Therapeutic Target Details
| Target ID: | T04 |
| Target Name: | Peroxisome proliferator-activated receptor delta |
| Synonyms: | PPARD; PPAR-δ; PPAR-delta; NR1C2; NUC1; NUCI; Nuclear hormone receptor 1; Nuclear receptor subfamily 1 group C member 2; Peroxisome proliferator-activated receptor beta; PPAR-beta; PPARB; PPAR-β; PPAR β/δ |
| GENE: | PPARD |
| Action: | agonist |
| Class: | Nuclear hormone receptor |
| UniProtKB ID: | Q03181 |
| Entry Name: | PPARD_HUMAN |
| Related Drugs: | Bezafibrate; Elafibranor; Rosiglitazone |
| Mechanism: | Activation of PPARβ/δ promotes fatty acid metabolism and suppresses macrophage-mediated inflammation; Hepatic PPARβ/δ is involved in transforming potentially toxic lipids into less toxic molecules by regulating monounsaturated fatty acid synthesis and increasing AMP-activated protein kinase activity, thereby suppressing lipogenesis and glycogen synthesis, reducing gluconeogenesis, and increasing fatty acid oxidation. PPARβ/δ also stimulates anti-inflammatory responses in the liver. |
| Reference (PMIDs): | 35242173 |
| 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 |
| D119 | Elafibranor | Chemical drug | DB05187 | PPARA; PPARD; PPARG | Anti-inflammatory | Failed in clinical trials | Details |
| D311 | Rosiglitazone | Chemical drug | DB00412 | PPARG agonist; PPARA; PPARD | Improve insulin resistance | Failed in 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 |
| R0112 | DB00313 | approved; investigational | small molecule | Valproic acid | Therapeutic strategy associated | Details |
| R0134 | DB00374 | approved; investigational | small molecule | Treprostinil | Therapeutic strategy associated | Details |
| R0212 | DB00605 | approved; investigational | small molecule | Sulindac | Therapeutic strategy associated | Details |
| R0570 | DB02746 | experimental | small molecule | Phthalic Acid | Target associated | Details |
| R0582 | DB03338 | experimental | small molecule | Heptyl glucoside | Target associated | Details |
| R0597 | DB04224 | approved; investigational; vet_approved | small molecule | Oleic Acid | Target associated | Details |
| R0616 | DB04801 | experimental | small molecule | cis-Vaccenic acid | Target associated | Details |
| R0727 | DB05188 | investigational | small molecule | KD3010 | 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 |
| B000037 | CHEMBL101326 | Small molecule | FIPRONIL | 437.15 | C12H4Cl2F6N4OS | NEUTRAL | Details |
| B000055 | CHEMBL1017 | Small molecule | TELMISARTAN | 514.63 | C33H30N4O2 | ACID | Details |
| B000066 | CHEMBL102004 | Small molecule | -- | 649.55 | C31H28F9NO4 | ACID | Details |
| B000083 | CHEMBL103 | Small molecule | PROGESTERONE | 314.47 | C21H30O2 | NEUTRAL | Details |
| B000104 | CHEMBL1042 | Small molecule | CHOLECALCIFEROL | 384.65 | C27H44O | NEUTRAL | Details |
| B000131 | CHEMBL104850 | Small molecule | -- | 416.48 | C25H24N2O4 | ACID | Details |
| B000134 | CHEMBL104943 | Small molecule | MONOETHANOLAMINE | 61.08 | C2H7NO | BASE | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A11238 | 30978698 | J Mol Endocrinol | Humulus japonicus stimulates thermogenesis and ameliorates oxidative stress in mouse adipocytes. | Details |
| A44517 | 28386270 | PPAR Res | Fimasartan Ameliorates Nonalcoholic Fatty Liver Disease through PPARδ Regulation in Hyperlipidemic and Hypertensive Conditions. | Details |
| A49895 | 35605662 | J Biol Chem | Selective PPARδ agonist seladelpar suppresses bile acid synthesis by reducing hepatocyte CYP7A1 via the fibroblast growth factor 21 signaling pathway. | Details |