Therapeutic Target Details
| Target ID: | T05 |
| Target Name: | Peroxisome proliferator-activated receptor gamma |
| Synonyms: | PPARG; PPARG-γ; PPARG-gamma; NR1C3; Nuclear receptor subfamily 1 group C member 3 |
| GENE: | PPARG |
| Action: | agonist |
| Class: | Nuclear hormone receptor |
| UniProtKB ID: | P37231 |
| Entry Name: | PPARG_HUMAN |
| Related Drugs: | Bezafibrate; Curcumin; DHA; Elafibranor; Epanova; Lobeglitazone; Omega 3 PUFA; Pioglitazone; Rosiglitazone; Telmisartan; Troglitazone |
| Mechanism: | The induction of PPARγ promotes the differentiation of large insulin-resistant pre-adipocytes into small, insulin-sensitive adipocytes. |
| Reference (PMIDs): | 8754811 |
| Drug ID | Drug Name | Type | DrugBank ID | Targets | Category | Latest Progress | |
|---|---|---|---|---|---|---|---|
| D033 | Bezafibrate | Chemical drug | DB01393 | PPARA agonist; PPARD agonist; PPARG agonist; NR1I2 partial agonist | Improve insulin resistance; Anti-inflammatory | Under clinical trials | Details |
| D092 | Curcumin | Chemical drug | DB11672 | PPARG; COX inhibitor | Anticancer agent; NSAID | Under clinical trials | Details |
| D105 | DHA | Chemical drug | DB03756 | PPARA ligand; PPARG ligand | Anti-inflammatory | Under clinical trials | Details |
| D119 | Elafibranor | Chemical drug | DB05187 | PPARA; PPARD; PPARG | Anti-inflammatory | Failed in clinical trials | Details |
| D125 | Epanova | Chemical drug | DB11133 | PPARG ligand; PPARA activator | Enhance lipid metabolism | Under clinical trials | Details |
| D208 | Lobeglitazone | Chemical drug | DB09198 | PPARG activator | Improve insulin resistance | Under clinical trials | Details |
| D258 | Omega 3 PUFA | Chemical drug | DB11133 | PPARG ligand; PPARA activator | Hypolipidemic drug | Under clinical trials | Details |
| D275 | Pioglitazone | Chemical drug | DB01132 | PPARG agonist | Improve insulin resistance | Advanced in clinical trials | Details |
| D311 | Rosiglitazone | Chemical drug | DB00412 | PPARG agonist; PPARA; PPARD | Improve insulin resistance | Failed in clinical trials | Details |
| D360 | Telmisartan | Chemical drug | DB00966 | PPARG partial agonist | Improve insulin resistance | Under clinical trials | Details |
| Candidate ID | Source ID | Source Type | Compound Type | Candidate Name | Inclusion Criteria | |
|---|---|---|---|---|---|---|
| R0043 | DB00132 | approved; investigational; nutraceutical | small molecule | alpha-Linolenic acid | Therapeutic strategy associated | Details |
| R0056 | DB00159 | approved; nutraceutical | small molecule | Icosapent | Therapeutic strategy associated | Details |
| R0093 | DB00244 | approved | small molecule | Mesalazine | Therapeutic strategy associated | Details |
| R0112 | DB00313 | approved; investigational | small molecule | Valproic acid | Therapeutic strategy associated | Details |
| R0117 | DB00328 | approved; investigational | small molecule | Indomethacin | Therapeutic strategy associated | Details |
| R0197 | DB00573 | approved | small molecule | Fenoprofen | Target associated | Details |
| R0257 | DB00731 | approved; investigational | small molecule | Nateglinide | Target associated | Details |
| R0282 | DB00795 | approved | small molecule | Sulfasalazine | Therapeutic strategy associated | Details |
| R0306 | DB00845 | approved; investigational | small molecule | Clofazimine | Therapeutic strategy associated | Details |
| R0330 | DB00912 | approved; investigational | small molecule | Repaglinide | Target associated | Details |
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| B000007 | CHEMBL10041 | Small molecule | AFIMOXIFENE | 387.52 | C26H29NO2 | BASE | Details |
| B000028 | CHEMBL101123 | Small molecule | -- | 661.6 | C33H29F6N3O5 | ACID | Details |
| B000036 | CHEMBL101263 | Small molecule | 4-NITROBENZOIC ACID | 167.12 | C7H5NO4 | ACID | Details |
| B000042 | CHEMBL1014 | Small molecule | CANDESARTAN CILEXETIL | 610.67 | C33H34N6O6 | ACID | Details |
| B000049 | CHEMBL1016 | Small molecule | CANDESARTAN | 440.46 | C24H20N6O3 | ACID | Details |
| B000055 | CHEMBL1017 | Small molecule | TELMISARTAN | 514.63 | C33H30N4O2 | ACID | Details |
| B000066 | CHEMBL102004 | Small molecule | -- | 649.55 | C31H28F9NO4 | ACID | Details |
| B000072 | CHEMBL1023 | Small molecule | BEXAROTENE | 348.49 | C24H28O2 | ACID | Details |
| B000083 | CHEMBL103 | Small molecule | PROGESTERONE | 314.47 | C21H30O2 | NEUTRAL | Details |
| B000104 | CHEMBL1042 | Small molecule | CHOLECALCIFEROL | 384.65 | C27H44O | NEUTRAL | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00219 | 35178989 | Zhongguo Zhong Yao Za Zhi | [Mechanism of Zexie Decoction in improvement of nonalcoholic fatty liver disease based on LKB1/AMPK/PGC-1α pathway]. | Details |
| A00383 | 35108454 | FEBS Open Bio | Carbonic anhydrase 3 increases during liver adipogenesis even in pre-obesity, and its inhibitors reduce liver adipose accumulation. | Details |
| A00390 | 35104757 | Phytomedicine | Seed oil of Rosa roxburghii Tratt against non-alcoholic fatty liver disease in vivo and in vitro through PPARα/PGC-1α-mediated mitochondrial oxidative metabolism. | Details |
| A00579 | 35041255 | Phytother Res | Activation of PGC-1α via isoliquiritigenin-induced downregulation of miR-138-5p alleviates nonalcoholic fatty liver disease. | Details |
| A00808 | 34959747 | Nutrients | High-Fructose, High-Fat Diet Alters Muscle Composition and Fuel Utilization in a Juvenile Iberian Pig Model of Non-Alcoholic Fatty Liver Disease. | Details |
| A01000 | 34906049 | Biochemistry (Mosc) | AMPK/PGC-1α/GLUT4-Mediated Effect of Icariin on Hyperlipidemia-Induced Non-Alcoholic Fatty Liver Disease and Lipid Metabolism Disorder in Mice. | Details |
| A01029 | 34897744 | J Appl Toxicol | Fluoxetine-induced hepatic lipid accumulation is mediated by prostaglandin endoperoxide synthase 1 and is linked to elevated 15-deoxy-Δ12,14 PGJ2. | Details |
| A01082 | 34874519 | Chin J Integr Med | Lycium barbarum Polysaccharides Promotes Mitochondrial Biogenesis and Energy Balance in a NAFLD Cell Model. | Details |
| A01811 | 34606980 | Endocr Pract | Antidiabetic Medications for Type 2 Diabetics with Nonalcoholic Fatty Liver Disease: Evidence From a Network Meta-Analysis of Randomized Controlled Trials. | Details |
| A01884 | 34573421 | Genes (Basel) | The Mitochondrial Trigger in an Animal Model of Nonalcoholic Fatty Liver Disease. | Details |
| A02434 | 34372491 | Viruses | Findings from Studies Are Congruent with Obesity Having a Viral Origin, but What about Obesity-Related NAFLD? | Details |
| A02523 | 34341928 | Environ Sci Pollut Res Int | Metronidazole enhances steatosis-related early-stage hepatocarcinogenesis in high fat diet-fed rats through DNA double-strand breaks and modulation of autophagy. | Details |
| A02528 | 34340181 | Environ Pollut | An adverse outcome pathway based in vitro characterization of novel flame retardants-induced hepatic steatosis. | Details |
| A02587 | 34321850 | World J Gastroenterol | PPARGC1A rs8192678 G>A polymorphism affects the severity of hepatic histological features and nonalcoholic steatohepatitis in patients with nonalcoholic fatty liver disease. | Details |
| A03245 | 34073834 | Int J Mol Sci | P2Y2R Deficiency Ameliorates Hepatic Steatosis by Reducing Lipogenesis and Enhancing Fatty Acid β-Oxidation through AMPK and PGC-1α Induction in High-Fat Diet-Fed Mice. | Details |
| A03247 | 34072832 | Cells | Epigenetic Regulation of Peroxisome Proliferator-Activated Receptor Gamma Mediates High-Fat Diet-Induced Non-Alcoholic Fatty Liver Disease. | Details |
| A03255 | 34069390 | Cells | Maternal Exercise Mediates Hepatic Metabolic Programming via Activation of AMPK-PGC1α Axis in the Offspring of Obese Mothers. | Details |
| A03289 | 34059612 | Curr Opin Cardiol | Update on cardiovascular risk in nonalcoholic fatty liver disease. | Details |
| A03632 | 33924115 | Int J Mol Sci | Chronic High Fat Diet Intake Impairs Hepatic Metabolic Parameters in Ovariectomized Sirt3 KO Mice. | Details |
| A03684 | 33902605 | Lipids Health Dis | Elucidation of SIRT-1/PGC-1α-associated mitochondrial dysfunction and autophagy in nonalcoholic fatty liver disease. | Details |