Role of TGR5 (GPBAR1) in Liver Disease

Identification of a nuclear receptor for bile acids

Makishima, M., Okamoto, A. Y., Repa, J. J., Tu, H., Learned, R. M., Luk, A., Hull, M. V., Lustig, K. D., Mangelsdorf, D. J., & Shan, B. (1999) · Science · doi:10.1126/science.284.5418.1362 · Cited by 2,714 · see citing works

Bile Acids: Natural Ligands for an Orphan Nuclear Receptor

Parks, D. J., Blanchard, S. G., Bledsoe, R. K., Chandra, G., Consler, T. G., Kliewer, S. A., Stimmel, J. B., Willson, T. M., Zavacki, A. M., Moore, D. D., et al. (1999) · Science · doi:10.1126/science.284.5418.1365 · Cited by 2,274 · see citing works

Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): A multicentre, randomised, placebo-controlled trial

Neuschwander-Tetri, B. A., Loomba, R., Sanyal, A. J., Lavine, J. E., Van Natta, M. L., Abdelmalek, M. F., Chalasani, N., Dasarathy, S., Diehl, A. M., Hameed, B., et al. (2015) · The Lancet · doi:10.1016/s0140-6736(14)61933-4 · Cited by 2,237 · see citing works

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

Thomas, C., Gioiello, A., Noriega, L., Strehle, A., Oury, J., Rizzo, G., Macchiarulo, A., Yamamoto, H., Mataki, C., Pruzanski, M., et al. (2009) · Cell Metabolism · doi:10.1016/j.cmet.2009.08.001 · Cited by 1,885 · see citing works

Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis

Inagaki, T., Choi, M., Moschetta, A., Peng, L., Cummins, C. L., McDonald, J. G., Luo, G., Jones, S. A., Goodwin, B., Richardson, J. A., et al. (2005) · Cell Metabolism · doi:10.1016/j.cmet.2005.09.001 · Cited by 1,865 · see citing works

Targeted Disruption of the Nuclear Receptor FXR/BAR Impairs Bile Acid and Lipid Homeostasis

Sinal, C. J., Tohkin, M., Miyata, M., Ward, J. M., Lambert, G., & Gonzalez, F. J. (2000) · Cell · doi:10.1016/s0092-8674(00)00062-3 · Cited by 1,819 · see citing works

Endogenous Bile Acids Are Ligands for the Nuclear Receptor FXR/BAR

Wang, H., Chen, J., Hollister, K., Sowers, L. C., & Forman, B. M. (1999) · Molecular Cell · doi:10.1016/s1097-2765(00)80348-2 · Cited by 1,636 · see citing works

A G Protein-coupled Receptor Responsive to Bile Acids

Kawamata, Y., Fujii, R., Hosoya, M., Harada, M., Yoshida, H., Miwa, M., Fukusumi, S., Habata, Y., Itoh, T., Shintani, Y., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m209706200 · Cited by 1,628 · see citing works

The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity

Staudinger, J. L., Goodwin, B. J., Jones, S. A., Hawkins‐Brown, D., MacKenzie, K. I., Latour, A. M., Liu, Y., Klaassen, C. D., Brown, K. K., Reinhard, J. F., et al. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.051551698 · Cited by 1,378 · see citing works

Identification of a nuclear receptor that is activated by farnesol metabolites

Forman, B. M., Goode, E., Chen, J., Oro, A. E., Bradley, D. J., Perlmann, T., Noonan, D. J., Burka, L. T., McMorris, T., Lamph, W. W., et al. (1995) · Cell · doi:10.1016/0092-8674(95)90530-8 · Cited by 1,210 · see citing works

Regulation of antibacterial defense in the small intestine by the nuclear bile acid receptor

Inagaki, T., Moschetta, A., Lee, Y.-K., Peng, L., Zhao, G., Downes, M., Yu, R. T., Shelton, J. M., Richardson, J. A., Repa, J. J., et al. (2006) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0509592103 · Cited by 1,164 · see citing works

A Placebo-Controlled Trial of Obeticholic Acid in Primary Biliary Cholangitis

Nevens, F., Andreone, P., Mazzella, G., Strasser, S. I., Bowlus, C., Invernizzi, P., Drenth, J. P. H., Pockros, P. J., Regula, J., Beuers, U., et al. (2016) · New England Journal of Medicine · doi:10.1056/nejmoa1509840 · Cited by 1,131 · see citing works

Targeting hepatic macrophages to treat liver diseases

Tacke, F. (2017) · Journal of Hepatology · doi:10.1016/j.jhep.2017.02.026 · Cited by 1,003 · see citing works

Identification of membrane-type receptor for bile acids (M-BAR)

Maruyama, T., Miyamoto, Y., Nakamura, T., Tamai, Y., Okada, H., Sugiyama, E., Nakamura, T., Itadani, H., & Tanaka, K. (2002) · Biochemical and Biophysical Research Communications · doi:10.1016/s0006-291x(02)02550-0 · Cited by 993 · see citing works

Bile Acid Control of Metabolism and Inflammation in Obesity, Type 2 Diabetes, Dyslipidemia, and Nonalcoholic Fatty Liver Disease

Chávez-Talavera, O., Tailleux, A., Lefebvre, P., & Staels, B. (2017) · Gastroenterology · doi:10.1053/j.gastro.2017.01.055 · Cited by 970 · see citing works

Bile Acids Control Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome

Guo, C., Xie, S., Chi, Z., Zhang, J., Liu, Y., Zhang, L., Zheng, M., Zhang, X., Xia, D., Ke, Y., et al. (2016) · Immunity · doi:10.1016/j.immuni.2016.09.008 · Cited by 838 · see citing works

Farnesoid X receptor antagonizes nuclear factor κB in hepatic inflammatory response

Wang, Y.-D., Chen, W.-D., Wang, M., Yu, D., Forman, B. M., & Huang, W. (2008) · Hepatology · doi:10.1002/hep.22519 · Cited by 639 · see citing works

FGF19 as a Postprandial, Insulin-Independent Activator of Hepatic Protein and Glycogen Synthesis

Kir, S., Beddow, S. A., Samuel, V. T., Miller, P., Previs, S. F., Suino-Powell, K., Xu, H. E., Shulman, G. I., Kliewer, S. A., & Mangelsdorf, D. J. (2011) · Science · doi:10.1126/science.1198363 · Cited by 637 · see citing works

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

Pols, T. W. H., Nomura, M., Harach, T., Sasso, G. L., Oosterveer, M. H., Thomas, C., Rizzo, G., Gioiello, A., Adorini, L., Pellicciari, R., et al. (2011) · Cell Metabolism · doi:10.1016/j.cmet.2011.11.006 · Cited by 622 · see citing works

Sequence variants in IL10, ARPC2 and multiple other loci contribute to ulcerative colitis susceptibility

the IBSEN study group, Franke, A., Balschun, T. C., Karlsen, T. H., Skiecevičienė, J., Nikolaus, S., Gabriele Mayr, B., Domingues, F. S., Albrecht, M., Nothnagel, M., et al. (2008) · Nature Genetics · doi:10.1038/ng.221 · Cited by 590 · see citing works

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

Wang, Y., Chen, W., Yu, D. D., FORMAN, B. M., & Huang, W. (2011) · Hepatology · doi:10.1002/hep.24525 · Cited by 488 · see citing works

The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation

Pols, T. W. H., Noriega, L. G., Nomura, M., Auwerx, J., & Schoonjans, K. (2011) · Journal of Hepatology · doi:10.1016/j.jhep.2010.12.004 · Cited by 454 · see citing works

NGM282 for treatment of non-alcoholic steatohepatitis: A multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

Harrison, S. A., Rinella, M. E., Abdelmalek, M. F., Trotter, J. F., Paredes, A. H., Arnold, H. L., Kugelmas, M., Bashir, M. R., Jaros, M. J., Ling, L., et al. (2018) · The Lancet · doi:10.1016/s0140-6736(18)30474-4 · Cited by 425 · see citing works

Bile Acids as Hormones: The FXR-FGF15/19 Pathway

Kliewer, S. A., & Mangelsdorf, D. J. (2015) · Digestive Diseases · doi:10.1159/000371670 · Cited by 424 · see citing works

Expression and function of the bile acid receptor TGR5 in Kupffer cells

Keitel, V., Donner, M., Winandy, S., Kubitz, R., & Häussinger, D. (2008) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2008.04.171 · Cited by 418 · see citing works

The TGR5 receptor mediates bile acid–induced itch and analgesia

Alemi, F., Kwon, E., Poole, D. P., Lieu, T., Lyo, V., Cattaruzza, F., Cevikbas, F., Steinhoff, M. S., Nassini, R., Materazzi, S., et al. (2013) · Journal of Clinical Investigation · doi:10.1172/jci64551 · Cited by 380 · see citing works

Genome-Wide Association Analysis in Primary Sclerosing Cholangitis

Karlsen, T. H., Franke, A., Melum, E., Kaser, A., Hov, J. R., Balschun, T. C., Lie, B. A., Bergquist, A. M., Schramm, C., Weismüller, T. J., et al. (2009) · Gastroenterology · doi:10.1053/j.gastro.2009.11.046 · Cited by 360 · see citing works

The Biliary HCO3 − Umbrella: A Unifying Hypothesis on Pathogenetic and Therapeutic Aspects of Fibrosing Cholangiopathies

Beuers, U., Hohenester, S., de Buy Wenniger, L. J. M., Kremer, A. E., Jansen, P. L. M., & Elferink, R. P. J. O. (2010) · Hepatology · doi:10.1002/hep.23810 · Cited by 351 · see citing works

Conjugated Bile Acids Activate the Sphingosine–1–Phosphate Receptor 2 in Primary Rodent Hepatocytes

Studer, E. J., Zhou, X., Zhao, R., Wang, Y., Takabe, K., Nagahashi, M., Pandak, W. M., Dent, P., Spiegel, S., Shi, R., et al. (2011) · Hepatology · doi:10.1002/hep.24681 · Cited by 319 · see citing works

Vascular pathobiology in chronic liver disease and cirrhosis – Current status and future directions

Iwakiri, Y., Shah, V. H., & Rockey, D. C. (2014) · Journal of Hepatology · doi:10.1016/j.jhep.2014.05.047 · Cited by 312 · see citing works

Vascular endothelial dysfunction in cirrhosis

Iwakiri, Y., & Groszmann, R. J. (2007) · Journal of Hepatology · doi:10.1016/j.jhep.2007.02.006 · Cited by 310 · see citing works

The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells

Keitel, V., Reinehr, R., Gatsios, P., Rupprecht, C., Görg, B., Selbach, O., Häussinger, D., & Kubitz, R. (2007) · Hepatology · doi:10.1002/hep.21458 · Cited by 308 · see citing works

Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure−Activity Relationships, and Molecular Modeling Studies

Sato, H., Macchiarulo, A., Thomas, C., Gioiello, A., Une, M., Hofmann, A. F., Saladin, R., Schoonjans, K., Pellicciari, R., & Auwerx, J. H. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm7015864 · Cited by 302 · see citing works

Deciphering the nuclear bile acid receptor FXR paradigm

Modica, S., Gadaleta, R. M., & Moschetta, A. (2010) · Nuclear Receptor Signaling · doi:10.1621/nrs.08005 · Cited by 292 · see citing works

Identification of a hormonal basis for gallbladder filling

Choi, M., Moschetta, A., Bookout, A., Peng, L., Umetani, M., Holmstrom, S. R., Suino-Powell, K., Xu, H. E., Richardson, J., Gerard, R., et al. (2006) · Nature Medicine · doi:10.1038/nm1501 · Cited by 289 · see citing works

Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice

Maruyama, T., Tanaka, K., Suzuki, J., Miyoshi, H., Harada, N., Nakamura, T., Miyamoto, Y., Kanatani, A., & Tamai, Y. (2006) · Journal of Endocrinology · doi:10.1677/joe.1.06546 · Cited by 285 · see citing works

The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders #

Keitel, V., Cupisti, K., Ullmer, C., Knoefel, W. T., Kubitz, R., & Häussinger, D. (2009) · Hepatology · doi:10.1002/hep.23032 · Cited by 285 · see citing works

Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation

Vassileva, G., Golovko, A., Markowitz, L., Abbondanzo, S. J., Zeng, M., Yang, S., Hoos, L. M., Tetzloff, G. G., Levitan, D. J., Murgolo, N., et al. (2006) · Biochemical Journal · doi:10.1042/bj20060537 · Cited by 277 · see citing works

The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain

Keitel, V., Görg, B., Bidmon, H. J., Zemtsova, I., Spomer, L., Zilles, K., & Häussinger, D. (2010) · Glia · doi:10.1002/glia.21049 · Cited by 274 · see citing works

The G Protein-Coupled Bile Acid Receptor, TGR5, Stimulates Gallbladder Filling

Li, T., Holmstrom, S. R., Kır, S., Umetani, M., Schmidt, D. R., Kliewer, S. A., & Mangelsdorf, D. J. (2011) · Molecular Endocrinology · doi:10.1210/me.2010-0460 · Cited by 267 · see citing works

The normal liver harbors the vitamin D nuclear receptor in nonparenchymal and biliary epithelial cells

Gascon-Barré, M., Demers, C., Mirshahi, A., Néron, S., Zalzal, S., & Nanci, A. (2003) · Hepatology · doi:10.1053/jhep.2003.50176 · Cited by 254 · see citing works

Pharmacology of bile acid receptors: Evolution of bile acids from simple detergents to complex signaling molecules

Copple, B. L., & Li, T. (2015) · Pharmacological Research · doi:10.1016/j.phrs.2015.12.007 · Cited by 235 · see citing works

Bile Acid Receptor Activation Modulates Hepatic Monocyte Activity and Improves Nonalcoholic Fatty Liver Disease

McMahan, R. H., Wang, X. X., Cheng, L. L., Krisko, T., Smith, M., El Kasmi, K., Pruzanski, M., Adorini, L., Golden-Mason, L., Levi, M., et al. (2013) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.446575 · Cited by 225 · see citing works

The Bile Acid Receptor TGR5 Activates the TRPA1 Channel to Induce Itch in Mice

Lieu, T., Jayaweera, G., Zhao, P., Poole, D. P., Jensen, D. D., Grace, M. S., McIntyre, P., Bron, R., Wilson, Y. M., Krappitz, M., et al. (2014) · Gastroenterology · doi:10.1053/j.gastro.2014.08.042 · Cited by 221 · see citing works

Enterohepatic Circulation of Bile Salts in Farnesoid X Receptor-deficient Mice

Kok, T., Hulzebos, C. V., Wolters, H., Havinga, R., Agellon, L. B., Stellaard, F., Shan, B., Schwarz, M., & Kuipers, F. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m306309200 · Cited by 219 · see citing works

TGR5 is essential for bile acid-dependent cholangiocyte proliferation in vivo and in vitro

Reich, M., Deutschmann, K., Sommerfeld, A., Klindt, C., Kluge, S., Kubitz, R., Ullmer, C., Knoefel, W. T., Herebian, D. A., Mayatepek, E., et al. (2015) · Gut · doi:10.1136/gutjnl-2015-309458 · Cited by 210 · see citing works

TGR5 reduces macrophage migration through mTOR-induced C/EBPβ differential translation.

Perino, A., Pols, T. W., Nomura, M., Stein, S., Pellicciari, R., & Schoonjans, K. (2014) · Journal of Clinical Investigation · doi:10.1172/jci76289 · Cited by 209 · see citing works

Identification of fibroblast growth factor 15 as a novel mediator of liver regeneration and its application in the prevention of post-resection liver failure in mice

Uriarte, I., Fernandez-Barrena, M. G., Monte, M., Latasa, M., Chang, H. C. Y., Carotti, S., Vespasiani-Gentilucci, U., Morini, S., Vicente, E., Concepcion, A., et al. (2013) · Gut · doi:10.1136/gutjnl-2012-302945 · Cited by 196 · see citing works

The receptor TGR5 protects the liver from bile acid overload during liver regeneration in mice

Péan, N., Doignon, I., Garcin, I., Besnard, A., Julien, B., Liu, B., Branchereau, S., Spraul, A., Guettier, C., Humbert, L., et al. (2013) · Hepatology · doi:10.1002/hep.26463 · Cited by 193 · see citing works

NGM282 for treatment of non-alcoholic steatohepatitis: a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

Harrison, S. A., Rinella, M. E., Abdelmalek, M. F., Jf, T., Paredes, A. H., Arnold, H. L., Kugelmas, M., Bashir, M. R., Jaros, M. J., Li, L., et al. (2018) · Yearbook of pediatric endocrinology · doi:10.1530/ey.15.15.7 · Cited by 188 · see citing works

The FXR agonist PX20606 ameliorates portal hypertension by targeting vascular remodelling and sinusoidal dysfunction

Schwabl, P., Hambruch, E., Seeland, B. A., Hayden, H., Wagner, M., Garnys, L., Strobel, B., Schubert, T.-L., Riedl, F., Mitteregger, D., et al. (2017) · Journal of Hepatology · doi:10.1016/j.jhep.2016.12.005 · Cited by 178 · see citing works

Bile Acid Receptor TGR5 Agonism Induces NO Production and Reduces Monocyte Adhesion in Vascular Endothelial Cells

Kida, T., Tsubosaka, Y., Hori, M., Ozaki, H., & Murata, T. (2013) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.113.301565 · Cited by 166 · see citing works

Antibiotic effects on gut microbiota and metabolism are host dependent

Fujisaka, S., Ussar, S., Clish, C. B., Devkota, S., Dreyfuss, J. M., Sakaguchi, M., Soto, M., Konishi, M., Softic, S., Altındiş, E., et al. (2016) · Journal of Clinical Investigation · doi:10.1172/jci86674 · Cited by 166 · see citing works

Bile acids PKA-dependently induce a switch of the IL-10/IL-12 ratio and reduce proinflammatory capability of human macrophages

Haselow, K., Bode, J. G., Wammers, M., Ehlting, C., Keitel, V., Kleinebrecht, L., Schupp, A.-K., Häussinger, D., & Graf, D. (2013) · Journal of Leukocyte Biology · doi:10.1189/jlb.0812396 · Cited by 164 · see citing works

Bile acids induce monocyte differentiation toward interleukin‐12 hypo‐producing dendritic cells via a TGR5‐dependent pathway

Ichikawa, R., Takayama, T., Yoneno∥, K., Kamada, N., Kitazume, M. T., Higuchi, H., Matsuoka, K., 渡辺, 光., Itoh, H., Kanai∥, T., et al. (2012) · Immunology · doi:10.1111/j.1365-2567.2012.03554.x · Cited by 163 · see citing works

Ciliary subcellular localization of TGR5 determines the cholangiocyte functional response to bile acid signaling

Masyuk, A. I., Huang, B. Q., Radtke, B. N., Gajdos, G. B., Splinter, P. L., Masyuk, T. V., Gradilone, S. A., & LaRusso, N. F. (2013) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.00383.2012 · Cited by 143 · see citing works

TGR5 and Immunometabolism: Insights from Physiology and Pharmacology.

Perino, A., & Schoonjans, K. (2015) · TIPS - Trends in Pharmacological Sciences · doi:10.1016/j.tips.2015.08.002 · Cited by 141 · see citing works

Bile acid receptors in the biliary tree: TGR5 in physiology and disease

Deutschmann, K., Reich, M., Klindt, C., Dröge, C., Spomer, L., Häussinger, D., & Keitel, V. (2017) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2017.08.021 · Cited by 140 · see citing works

Hydrophobic bile salts inhibit gallbladder smooth muscle function via stimulation of GPBAR1 receptors and activation of KATPchannels

Lavoie, B. A., Balemba, O. B., Godfrey, C. B., Watson, C. A., Vassileva, G., Corvera, C. U., Nelson, M. T., & Mawe, G. M. (2010) · The Journal of Physiology · doi:10.1113/jphysiol.2010.192146 · Cited by 130 · see citing works

TGR 5 signaling reduces neuroinflammation during hepatic encephalopathy

McMillin, M., Frampton, G. A., Tobin, R. P., Dusio, G. F., Smith, J., Shin, H. D., Newell‐Rogers, K., Grant, S. M., & DeMorrow, S. (2015) · Journal of Neurochemistry · doi:10.1111/jnc.13243 · Cited by 129 · see citing works

Mutational Characterization of the Bile Acid Receptor TGR5 in Primary Sclerosing Cholangitis

Hov, J. R., Keitel, V., Laerdahl, J. K., Spomer, L., Ellinghaus, E., ElSharawy, A., Melum, E., Boberg, K. M., Manke, T., Balschun, T. C., et al. (2010) · PLoS ONE · doi:10.1371/journal.pone.0012403 · Cited by 129 · see citing works

The membrane-bound bile acid receptor TGR5 (Gpbar-1) is localized in the primary cilium of cholangiocytes

Keitel, V., Ullmer, C., & Häussinger, D. (2010) · Biological Chemistry · doi:10.1515/bc.2010.077 · Cited by 129 · see citing works

Perspective: TGR5 (Gpbar-1) in liver physiology and disease

Keitel, V., & Häussinger, D. (2012) · Clinics and Research in Hepatology and Gastroenterology · doi:10.1016/j.clinre.2012.03.008 · Cited by 123 · see citing works

Cell Lineage Tracing Reveals a Biliary Origin of Intrahepatic Cholangiocarcinoma

Guest, R. V., Boulter, L., Kendall, T. J., Minnis-Lyons, S. E., WALKER, R. E., Wigmore, S. J., Sansom, O. J., & Forbes, S. J. (2013) · Cancer Research · doi:10.1158/0008-5472.can-13-1911 · Cited by 120 · see citing works

G-Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5) Agonists Reduce the Production of Proinflammatory Cytokines and Stabilize the Alternative Macrophage Phenotype

Hoegenauer, K., Arista, L., Schmiedeberg, N., Werner, G., Jaksche, H., Bouhelal, R., Nguyen, D. G., Bhat, B. G., Raad, L., Rauld, C., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm501052c · Cited by 96 · see citing works

Immediate neuroendocrine signaling after partial hepatectomy through acute portal hyperpressure and cholestasis

Doignon, I., Julien, B., Serrière-Lanneau, V., Garcin, I., Alonso, G., Nicou, A., Monnet, F., Gigou, M., Humbert, L., Rainteau, D., et al. (2011) · Journal of Hepatology · doi:10.1016/j.jhep.2010.07.012 · Cited by 87 · see citing works

Design, Synthesis, and Antidiabetic Activity of 4-Phenoxynicotinamide and 4-Phenoxypyrimidine-5-carboxamide Derivatives as Potent and Orally Efficacious TGR5 Agonists

Duan, H., Ning, M., Chen, X., Zou, Q., Zhang, L., Feng, Y., Zhang, L., Leng, Y., & Shen, J. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm301071h · Cited by 85 · see citing works

Gender-dependent effect of Gpbar1 genetic deletion on the metabolic profiles of diet-induced obese mice

Vassileva, G., Hu, W., Hoos, L. M., Tetzloff, G. G., Yang, S., Liu, L., Kang, L., Davis, H. R., Hedrick, J. A., Hong, L., et al. (2010) · Journal of Endocrinology · doi:10.1677/joe-10-0009 · Cited by 83 · see citing works

Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice

Briere, D. A., Ruan, X., Cheng, C., Siesky, A. M., Fitch, T. E., Dominguez, C., Sanfeliciano, S. G., Montero, C., Suen, C. S., Xu, Y., et al. (2015) · PLoS ONE · doi:10.1371/journal.pone.0136873 · Cited by 79 · see citing works

Differential effects of FXR or TGR5 activation in cholangiocarcinoma progression

Erice, O., Labiano, I., Arbelaiz, A., Santos‐Laso, Á., Muñoz-Garrido, P., Jiménez-Agüero, R., Olaizola, P., Caro‐Maldonado, A., Martín-Martín, N., Carracedo, A., et al. (2017) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2017.08.016 · Cited by 79 · see citing works

TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling

Masyuk, T. V., Masyuk, A. I., Pisarello, M. J. L., Howard, B. N., Huang, B. Q., Lee, P. Y., Fung, X., Sergienko, E. A., Ardecky, R., Chung, T. D. Y., et al. (2017) · Hepatology · doi:10.1002/hep.29284 · Cited by 77 · see citing works

α5β1-integrins are sensors for tauroursodeoxycholic acid in hepatocytes

Gohlke, H., Schmitz, B., Sommerfeld, A., Reinehr, R., & Häussinger, D. (2013) · Hepatology · doi:10.1002/hep.25992 · Cited by 77 · see citing works

Selective interaction of bile acids with muscarinic receptors: a case of molecular mimicry

Raufman, J., Chen, Y., Cheng, K., Compadre, C. M., Compadre, L., & Zimniak, P. (2002) · European Journal of Pharmacology · doi:10.1016/s0014-2999(02)02690-0 · Cited by 72 · see citing works

Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1

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Cystathionine γ-lyase, a H2S-generating enzyme, is a GPBAR1-regulated gene and contributes to vasodilation caused by secondary bile acids

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TGR5 and FXR receptors in motor degeneration: Molecular mechanism, crosstalk pathways and therapeutic prospects

Banerjee, S., Panjwani, D., Singh, S., & Singh, T. G. (2026) · Journal of Neuroimmunology · doi:10.1016/j.jneuroim.2026.578942 · Cited by 1 · see citing works

Mechanisms of Bile Formation and the Pathogenesis of Cholestasis

Karpen, S. J. (2021) · Cambridge University Press eBooks · doi:10.1017/9781108918978.003 · Cited by 1 · see citing works

Diagnosing Liver Cirrhosis by Overlooked Tools: A Retrospective StudyPreprint

Tarantino, G., Citro, V., Tarantino, M., & Capone, D. (2023) · Preprints.org · doi:10.20944/preprints202309.2059.v1 · Cited by 1 · see citing works

Bile Acid Receptors in Cholangiocyte

Park, J. M. (2021) · The Korean Journal of Pancreas and Biliary Tract · doi:10.15279/kpba.2021.26.4.254

GPBAR1 Promotes Proliferation and Is Related to Poor Prognosis of High-Grade Glioma via Inducing MAFB ExpressionPreprint

Sun, S., Guo, H., Liang, N., Wu, T., Zhang, C., & Li, H. (2021) · Research Square · doi:10.21203/rs.3.rs-419714/v1

My lifelong dedication to bile acid research

Chiang, J. Y. L. (2023) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2023.103070

The role of G-proteins and G-protein-coupledreceptors in human disease

Xian, Y. (2023) · MedScien · doi:10.61173/d7dc6a45

Avaliação dos efeitos do TUDCA na deposição de gordura hepática e na regulação do metabolismo dos ácidos biliares durante a restrição proteica

Bonfim, M. F. (2021) · doi:10.47749/t/unicamp.2021.1244895

Exploring the unknown territory of gut–brain axis in type 2 diabetes mellitus patients

Rahim, S., & Karim, M. M. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-33355-2.00007-4

Additional file 3 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741360

Additional file 2 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26143803

Additional file 8 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741375

Additional file 5 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741366

Additional file 10 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741381

Additional file 7 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741372

Additional file 9 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741378

Additional file 11 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741384

Additional file 12 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741387

Additional file 1 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26143716

Additional file 4 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741363

Additional file 6 of Cholestasis-induced phenotypic transformation of neutrophils contributes to immune escape of colorectal cancer liver metastasis

Sun, L., Yang, N., Liu, Z., Ye, X., Cheng, M., Deng, L., Zhang, J., Wu, J., Shi, M., & Liao, W. (2024) · Figshare · doi:10.6084/m9.figshare.26741369

Research Progress on the Mechanism and Targeted Intervention of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1)-Mediated “Inflammation-Apoptosis-Metabolism-Microcirculation” Regulatory Network in Hepatitis B-Associated Liver Failure

Cui, C., Sun, Y., Zhang, K., Shi, J., Wang, K., & Gao, S. (2026) · Drug Design Development and Therapy · doi:10.2147/dddt.s573597

Bile acids signaling as a novel mechanism in the hypothalamic control of energy balance.

Castellanos-Jankiewicz, A. (2019) · doi:10.70675/add823eez1845z4f7ezbe46zb57c0325a3fc

Role of the G Protein-Coupled Bile Acid Receptor TGR5 in Liver Damage

Reich, M., Klindt, C., Deutschmann, K., Spomer, L., Häussinger, D., & Keitel, V. (2017) · Digestive Diseases · doi:10.1159/000450917 · Cited by 52 · see citing works

Progress in research on the roles of TGR5 receptor in liver diseases

Ma, K., Tang, D., Yu, C. J., & Zhao, L. (2021) · Scandinavian Journal of Gastroenterology · doi:10.1080/00365521.2021.1903547 · Cited by 25 · see citing works

TGR5 in cholangiocytes

Keitel, V., & Häussinger, D. (2013) · Current Opinion in Gastroenterology · doi:10.1097/mog.0b013e32835f3f14 · Cited by 44 · see citing works

Perspective: TGR5 (Gpbar-1) in liver physiology and disease

Keitel, V., & Häussinger, D. (2012) · Clinics and Research in Hepatology and Gastroenterology · doi:10.1016/j.clinre.2012.03.008 · Cited by 123 · see citing works

The role of bile acid-activated receptor TGR5 in inflammation and liver diseases

Xiang, H., Xiang, H., Wang, S., Wu, P., Luo, Z., & Zhang, J. (2026) · Frontiers in Physiology · doi:10.3389/fphys.2026.1747341 · Cited by 12 · see citing works