Target intelligence / Profile preview

Toll-like receptor 2 (TLR2) (TLR2)

Target
TLR2
Molecular classification
Receptor, Pattern recognition receptor, Toll-like receptor family
01

Overview

Toll-like receptor 2 (TLR2) is a pivotal transmembrane protein belonging to the pattern recognition receptor (PRR) family, primarily expressed on the surface of macrophages, monocytes, and dendritic cells (UniProt P49768). It plays a central role in the innate immune system by detecting various pathogen-associated molecular patterns (PAMPs), including lipoproteins, lipoteichoic acid, and peptidoglycan from Gram-positive bacteria (PubMed: 11113287). Upon ligand recognition, TLR2 typically functions as a heterodimer with either TLR1 or TLR6, initiating a signaling cascade through the MyD88 adapter protein that leads to the activation of NF-kappaB and the production of pro-inflammatory cytokines (NIH: PMC3002672). In clinical pathology, TLR2 is implicated in a wide range of conditions, including sepsis, rheumatoid arthritis, and ischemia-reperfusion injury, where its overactivation drives harmful systemic inflammation (PubMed: 25617461). Therapeutic interventions targeting TLR2 include monoclonal antibodies like Tomaralimab (OPN-305), which acts as an antagonist to reduce inflammation in transplant and cardiac settings, as well as various synthetic agonists used as vaccine adjuvants to enhance immunogenicity (ClinicalTrials.gov: NCT01794663). These agents aim to either suppress pathological inflammation or harness the innate immune system to combat pathogens and malignant cells (PubMed: 25617461).

Other names
CD282Toll/interleukin-1 receptor-like protein 4TIL4
02

Mechanism of action

TLR2 modulators function by either antagonizing the receptor to block pro-inflammatory signaling pathways (e.g., NF-kappaB) in inflammatory diseases or by agonizing the receptor to stimulate innate immune responses for vaccine adjuvancy and oncology.

03

Biological functions

Immune responseSignal transductionCytokine productionApoptosis
04

Disease associations

InflammationInfectionCancerCardiovascular diseaseAutoimmune disease
05

Safety considerations

Increased susceptibility to Gram-positive bacterial infectionsRisk of cytokine release syndrome with agonistsPotential interference with tissue repair and wound healing
06

Interacting drugs

Tomaralimab (OPN-305)

4 more in the full profile.

07

Biomarkers

TLR2 surface expression on CD14+ monocytesSerum IL-6 levelsTNF-alpha production capacity

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