Mechanism of action of the bile acid receptor TGR5 in obesity
Acta Pharmaceutica Sinica B - 2023
Tài liệu tham khảo
2017, Worldwide trends in body-mass index, underweight, overweight, and obesity from 1975 to 2016: a pooled analysis of 2416 population-based measurement studies in 128.9 million children, adolescents, and adults, Lancet, 390, 2627, 10.1016/S0140-6736(17)32129-3
Chooi, 2019, The epidemiology of obesity, Metabolism, 92, 6, 10.1016/j.metabol.2018.09.005
Johnson, 2014, CDC National Health Report: leading causes of morbidity and mortality and associated behavioral risk and protective factors—United States, 2005–2013, MMWR Suppl, 63, 3
Locke, 2015, Genetic studies of body mass index yield new insights for obesity biology, Nature, 518, 197, 10.1038/nature14177
Yang, 2017, Complex relationship between obesity and the fat mass and obesity locus, Int J Biol Sci, 13, 615, 10.7150/ijbs.17051
Bhaskaran, 2018, Association of BMI with overall and cause-specific mortality: a population-based cohort study of 3.6 million adults in the UK, Lancet Diabetes Endocrinol, 6, 944, 10.1016/S2213-8587(18)30288-2
Zhong, 2010, TGR5 as a therapeutic target for treating obesity, Curr Top Med Chem, 10, 386, 10.2174/156802610790980576
Ye, 2018, Hypothalamic endoplasmic reticulum stress as a key mediator of obesity-induced leptin resistance, Obes Rev, 19, 770, 10.1111/obr.12673
Chiang, 2019, Bile acids as metabolic regulators and nutrient sensors, Annu Rev Nutr, 39, 175, 10.1146/annurev-nutr-082018-124344
Byrnes, 2022, Therapeutic regulation of autophagy in hepatic metabolism, Acta Pharm Sin B, 12, 33, 10.1016/j.apsb.2021.07.021
Holter, 2020, TGR5 signaling in hepatic metabolic health, Nutrients, 12, 2598, 10.3390/nu12092598
Liu, 2020, Nondigestible oligosaccharides with anti-obesity effects, J Agric Food Chem, 68, 4, 10.1021/acs.jafc.9b06079
Guan, 2022, Bile acid coordinates microbiota homeostasis and systemic immunometabolism in cardiometabolic diseases, Acta Pharm Sin B, 12, 2129, 10.1016/j.apsb.2021.12.011
Chiang, 2020, Bile acid receptors FXR and TGR5 signaling in fatty liver diseases and therapy, Am J Physiol Gastrointest Liver Physiol, 318, G554, 10.1152/ajpgi.00223.2019
Chávez-Talavera, 2017, Bile acid control of metabolism and inflammation in obesity, type 2 diabetes, dyslipidemia, and nonalcoholic fatty liver disease, Gastroenterology, 152, 1679, 10.1053/j.gastro.2017.01.055
Gou, 2023, Research progress of Takeda G protein-coupled receptor 5 in metabolic syndrome, Molecules, 28, 5870, 10.3390/molecules28155870
Guo, 2016, TGR5, not only a metabolic regulator, Front Physiol, 7, 646, 10.3389/fphys.2016.00646
Maruyama, 2002, Identification of membrane-type receptor for bile acids (M-BAR), Biochem Biophys Res Commun, 298, 714, 10.1016/S0006-291X(02)02550-0
Keitel, 2012, Perspective: TGR5 (Gpbar-1) in liver physiology and disease, Clin Res Hepatol Gastroenterol, 36, 412, 10.1016/j.clinre.2012.03.008
Stepanov, 2013, The bile acid membrane receptor TGR5: a novel pharmacological target in metabolic, inflammatory and neoplastic disorders, J Recept Signal Transduct Res, 33, 213, 10.3109/10799893.2013.802805
Velazquez-Villegas, 2018, TGR5 signalling promotes mitochondrial fission and beige remodelling of white adipose tissue, Nat Commun, 9, 245, 10.1038/s41467-017-02068-0
Schoeler, 2019, Dietary lipids, gut microbiota and lipid metabolism, Rev Endocr Metab Disord, 20, 461, 10.1007/s11154-019-09512-0
Han, 2020, Grape extract activates brown adipose tissue through pathway involving the regulation of gut microbiota and bile acid, Mol Nutr Food Res, 64, 10.1002/mnfr.202000149
Finn, 2019, Intestinal TGR5 agonism improves hepatic steatosis and insulin sensitivity in Western diet-fed mice, Am J Physiol Gastrointest Liver Physiol, 316, G412, 10.1152/ajpgi.00300.2018
Yuan, 2015, Bile acid receptors and nonalcoholic fatty liver disease, World J Hepatol, 7, 2811, 10.4254/wjh.v7.i28.2811
Yang, 2017, Plasma membrane-bound G protein-coupled bile acid receptor attenuates liver ischemia/reperfusion injury via the inhibition of toll-like receptor 4 signaling in mice, Liver Transpl, 23, 63, 10.1002/lt.24628
Ciesielska, 2021, TLR4 and CD14 trafficking and its influence on LPS-induced pro-inflammatory signaling, Cell Mol Life Sci, 78, 1233, 10.1007/s00018-020-03656-y
Sorrentino, 2020, Bile acids signal via TGR5 to activate intestinal stem cells and epithelial regeneration, Gastroenterology, 159, 956, 10.1053/j.gastro.2020.05.067
Sinha, 2020, Dysbiosis-induced secondary bile acid deficiency promotes intestinal inflammation, Cell Host Microbe, 27, 10.1016/j.chom.2020.01.021
Keitel, 2015, TGR5: pathogenetic role and/or therapeutic target in fibrosing cholangitis?, Clin Rev Allergy Immunol, 48, 218, 10.1007/s12016-014-8443-x
Chen, 2020, Cryo-EM structure of activated bile acids receptor TGR5 in complex with stimulatory G protein, Signal Transduct Target Ther, 5, 142, 10.1038/s41392-020-00262-z
Ma, 2022, Structural basis and molecular mechanism of biased GPBAR signaling in regulating NSCLC cell growth via YAP activity, Proc Natl Acad Sci U S A, 119, 10.1073/pnas.2117054119
Yang, 2020, Structural basis of GPBAR activation and bile acid recognition, Nature, 587, 499, 10.1038/s41586-020-2569-1
Chiang, 2018, Bile acid metabolism in liver pathobiology, Gene Expr, 18, 71, 10.3727/105221618X15156018385515
Vaz, 2017, Bile acid analysis in human disorders of bile acid biosynthesis, Mol Aspects Med, 56, 10, 10.1016/j.mam.2017.03.003
Liu, 2018, 25-Hydroxycholesterol activates the expression of cholesterol 25-hydroxylase in an LXR-dependent mechanism, J Lipid Res, 59, 439, 10.1194/jlr.M080440
Pikuleva, 1998, Activities of recombinant human cytochrome P450c27 (CYP27) which produce intermediates of alternative bile acid biosynthetic pathways, J Biol Chem, 273, 18153, 10.1074/jbc.273.29.18153
Fuchs, 2003, Bile acid regulation of hepatic physiology: III. Regulation of bile acid synthesis: past progress and future challenges, Am J Physiol Gastrointest Liver Physiol, 284, G551, 10.1152/ajpgi.00468.2002
Evangelakos, 2021, Role of bile acids in inflammatory liver diseases, Semin Immunopathol, 43, 577, 10.1007/s00281-021-00869-6
Li-Hawkins, 2002, Cholic acid mediates negative feedback regulation of bile acid synthesis in mice, J Clin Invest, 110, 1191, 10.1172/JCI0216309
Chiang, 2013, Bile acid metabolism and signaling, Compr Physiol, 3, 1191, 10.1002/cphy.c120023
Ticho, 2019, Intestinal absorption of bile acids in health and disease, Compr Physiol, 10, 21, 10.1002/cphy.c190007
Dawson, 2017, Roles of ileal ASBT and OSTα-OSTβ in regulating bile acid signaling, Dig Dis, 35, 261, 10.1159/000450987
de Aguiar Vallim, 2013, Pleiotropic roles of bile acids in metabolism, Cell Metab, 17, 657, 10.1016/j.cmet.2013.03.013
Kawamata, 2003, A G protein-coupled receptor responsive to bile acids, J Biol Chem, 278, 9435, 10.1074/jbc.M209706200
Pols, 2011, The bile acid membrane receptor TGR5: a valuable metabolic target, Dig Dis, 29, 37, 10.1159/000324126
Perino, 2021, Molecular physiology of bile acid signaling in health, disease, and aging, Physiol Rev, 101, 683, 10.1152/physrev.00049.2019
Sato, 2008, Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure–activity relationships, and molecular modeling studies, J Med Chem, 51, 1831, 10.1021/jm7015864
Hsu, 2021, TGR5 expression is associated with changes in the heart and urinary bladder of rats with metabolic syndrome, Life (Basel), 11, 695
Chen, 2017, Chenodeoxycholic acid attenuates high-fat diet-induced obesity and hyperglycemia via the G protein-coupled bile acid receptor 1 and proliferator-activated receptor gamma pathway, Exp Ther Med, 14, 5305
Chaudhari, 2021, Bariatric surgery reveals a gut-restricted TGR5 agonist with anti-diabetic effects, Nat Chem Biol, 17, 20, 10.1038/s41589-020-0604-z
Perino, 2015, TGR5 and Immunometabolism: insights from physiology and pharmacology, Trends Pharmacol Sci, 36, 847, 10.1016/j.tips.2015.08.002
Newman, 2007, Natural products as sources of new drugs over the last 25 years, J Nat Prod, 70, 461, 10.1021/np068054v
Genet, 2010, Structure–activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes, J Med Chem, 53, 178, 10.1021/jm900872z
Sato, 2007, Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea, Biochem Biophys Res Commun, 362, 793, 10.1016/j.bbrc.2007.06.130
Ladurner, 2017, Allspice and clove as source of triterpene acids activating the g protein-coupled bile acid receptor TGR5, Front Pharmacol, 8, 468, 10.3389/fphar.2017.00468
Lo, 2016, Development of betulinic acid as an agonist of TGR5 receptor using a new in vitro assay, Drug Des Devel Ther, 10, 2669, 10.2147/DDDT.S113197
Pellicciari, 2009, Discovery of 6α-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity, J Med Chem, 52, 7958, 10.1021/jm901390p
Qian, 2022, Discovery of novel cholic acid derivatives as highly potent agonists for G protein-coupled bile acid receptor, Bioorg Chem, 120, 10.1016/j.bioorg.2021.105588
Huang, 2019, TGR5 agonist ameliorates insulin resistance in the skeletal muscles and improves glucose homeostasis in diabetic mice, Metabolism, 99, 45, 10.1016/j.metabol.2019.07.003
Duan, 2012, Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists, J Med Chem, 55, 10475, 10.1021/jm301071h
Yu, 2015, Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled bile acid receptor 1 (GP-BAR1, TGR5) agonists, Bioorg Med Chem, 23, 1613, 10.1016/j.bmc.2015.01.048
Cerra, 2022, Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): process optimization, synthesis and characterization of metabolites, Eur J Med Chem, 242, 10.1016/j.ejmech.2022.114652
Dehmlow, 2013, Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists, Bioorg Med Chem Lett, 23, 4627, 10.1016/j.bmcl.2013.06.017
Agarwal, 2018, Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes, Bioorg Med Chem Lett, 28, 1849, 10.1016/j.bmcl.2018.04.011
Terui, 2021, Development of selective TGR5 ligands based on the 5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene skeleton, ChemMedChem, 16, 458, 10.1002/cmdc.202000567
Halkias, 2021, Marine bile natural products as agonists of the TGR5 receptor, J Nat Prod, 84, 1507, 10.1021/acs.jnatprod.0c01327
Yang, 2023, TGR5 agonist inhibits intestinal epithelial cell apoptosis via cAMP/PKA/c-FLIP/JNK signaling pathway and ameliorates dextran sulfate sodium-induced ulcerative colitis, Acta Pharmacol Sin, 44, 1649, 10.1038/s41401-023-01081-y
Joshi, 2020, Practical and efficient synthesis of 2-thio-imidazole derivative—ZY12201: a potent TGR5 agonist, Org Process Res Dev, 24, 1508, 10.1021/acs.oprd.0c00234
Gupta, 2022, Pregnane-oximino-alkyl-amino-ether compound as a novel class of TGR5 receptor agonist exhibiting antidiabetic and anti-dyslipidemic activities, Pharmacology, 107, 54, 10.1159/000519721
Biagioli, 2022, Combinatorial targeting of G-protein-coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug-induced liver injury, Hepatology, 78, 26, 10.1002/hep.32787
Zhao, 2021, Ligand-based pharmacophore modeling, virtual screening and biological evaluation to identify novel TGR5 agonists, RSC Adv, 11, 9403, 10.1039/D0RA10168K
Ure, 2022, Synthesis of 12β-methyl-18-nor-avicholic acid analogues as potential TGR5 agonists, Org Biomol Chem, 20, 3511, 10.1039/D1OB02401A
Zhao, 2022, Design, synthesis and evaluation of 3-phenoxypyrazine-2-carboxamide derivatives as potent TGR5 agonists, RSC Adv, 12, 3618, 10.1039/D1RA08867J
Zhao, 2021, Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists, Bioorg Med Chem, 32, 10.1016/j.bmc.2020.115972
Li, 2019, Dual targeting of bile acid receptor-1 (TGR5) and farnesoid X receptor (FXR) prevents estrogen-dependent bone loss in mice, J Bone Miner Res, 34, 765, 10.1002/jbmr.3652
Tang, 2021, Role of betulinic acid derivative SH-479 in triple negative breast cancer and bone microenvironment, Oncol Lett, 22, 605, 10.3892/ol.2021.12866
Nakhi, 2019, 7-Methylation of chenodeoxycholic acid derivatives yields a substantial increase in TGR5 receptor potency, J Med Chem, 62, 6824, 10.1021/acs.jmedchem.9b00770
Yun, 2021, Identification of betulinic acid derivatives as potent TGR5 agonists with antidiabetic effects via humanized TGR5(H88Y) mutant mice, J Med Chem, 64, 12181, 10.1021/acs.jmedchem.1c00851
Han, 2020, Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects, Eur J Med Chem, 203, 10.1016/j.ejmech.2020.112619
Hoguet, 2021, Beyond the rule of 5: impact of PEGylation with various polymer sizes on pharmacokinetic properties, structure–properties relationships of mPEGylated small agonists of TGR5 receptor, J Med Chem, 64, 1593, 10.1021/acs.jmedchem.0c01774
Chen, 2018, Design of gut-restricted thiazolidine agonists of G protein-coupled bile acid receptor 1 (GPBAR1, TGR5), J Med Chem, 61, 7589, 10.1021/acs.jmedchem.8b00308
Luxenburger, 2023, The discovery of 12β-methyl-17-epi-18-nor-bile acids as potent and selective TGR5 agonists, Eur J Med Chem, 250, 10.1016/j.ejmech.2023.115143
Fiorucci, 2022, Discovery of a potent and orally active dual GPBAR1/CysLT1R modulator for the treatment of metabolic fatty liver disease, Front Pharmacol, 13, 10.3389/fphar.2022.858137
Kirchweger, 2018, In silico workflow for the discovery of natural products activating the G protein-coupled bile acid receptor 1, Front Chem, 6, 242, 10.3389/fchem.2018.00242
Liu, 2019, Small molecules for fat combustion: targeting obesity, Acta Pharm Sin B, 9, 220, 10.1016/j.apsb.2018.09.007
Cypess, 2010, Brown fat as a therapy for obesity and diabetes, Curr Opin Endocrinol Diabetes Obes, 17, 143, 10.1097/MED.0b013e328337a81f
Zhang, 2021, Non-shivering thermogenesis signalling regulation and potential therapeutic applications of brown adipose tissue, Int J Biol Sci, 17, 2853, 10.7150/ijbs.60354
Cypess, 2009, Identification and importance of brown adipose tissue in adult humans, N Engl J Med, 360, 1509, 10.1056/NEJMoa0810780
Saito, 2020, Brown adipose tissue, diet-induced thermogenesis, and thermogenic food ingredients: from mice to men, Front Endocrinol (Lausanne), 11, 222, 10.3389/fendo.2020.00222
Shamsi, 2021, The evolving view of thermogenic adipocytes—ontogeny, niche and function, Nat Rev Endocrinol, 17, 726, 10.1038/s41574-021-00562-6
Rial-Pensado, 2022, Temperature modulates systemic and central actions of thyroid hormones on BAT thermogenesis, Front Physiol, 13, 10.3389/fphys.2022.1017381
Schroeder, 2014, Thyroid hormones, T3 AND T4, in the brain, Front Endocrinol (Lausanne), 5, 40, 10.3389/fendo.2014.00040
Mullur, 2014, Thyroid hormone regulation of metabolism, Physiol Rev, 94, 355, 10.1152/physrev.00030.2013
Yau, 2019, Thyroid hormone (T3) stimulates brown adipose tissue activation via mitochondrial biogenesis and MTOR-mediated mitophagy, Autophagy, 15, 131, 10.1080/15548627.2018.1511263
Zekri, 2022, Brown adipocytes local response to thyroid hormone is required for adaptive thermogenesis in adult male mice, Elife, 11, 10.7554/eLife.81996
Bianco, 2013, The role of thyroid hormone and brown adipose tissue in energy homoeostasis, Lancet Diabetes Endocrinol, 1, 250, 10.1016/S2213-8587(13)70069-X
Santillo, 2013, Triiodothyronine induces lipid oxidation and mitochondrial biogenesis in rat Harderian gland, J Endocrinol, 219, 69, 10.1530/JOE-13-0127
Watanabe, 2006, Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation, Nature, 439, 484, 10.1038/nature04330
Qi, 2019, The structure of a membrane adenylyl cyclase bound to an activated stimulatory G protein, Science, 364, 389, 10.1126/science.aav0778
Ould Amer, 2018, Mitochondrial cAMP–PKA signaling: what do we really know?, Biochim Biophys Acta Bioenerg, 1859, 868, 10.1016/j.bbabio.2018.04.005
Hu, 2021, INT-777 attenuates NLRP3-ASC inflammasome-mediated neuroinflammation via TGR5/cAMP/PKA signaling pathway after subarachnoid hemorrhage in rats, Brain Behav Immun, 91, 587, 10.1016/j.bbi.2020.09.016
London, 2022, The regulation of PKA signaling in obesity and in the maintenance of metabolic health, Pharmacol Ther, 237, 10.1016/j.pharmthera.2022.108113
Imai, 2001, Type 2 iodothyronine deiodinase expression is upregulated by the protein kinase A-dependent pathway and is downregulated by the protein kinase C-dependent pathway in cultured human thyroid cells, Thyroid, 11, 899, 10.1089/105072501753210957
Kohrle, 2022, Deiodinases control local cellular and systemic thyroid hormone availability, Free Radic Biol Med, 193, 59, 10.1016/j.freeradbiomed.2022.09.024
Fonseca, 2014, Tissue-specific inactivation of type 2 deiodinase reveals multilevel control of fatty acid oxidation by thyroid hormone in the mouse, Diabetes, 63, 1594, 10.2337/db13-1768
Bianco, 2006, Deiodinases: implications of the local control of thyroid hormone action, J Clin Invest, 116, 2571, 10.1172/JCI29812
Russo, 2021, Deiodinases and the metabolic code for thyroid hormone action, Endocrinology, 162, bqab059, 10.1210/endocr/bqab059
Giralt, 2013, White, brown, beige/brite: different adipose cells for different functions?, Endocrinology, 154, 2992, 10.1210/en.2013-1403
Wu, 2012, Beige adipocytes are a distinct type of thermogenic fat cell in mouse and human, Cell, 150, 366, 10.1016/j.cell.2012.05.016
Fan, 2020, Cold-inducible Klf9 regulates thermogenesis of brown and beige fat, Diabetes, 69, 2603, 10.2337/db19-1153
Casaburi, 2012, Chenodeoxycholic acid through a TGR5-dependent CREB signaling activation enhances cyclin D1 expression and promotes human endometrial cancer cell proliferation, Cell Cycle, 11, 2699, 10.4161/cc.21029
Qi, 2020, Taurochenodeoxycholic acid mediates cAMP–PKA–CREB signaling pathway, Chin J Nat Med, 18, 898
Song, 2020, Creb–Pgc1α pathway modulates the interaction between lipid droplets and mitochondria and influences high fat diet-induced changes of lipid metabolism in the liver and isolated hepatocytes of yellow catfish, J Nutr Biochem, 80, 10.1016/j.jnutbio.2020.108364
Zhao, 2018, Activation of TGR5 promotes mitochondrial biogenesis in human aortic endothelial cells, Biochem Biophys Res Commun, 500, 952, 10.1016/j.bbrc.2018.04.210
Wu, 2021, Intestinal hypoxia-inducible factor 2alpha regulates lactate levels to shape the gut microbiome and alter thermogenesis, Cell Metab, 33, 1988, 10.1016/j.cmet.2021.07.007
Bertholet, 2017, Mitochondrial patch clamp of beige adipocytes reveals UCP1-positive and UCP1-negative cells both exhibiting futile creatine cycling, Cell Metab, 25, 811, 10.1016/j.cmet.2017.03.002
Kazak, 2015, A creatine-driven substrate cycle enhances energy expenditure and thermogenesis in beige fat, Cell, 163, 643, 10.1016/j.cell.2015.09.035
Dieni, 2009, Creatine kinase regulation by reversible phosphorylation in frog muscle, Comp Biochem Physiol B Biochem Mol Biol, 152, 405, 10.1016/j.cbpb.2009.01.012
Bak, 2013, Tissue specific phosphorylation of mitochondrial proteins isolated from rat liver, heart muscle, and skeletal muscle, J Proteome Res, 12, 4327, 10.1021/pr400281r
Sun, 2021, Mitochondrial TNAP controls thermogenesis by hydrolysis of phosphocreatine, Nature, 593, 580, 10.1038/s41586-021-03533-z
Rahbani, 2022, ADRA1A-Gαq signalling potentiates adipocyte thermogenesis through CKB and TNAP, Nat Metab, 4, 1459, 10.1038/s42255-022-00667-w
Esteves, 2021, Crucial role of fatty acid oxidation in asthmatic bronchial smooth muscle remodelling, Eur Respir J, 58, 10.1183/13993003.04252-2020
Turchi, 2020, Frataxin deficiency induces lipid accumulation and affects thermogenesis in brown adipose tissue, Cell Death Dis, 11, 51, 10.1038/s41419-020-2253-2
Ding, 2021, Notoginsenoside Ft1 acts as a TGR5 agonist but FXR antagonist to alleviate high fat diet-induced obesity and insulin resistance in mice, Acta Pharm Sin B, 11, 1541, 10.1016/j.apsb.2021.03.038
Recazens, 2021, Hormone-sensitive lipase: sixty years later, Prog Lipid Res, 82, 10.1016/j.plipres.2020.101084
Clapham, 2012, Central control of thermogenesis, Neuropharmacology, 63, 111, 10.1016/j.neuropharm.2011.10.014
Keitel, 2010, The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain, Glia, 58, 1794, 10.1002/glia.21049
Parry, 2010, Safety, tolerability, and cerebrospinal fluid penetration of ursodeoxycholic acid in patients with amyotrophic lateral sclerosis, Clin Neuropharmacol, 33, 17, 10.1097/WNF.0b013e3181c47569
Fénelon, 2022, Hypothalamic bile acid–TGR5 signaling: a therapeutic target in the fight against obesity?, Med Sci (Paris), 38, 413, 10.1051/medsci/2022052
Waterson, 2015, Neuronal regulation of energy homeostasis: beyond the hypothalamus and feeding, Cell Metab, 22, 962, 10.1016/j.cmet.2015.09.026
Perino, 2021, Central anorexigenic actions of bile acids are mediated by TGR5, Nat Metab, 3, 595, 10.1038/s42255-021-00398-4
Schone, 2012, Glutamate and GABA as rapid effectors of hypothalamic “peptidergic” neurons, Front Behav Neurosci, 6, 81, 10.3389/fnbeh.2012.00081
Meunier, 2016, Captivating new roles of F-actin cortex in exocytosis and bulk endocytosis in neurosecretory cells, Trends Neurosci, 39, 605, 10.1016/j.tins.2016.07.003
Sit, 2011, Rho GTPases and their role in organizing the actin cytoskeleton, J Cell Sci, 124, 679, 10.1242/jcs.064964
Kuhre, 2018, Bile acids are important direct and indirect regulators of the secretion of appetite- and metabolism-regulating hormones from the gut and pancreas, Mol Metab, 11, 84, 10.1016/j.molmet.2018.03.007
Dong, 2021, Time and metabolic state-dependent effects of GLP-1R agonists on NPY/AgRP and POMC neuronal activity in vivo, Mol Metab, 54, 10.1016/j.molmet.2021.101352
Schalla, 2021, Neuroendocrine peptides of the gut and their role in the regulation of food intake, Compr Physiol, 11, 1679, 10.1002/cphy.c200007
Roh, 2023, Hormonal gut–brain signaling for the treatment of obesity, Int J Mol Sci, 24, 3384, 10.3390/ijms24043384
Pizarroso, 2021, A review on the role of food-derived bioactive molecules and the microbiota–gut–brain axis in satiety regulation, Nutrients, 13, 632, 10.3390/nu13020632
Akhlaghi, 2022, The role of dietary fibers in regulating appetite, an overview of mechanisms and weight consequences, Crit Rev Food Sci Nutr, 1, 10.1080/10408398.2022.2130160
Weatherford, 1993, CCK satiety is differentially mediated by high- and low-affinity CCK receptors in mice and rats, Am J Physiol, 264, R244
Wu, 2020, Satiety induced by bile acids is mediated via vagal afferent pathways, JCI Insight, 5, 10.1172/jci.insight.132400
Malone, 2019, Does obesity cause type 2 diabetes mellitus (T2DM)? Or is it the opposite?, Pediatr Diabetes, 20, 5, 10.1111/pedi.12787
Deng, 2020, Chitosan oligosaccharide ameliorated obesity by reducing endoplasmic reticulum stress in diet-induced obese rats, Food Funct, 11, 6285, 10.1039/D0FO01107J
Drucker, 2006, The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes, Lancet, 368, 1696, 10.1016/S0140-6736(06)69705-5
Drucker, 2017, Discovery, characterization, and clinical development of the glucagon-like peptides, J Clin Invest, 127, 4217, 10.1172/JCI97233
Fu, 2016, Natural products with anti-obesity effects and different mechanisms of action, J Agric Food Chem, 64, 9571, 10.1021/acs.jafc.6b04468
Jiang, 2021, Ginsenoside Ro ameliorates high-fat diet-induced obesity and insulin resistance in mice via activation of the g protein-coupled bile acid receptor 5 pathway, J Pharmacol Exp Ther, 377, 441, 10.1124/jpet.120.000435
Yang, 2021, Finger citron extract ameliorates glycolipid metabolism and inflammation by regulating GLP-1 secretion via TGR5 receptors in obese rats, Evid Based Complement Alternat Med, 2021
Ding, 2016, Vertical sleeve gastrectomy activates GPBAR-1/TGR5 to sustain weight loss, improve fatty liver, and remit insulin resistance in mice, Hepatology, 64, 760, 10.1002/hep.28689
Ono, 2011, Anti-obesity and anti-hyperglycemic effects of the dietary citrus limonoid nomilin in mice fed a high-fat diet, Biochem Biophys Res Commun, 410, 677, 10.1016/j.bbrc.2011.06.055
Chaudhari, 2021, A microbial metabolite remodels the gut–liver axis following bariatric surgery, Cell Host Microbe, 29, 408, 10.1016/j.chom.2020.12.004
Trabelsi, 2015, Farnesoid X receptor inhibits glucagon-like peptide-1 production by enteroendocrine L cells, Nat Commun, 6, 7629, 10.1038/ncomms8629
Ducastel, 2020, The nuclear receptor FXR inhibits glucagon-like peptide-1 secretion in response to microbiota-derived short-chain fatty acids, Sci Rep, 10, 174, 10.1038/s41598-019-56743-x
Kim, 2018, Crosstalk between FXR and TGR5 controls glucagon-like peptide 1 secretion to maintain glycemic homeostasis, Lab Anim Res, 34, 140, 10.5625/lar.2018.34.4.140
Pathak, 2018, Intestine farnesoid X receptor agonist and the gut microbiota activate G-protein bile acid receptor-1 signaling to improve metabolism, Hepatology, 68, 1574, 10.1002/hep.29857
Bronden, 2020, Gluco-metabolic effects of pharmacotherapy-induced modulation of bile acid physiology, J Clin Endocrinol Metab, 105, dgz025, 10.1210/clinem/dgz025
Comeglio, 2018, INT-767 prevents NASH and promotes visceral fat brown adipogenesis and mitochondrial function, J Endocrinol, 238, 107, 10.1530/JOE-17-0557
Vettorazzi, 2016, The bile acid TUDCA increases glucose-induced insulin secretion via the cAMP/PKA pathway in pancreatic beta cells, Metabolism, 65, 54, 10.1016/j.metabol.2015.10.021
Kumar, 2016, Activation of transmembrane bile acid receptor TGR5 modulates pancreatic islet alpha cells to promote glucose homeostasis, J Biol Chem, 291, 6626, 10.1074/jbc.M115.699504
Huang, 2018, The PI3K/AKT pathway in obesity and type 2 diabetes, Int J Biol Sci, 14, 1483, 10.7150/ijbs.27173
Kahn, 2006, Mechanisms linking obesity to insulin resistance and type 2 diabetes, Nature, 444, 840, 10.1038/nature05482
Gai, 2019, Lipid accumulation and chronic kidney disease, Nutrients, 11, 722, 10.3390/nu11040722
Tamai, 2022, Association of lithocholic acid with skeletal muscle hypertrophy through TGR5-IGF-1 and skeletal muscle mass in cultured mouse myotubes, chronic liver disease rats and humans, Elife, 11, 10.7554/eLife.80638
Mikami, 2021, Olive leaf extract prevents obesity, cognitive decline, and depression and improves exercise capacity in mice, Sci Rep, 11, 10.1038/s41598-021-90589-6
Sasaki, 2021, Muscle-specific TGR5 overexpression improves glucose clearance in glucose-intolerant mice, J Biol Chem, 296, 10.1074/jbc.RA120.016203
Wei, 2023, G protein-coupled receptor 35 attenuates nonalcoholic steatohepatitis by reprogramming cholesterol homeostasis in hepatocytes, Acta Pharm Sin B, 13, 1128, 10.1016/j.apsb.2022.10.011
Jeon, 2019, GLP-1 improves palmitate-induced insulin resistance in human skeletal muscle via SIRT1 activity, Int J Mol Med, 44, 1161
Wu, 2022, GLP-1 regulates exercise endurance and skeletal muscle remodeling via GLP-1R/AMPK pathway, Biochim Biophys Acta Mol Cell Res, 1869, 10.1016/j.bbamcr.2022.119300
Andreozzi, 2016, The GLP-1 receptor agonists exenatide and liraglutide activate glucose transport by an AMPK-dependent mechanism, J Transl Med, 14, 229, 10.1186/s12967-016-0985-7
Tian, 2023, GLP-1 receptor agonist protects palmitate-induced insulin resistance in skeletal muscle cells by up-regulating sestrin2 to promote autophagy, Sci Rep, 13, 9446, 10.1038/s41598-023-36602-6
Lee, 2012, Glucagon-like peptide-1 inhibits adipose tissue macrophage infiltration and inflammation in an obese mouse model of diabetes, Diabetologia, 55, 2456, 10.1007/s00125-012-2592-3
Zhou, 2021, TGR5/Cathepsin E signaling regulates macrophage innate immune activation in liver ischemia and reperfusion injury, Am J Transplant, 21, 1453, 10.1111/ajt.16327
Guo, 2016, Glucagon-like peptide 1 improves insulin resistance in vitro through anti-inflammation of macrophages, Braz J Med Biol Res, 49, 10.1590/1414-431x20165826
Zhuo, 2023, Genome editing of PAR2 through targeted delivery of CRISPR-Cas9 system for alleviating acute lung inflammation via ERK/NLRP3/IL-1β and NO/iNOS signalling, Acta Pharm Sin B
Yang, 2021, TGR5 protects against cholestatic liver disease via suppressing the NF-κB pathway and activating the Nrf2/HO-1 pathway, Ann Transl Med, 9, 1158, 10.21037/atm-21-2631
Biagioli, 2017, The bile acid receptor GPBAR1 regulates the M1/M2 phenotype of intestinal macrophages and activation of GPBAR1 rescues mice from murine colitis, J Immunol, 199, 718, 10.4049/jimmunol.1700183
Shi, 2020, TGR5 regulates macrophage inflammation in nonalcoholic steatohepatitis by modulating NLRP3 inflammasome activation, Front Immunol, 11
Guo, 2016, Bile acids control inflammation and metabolic disorder through inhibition of NLRP3 inflammasome, Immunity, 45, 802, 10.1016/j.immuni.2016.09.008
Yoneno, 2013, TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease, Immunology, 139, 19, 10.1111/imm.12045
Zhao, 2022, TGR5 deficiency activates antitumor immunity in non-small cell lung cancer via restraining M2 macrophage polarization, Acta Pharm Sin B, 12, 787, 10.1016/j.apsb.2021.07.011
Perino, 2014, TGR5 reduces macrophage migration through mTOR-induced C/EBPbeta differential translation, J Clin Invest, 124, 5424, 10.1172/JCI76289
Wang, 2011, The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor kappa light-chain enhancer of activated B cells (NF-κB) in mice, Hepatology, 54, 1421, 10.1002/hep.24525
Sharma, 2018, Recent updates on GLP-1 agonists: current advancements & challenges, Biomed Pharmacother, 108, 952, 10.1016/j.biopha.2018.08.088
Yu, 2019, Liraglutide ameliorates non-alcoholic steatohepatitis by inhibiting NLRP3 inflammasome and pyroptosis activation via mitophagy, Eur J Pharmacol, 864, 10.1016/j.ejphar.2019.172715
Han, 2020, Liraglutide ameliorates obesity-related nonalcoholic fatty liver disease by regulating Sestrin2-mediated Nrf2/HO-1 pathway, Biochem Biophys Res Commun, 525, 895, 10.1016/j.bbrc.2020.03.032
Loboda, 2016, Role of Nrf2/HO-1 system in development, oxidative stress response and diseases: an evolutionarily conserved mechanism, Cell Mol Life Sci, 73, 3221, 10.1007/s00018-016-2223-0
Soedono, 2021, Adipose tissue dendritic cells: critical regulators of obesity-induced inflammation and insulin resistance, Int J Mol Sci, 22, 8666, 10.3390/ijms22168666
Ichikawa, 2012, Bile acids induce monocyte differentiation toward interleukin-12 hypo-producing dendritic cells via a TGR5-dependent pathway, Immunology, 136, 153, 10.1111/j.1365-2567.2012.03554.x
Hu, 2022, Lithocholic acid inhibits dendritic cell activation by reducing intracellular glutathione via TGR5 signaling, Int J Biol Sci, 18, 4545, 10.7150/ijbs.71287
Hu, 2021, Gut microbiota-mediated secondary bile acids regulate dendritic cells to attenuate autoimmune uveitis through TGR5 signaling, Cell Rep, 36, 10.1016/j.celrep.2021.109726
Biagioli, 2019, GPBAR1 functions as gatekeeper for liver NKT cells and provides counterregulatory signals in mouse models of immune-mediated hepatitis, Cell Mol Gastroenterol Hepatol, 8, 447, 10.1016/j.jcmgh.2019.06.003
Wang, 2022, Roles and mechanisms of TGR5 in the modulation of CD4+ T cell functions in myocardial infarction, J Cardiovasc Transl Res, 15, 350, 10.1007/s12265-021-10164-2
Chao, 2011, Knockdown of NPY expression in the dorsomedial hypothalamus promotes development of brown adipocytes and prevents diet-induced obesity, Cell Metab, 13, 573, 10.1016/j.cmet.2011.02.019
Zhang, 2021, Neuropeptide Y plays an important role in the relationship between brain glucose metabolism and brown adipose tissue activity in healthy adults: a PET/CT study, Front Endocrinol (Lausanne), 12
Xiang, 2021, Effect of different bile acids on the intestine through enterohepatic circulation based on FXR, Gut Microbes, 13, 10.1080/19490976.2021.1949095
Deutschmann, 2018, Bile acid receptors in the biliary tree: TGR5 in physiology and disease, Biochim Biophys Acta Mol Basis Dis, 1864, 1319, 10.1016/j.bbadis.2017.08.021