Table 5.2. Mechanism of regulation of G-protein coupled receptors (GPCRs) and Nuclear hormone receptors (NHRs) by bioactive lipids).
| Gene id | Nomenclature | Tissue | Regulation | Substrate ligand | Protein interaction | Function | ||
|---|---|---|---|---|---|---|---|---|
| FFAR1 | GPR40 | Pancreas | — | C10-C18, TZD | Gq | GSIS secretion | ||
| FFAR2 | GPR43 | Adipose | PPARγ | C2-C5 | Gq,Gi | Inhibit lipolysis | ||
| FFAR3 | GPR41 | Intestine, adipose | — | C2-C4 | Gi | GLP, Leptin secretion | ||
| GPR84 | MT | — | C9-C12 | Gi | IL12-p40 | |||
| GPR119 | Pancreas, intestine | — | LysoPC, 5-HEPE | Gs | GLP-2,PYY secretion | |||
| GPR120 | Colon, adipose | — | C10-C18, PUFA | Gq | GLP-1 secretion | |||
| EP1 | — | |||||||
| EP2 | PGE2 receptor | MT, CNS, T-B | — | PGE2 | Gq | Ca2+↑, CVS, immune | ||
| EP3 | PGE2 receptor | MT, CNS, DC, E, F | — | PGE2 | Gs | cAMP↑, immune | ||
| EP4 | PGE2 receptor | MT, CNS,K, IM | — | PGE2 | GI,G12/13 | cAMP↓, fever | ||
| DP1 | PGE2 receptor | MT, DC, T,CAN | — | PGE2 | Gs,Gi | cAMP↑, inflammation | ||
| DP2 | PGD2 receptor | VSMC, BSMC, P | — | PGD2, PGJ2 | Gs | cAMP↑, intestine | ||
| IP | PGD2 receptor | Th2, MT, IM | — | PGD2, PGJ2 | Gi | cAMP↓,chemotaxis | ||
| FP | PGI2 receptor | VSC, MT, IM | — | PGI2 | Gs,Gq | cAMP↑ | ||
| TP | PGF2 receptor | MT, K, L, IM | — | PGF2α | Gq | Ca2+T | ||
| BLT1 | Thromboxane | MT, IM P, CNS | Sp1,AML1 | TXA2, isoprostanes | Gq | Ca2+T | ||
| BLT2 | LTB4 receptor | Myeloid, spleen | Sp1 | LTB4, 20-LTB4,12-HETE | Gi | Chemotaxis, proliferation | ||
| cysLT1 | LTB4 receptor | Spleen, Liver, | AP-1,GATA | LTB4,12-HETE, 20-LTB4 | Gi | Chemotaxis, proliferation | ||
| LTD4 receptor | myeloid | STAT6 | LTD4 > LTC4 > LTE4 | Gq | SRS-A, inflammation | |||
| cysLT2 | LTC4 receptor | Leukocytes, S,L,I | STAT1,Jak | LTC4 = LTC4 > LTE4 | Gq | SRS-A, inflammation | ||
| ALX/FPR2 | LXA4 receptor | Leukocytes, S,B, heart | — | LXA4, 15epiLXA4,peptides | Gs,i,q | Antiinflammatory | ||
| LPA1-5 | LPA receptor | MT, myeloid MT | — | Lysophosphatidic acid | Gi,Gq,G12/13 | CVS, proliferation | ||
| NR1C1 | PPARα | Liver, kidney | FXRα | LTB4, 8-HETE, EET, EPA, | B-oxidation | |||
| NR1C2 | PPARβ | Muscle | — | DHA, CLA, PL, fibrates | Antiinflammatory | |||
| NR1C2 | PPARγ | C/EBP | 15-keto PGE2, | β-oxidation, antiin-flammatory | ||||
| NR2A1 | HNF4α | Muscle, adipocyte | — | PGI2, 15-HETE,EPA, RA | Adipogenesis | |||
| NR1H3 | LXRα | macrophage | — | 15dPGJ2, 15-HETE, EPA | Antiinflammatory | |||
| NR1H4 | FXRα | Liver, MT | — | 13-HODE, PGF2α,TZD | β-oxidation | |||
| NR5A2 | LRH-1 | Liver | — | Aminosalicylic acid | Antiinflammation | |||
| NR2B1 | RXRα | Liver | — | Linoleic, saturate FA | Cholesterol sensor | |||
| NR1B1 | RARα | Liver | LXRα | Oxysterol | Bile acid sensor | |||
| Gene id | Nomenclature | Tissue | Regulation | Substrate ligand | Protein interaction | Function | ||
| NRA4 | NAR4 | MT | GPCR, | Bile acids | Antiinflammatory | |||
| NROB2 | SHP | MT | TLRs FXRα | Phospholipids | Glucocorticoids | |||
| MT | Cis-retinoic acid, | HNR partner | ||||||
| DHA, | ||||||||
| MT | All-trans retinoic acid Unknown Retinoids? | Differentiation β-adrenergic signal β-oxidation Energy glucose homeostasis | ||||||
AML1, acute myeloid leukemia1; B, basophils; CVS, cardiovascular system; Th2-CRTH2, chemoattractant receptor homologous receptor; CNS, central nervous system; BSM, bronchial smooth muscle; CLA, conjugated linoleic; DC, dendritic cell; E, endothelia; F, fibroblast; GSIS, glucose-stimulated insulin secretion; GLP, glucagon like peptide 1; K, kidney; L, lung; I, intestine; IM, immune cells; M T, multiple tissues; PYY, pancreatic YY peptide; SRSA, slow-reacting substance of anaphylaxis; S, spleen; STAT, signal transducer activator transcription; TZD, thiazolidinedione; TLR, Toll-like receptors.
This table includes receptor's primary tissue of expression, regulation, ligand or substrate activation and primary function in target tissue.