation)
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Disease associations

InflammationCardiovascular disease (atherosclerosis, thrombosis)Autoimmune disease (notably systemic lupus erythematosus)InfectionCancer (immunomodulation and tumor microenvironment involvement)Other immune-related disorders
05

Safety considerations

Potential for increased infection risk (impaired leukocyte migration and phagocytosis if blocked)Impaired wound healing or host defensePossible off-target or excessive immunosuppressionInterference with platelet function may raise bleeding risk during therapy targeting this integrin
06

Interacting drugs

Monoclonal antibodies that block integrin αMβ2 function

3 more in the full profile.

07

Biomarkers

CD11b/CD18 expression (flow cytometry for immune cell profiling)Activated CD11b measured in inflammation and cardiovascular diseaseGenetic polymorphisms in ITGAM associated with lupus risk

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