Therapeutic Target Details
| Target ID: | T09 |
| Target Name: | Toll-like receptor 4 |
| Synonyms: | TLR-4; hToll; TLR4 |
| GENE: | TLR4 |
| Action: | antagonist |
| Class: | Membrane receptor |
| UniProtKB ID: | O00206 |
| Entry Name: | TLR4_HUMAN |
| Related Drugs: | JKB-121 |
| Mechanism: | Increased hepatocyte Jagged1 is the proximal hit for Notch-induced liver fibrosis in mice and suggest translational potential of Jagged1 inhibitors in patients with NASH. |
| Reference (PMIDs): | 34162749 |
| Drug ID | Drug Name | Type | DrugBank ID | Targets | Category | Latest Progress |
|---|
| Candidate ID | Source ID | Source Type | Compound Type | Candidate Name | Inclusion Criteria | |
|---|---|---|---|---|---|---|
| R0334 | DB00924 | approved | small molecule | Cyclobenzaprine | Target associated | Details |
| R0437 | DB01183 | approved; vet_approved | small molecule | Naloxone | Target associated | Details |
| R0571 | DB02767 | experimental | small molecule | (R)-3-hydroxytetradecanoic acid | Target associated | Details |
| R0574 | DB03017 | approved; experimental | small molecule | Lauric acid | Target associated | Details |
| R0653 | DB04933 | investigational | small molecule | Eritoran | Target associated | Details |
| R0811 | DB05475 | investigational | small molecule | Golotimod | Target associated | Details |
| R0902 | DB05943 | investigational | small molecule | Resatorvid | Therapeutic strategy associated | Details |
| R1017 | DB06447 | investigational | small molecule | E5531 | Target associated | Details |
| R1140 | DB08231 | experimental | small molecule | Myristic acid | Target associated | Details |
| R1290 | DB09301 | approved; investigational; nutraceutical | small molecule | Chondroitin sulfate | Therapeutic strategy associated | Details |
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| B002069 | CHEMBL1223751 | Small molecule | -- | 458.0 | C25H32ClN3O3 | NEUTRAL | Details |
| B002070 | CHEMBL1223752 | Small molecule | -- | 355.48 | C22H29NO3 | NEUTRAL | Details |
| B017920 | CHEMBL1357139 | Small molecule | -- | 489.4 | C21H21BrN4O3S | NEUTRAL | Details |
| B029662 | CHEMBL1401818 | Small molecule | -- | 335.35 | C16H12F3N3S | NEUTRAL | Details |
| B038331 | CHEMBL1434377 | Small molecule | -- | 438.55 | C23H26N4O3S | NEUTRAL | Details |
| B040914 | CHEMBL1443979 | Small molecule | -- | 325.32 | C14H10F3N3OS | NEUTRAL | Details |
| B051772 | CHEMBL1485094 | Small molecule | -- | 450.54 | C24H23FN4O2S | NEUTRAL | Details |
| B055079 | CHEMBL1497476 | Small molecule | -- | 434.52 | C23H22N4O3S | NEUTRAL | Details |
| B059641 | CHEMBL1514722 | Small molecule | -- | 444.49 | C24H17FN4O2S | NEUTRAL | Details |
| B085194 | CHEMBL1612879 | Small molecule | -- | 363.42 | C20H21N5O2 | NEUTRAL | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00450 | 35077907 | Environ Toxicol Pharmacol | Enterobacter cloacae aggravates metabolic disease by inducing inflammation and lipid accumulation. | Details |
| A00598 | 35035359 | Front Physiol | Exercise Alleviates the Apolipoprotein A5-Toll-Like Receptor 4 Axis Impairment in Mice With High-Fat Diet-Induced Non-alcoholic Steatohepatitis. | Details |
| A00875 | 34943814 | Cells | Exercise-Induced Irisin Decreases Inflammation and Improves NAFLD by Competitive Binding with MD2. | Details |
| A00969 | 34915801 | Pharm Biol | Jiang Zhi Granule protects immunological barrier of intestinal mucosa in rats with non-alcoholic steatohepatitis. | Details |
| A01443 | 34743980 | Eur J Pharmacol | Preventive and therapeutic role of betaine in liver disease: A review on molecular mechanisms. | Details |
| A01446 | 34742934 | Arch Biochem Biophys | The probiotic effects of AB23A on high-fat-diet-induced non-alcoholic fatty liver disease in mice may be associated with suppressing the serum levels of lipopolysaccharides and branched-chain amino acids. | Details |
| A01652 | 34667947 | JHEP Rep | New targets for NAFLD. | Details |
| A01696 | 34651580 | J Clin Invest | Sparcl1 promotes nonalcoholic steatohepatitis progression in mice through upregulation of CCL2. | Details |
| A01969 | 34548598 | Sci Rep | Conditioned medium from stem cells derived from human exfoliated deciduous teeth ameliorates NASH via the Gut-Liver axis. | Details |
| A01980 | 34543583 | Arch Physiol Biochem | Dipeptedyl peptidase-4 (DPP-4) inhibitor downregulates HMGB1/TLR4/NF-κB signaling pathway in a diabetic rat model of non-alcoholic fatty liver disease. | Details |
| A02165 | 34478730 | Arch Biochem Biophys | Luteolin alleviates non-alcoholic fatty liver disease in rats via restoration of intestinal mucosal barrier damage and microbiota imbalance involving in gut-liver axis. | Details |
| A02254 | 34445644 | Int J Mol Sci | Resveratrol and Quercetin as Regulators of Inflammatory and Purinergic Receptors to Attenuate Liver Damage Associated to Metabolic Syndrome. | Details |
| A02307 | 34426178 | J Integr Med | Hepatic protective effects of Shenling Baizhu powder, a herbal compound, against inflammatory damage via TLR4/NLRP3 signalling pathway in rats with nonalcoholic fatty liver disease. | Details |
| A02462 | 34363921 | J Hepatol | Regulatory T-cell and neutrophil extracellular trap interaction contributes to carcinogenesis in non-alcoholic steatohepatitis. | Details |
| A02583 | 34322898 | Hepatology | Guanine Nucleotide-Binding Protein G(i) Subunit Alpha 2 Exacerbates NASH Progression by Regulating Peroxiredoxin 1-Related Inflammation and Lipophagy. | Details |
| A02898 | 34203178 | Int J Mol Sci | Intestinal Permeability Is a Mechanical Rheostat in the Pathogenesis of Liver Cirrhosis. | Details |
| A03017 | 34162749 | Sci Transl Med | Hepatocyte TLR4 triggers inter-hepatocyte Jagged1/Notch signaling to determine NASH-induced fibrosis. | Details |
| A03252 | 34070893 | Mar Drugs | Attenuating Effects of Dieckol on High-Fat Diet-Induced Nonalcoholic Fatty Liver Disease by Decreasing the NLRP3 Inflammasome and Pyroptosis. | Details |
| A03665 | 33915261 | J Nutr Biochem | Consumption of soybean or olive oil at recommended concentrations increased the intestinal microbiota diversity and insulin sensitivity and prevented fatty liver compared to the effects of coconut oil. | Details |
| A03945 | 33810882 | Clin Investig Arterioscler | Alleviation of non-alcoholic fatty liver disease by Huazhi Fugan Granules is associated with suppression of TLR4/NF-κB signaling pathway. | Details |