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50 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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TLR4
toll like receptor 4
Chromosome 9 · 9q33.1
NCBI Gene: 7099Ensembl: ENSG00000136869.16HGNC: HGNC:11850UniProt: O00206
2,775PubMed Papers
20Diseases
3Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Hub GeneReceptor
RESEARCH IMPACT
Highly Studied
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
defense response to bacteriumprotein heterodimerization activityplasma membranepositive regulation of chemokine (C-X-C motif) ligand 2 productionmajor depressive disorderSepsistype 2 diabetes mellitusulcerative colitis
✦AI Summary

TLR4 (Toll-like receptor 4) is a transmembrane pattern recognition receptor that initiates innate immune responses by detecting pathogen-associated molecular patterns (PAMPs) and damage-associated molecular patterns (DAMPs) 1. The receptor primarily recognizes bacterial lipopolysaccharide (LPS) at the plasma membrane in cooperation with LY96, triggering two distinct signaling cascades 12. Initially, TLR4 activates the MyD88/TIRAP pathway at the cell surface, leading to NF-κB activation and pro-inflammatory cytokine secretion 2. Subsequently, CD14-mediated endocytosis of TLR4 initiates a secondary TRIF/TRAM-dependent pathway in early endosomes, resulting in type I interferon production 1. TLR4 expression is regulated by m6A methylation through METTL3, which increases TLR4 mRNA translation and protein stability, enhancing neutrophil activation during endotoxemia 3. The receptor's clinical significance spans multiple diseases: it promotes hepatocellular carcinoma progression and metastasis through the HMGB1-KLF7-TLR4 feedback loop 4, associates with papillary thyroid carcinoma advancement 5, and modulates intestinal immune responses to breast milk components 6. Therapeutically, TLR4 can be targeted with specific inhibitors like TAK-242, which disrupts adaptor protein interactions 7, or with agonistic antibodies that require IgG3-mediated receptor clustering for tolerance induction 8.

Sources cited
1
TLR4 trafficking and dual signaling pathways involving MyD88 at plasma membrane and TRIF in endosomes
PMID: 33057840
2
TLR4-LPS signaling pathway overview and NF-κB activation
PMID: 18304834
3
METTL3-mediated m6A modification regulates TLR4 expression and neutrophil activation
PMID: 36920907
4
TLR4's role in hepatocellular carcinoma progression through HMGB1-KLF7-TLR4 axis
PMID: 37554278
5
TLR4 upregulation in papillary thyroid carcinoma and association with metastasis
PMID: 36165427
6
TLR4 modulation by human milk components in intestinal epithelial cells
PMID: 38862662
7
TAK-242 inhibitor mechanism through disruption of TLR4-adaptor interactions
PMID: 20881006
8
IgG3-mediated receptor clustering required for agonistic TLR4 antibody function
PMID: 40464120
Disease Associationsⓘ20
major depressive disorderOpen Targets
0.51Moderate
SepsisOpen Targets
0.41Moderate
type 2 diabetes mellitusOpen Targets
0.40Moderate
ulcerative colitisOpen Targets
0.40Weak
dengue diseaseOpen Targets
0.39Weak
inborn error of immunityOpen Targets
0.37Weak
psoriasisOpen Targets
0.37Weak
periodontitisOpen Targets
0.36Weak
Crohn's diseaseOpen Targets
0.36Weak
ankylosing spondylitisOpen Targets
0.36Weak
adolescent idiopathic scoliosisOpen Targets
0.35Weak
sclerosing cholangitisOpen Targets
0.35Weak
smoking behaviorOpen Targets
0.33Weak
obesityOpen Targets
0.33Weak
diabetic ketoacidosisOpen Targets
0.33Weak
chronic obstructive pulmonary diseaseOpen Targets
0.33Weak
metabolic syndromeOpen Targets
0.29Weak
osteoarthritis, kneeOpen Targets
0.29Weak
cervical carcinomaOpen Targets
0.27Weak
total knee arthroplastyOpen Targets
0.27Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets3
ERITORANPhase III
Toll-like receptor 4/MD-2 antagonist
Sepsis
ERITORAN TETRASODIUMPhase III
Toll-like receptor 4/MD-2 antagonist
Sepsis
RESATORVIDPhase III
Toll-like receptor 4 inhibitor
Sepsis
Related Genes
CD47Protein interaction100%HSPA1BProtein interaction100%HSPA9Protein interaction100%HSPD1Protein interaction100%IRF7Protein interaction100%S100A1Protein interaction100%
Tissue Expression6 tissues
Bone Marrow
100%
Lung
68%
Heart
53%
Brain
29%
Liver
18%
Ovary
17%
Gene Interaction Network
Click a node to explore
TLR4CD47HSPA1BHSPA9HSPD1IRF7S100A1
PROTEIN STRUCTURE
Preparing viewer…
PDB2Z62 · 1.70 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.86LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.58 [0.41–0.86]
RankingsWhere TLR4 stands among ~20K protein-coding genes
  • #24of 20,598
    Most Researched2,775 · top 1%
  • #7,496of 17,882
    Most Constrained (LOEUF)0.86
Genes detectedTLR4
Sources retrieved50 papers
Response time—
📄 Sources
50▼
1
TLR4 and CD14 trafficking and its influence on LPS-induced pro-inflammatory signaling.
PMID: 33057840
Cell Mol Life Sci · 2021
1.00
2
LPS/TLR4 signal transduction pathway.
PMID: 18304834
Cytokine · 2008
0.90
3
TLR2 and TLR4 Differentially Regulate the Osteogenic Capacity of Human Periodontal Ligament Fibroblasts.
PMID: 33512337
J Int Acad Periodontol · 2021
0.84
4
Association between TLR2 and TLR4 Gene Polymorphisms and the Susceptibility to Inflammatory Bowel Disease: A Meta-Analysis.
PMID: 26023918
PLoS One · 2015
0.82
5
HMGB1-mediated elevation of KLF7 facilitates hepatocellular carcinoma progression and metastasis through upregulating TLR4 and PTK2.
PMID: 37554278
Theranostics · 2023
0.80