Results 11 to 20 of about 1,660 (124)

Mutational characterization of the bile acid receptor TGR5 in primary sclerosing cholangitis. [PDF]

PLoS ONE, 2010
TGR5, the G protein-coupled bile acid receptor 1 (GPBAR1), has been linked to inflammatory pathways as well as bile homeostasis, and could therefore be involved in primary sclerosing cholangitis (PSC) a chronic inflammatory bile duct disease. We aimed to
Johannes R Hov, Verena Keitel, Jon K Laerdahl, Lina Spomer, Eva Ellinghaus, Abdou ElSharawy, Espen Melum, Kirsten M Boberg, Thomas Manke, Tobias Balschun, Christoph Schramm, Annika Bergquist, Tobias Weismüller, Daniel Gotthardt, Christian Rust, Liesbet Henckaerts, Clive M Onnie, Rinse K Weersma, Martina Sterneck, Andreas Teufel, Heiko Runz, Adolf Stiehl, Cyriel Y Ponsioen, Cisca Wijmenga, Morten H Vatn, IBSEN Study Group, Pieter C F Stokkers, Severine Vermeire, Christopher G Mathew, Benedicte A Lie, Ulrich Beuers, Michael P Manns, Stefan Schreiber, Erik Schrumpf, Dieter Häussinger, Andre Franke, Tom H Karlsen   +36 more
doaj   +5 more sources

Development of betulinic acid as an agonist of TGR5 receptor using a new in vitro assay [PDF]

Drug Design, Development and Therapy, 2016
Shih-Hsiang Lo,1,2 Kai-Chung Cheng,3 Ying-Xiao Li,3,4 Chin-Hong Chang,4,5 Juei-Tang Cheng,4,6 Kung-Shing Lee7,8 1Division of Cardiology, Department of Internal Medicine, Zhongxing Branch of Taipei City Hospital, 2Department of History and Geography ...
Lo SH, Cheng KC, Li YX, Chang CH, Cheng JT, Lee KS   +5 more
doaj   +2 more sources

Investigation of triamterene as an inhibitor of the TGR5 receptor: identification in cells and animals

Drug Design, Development and Therapy, 2017
Yingxiao Li,1,2 Kai Chun Cheng,1 Chiang-Shan Niu,3 Shih-Hsiang Lo,3,4 Juei-Tang Cheng,2,5 Ho-Shan Niu31Department of Psychosomatic Internal Medicine, Graduate School of Medical and Dental Sciences, Kagoshima University, Kagoshima, Japan; 2Department of ...
Li Y, Cheng KC, Niu C, Lo S, Cheng JT, Niu H   +5 more
doaj   +1 more source

TGR5 controls bile acid composition and gallbladder function to protect the liver from bile acid overload

JHEP Reports, 2021
Background & Aims: As the composition of the bile acid (BA) pool has a major impact on liver pathophysiology, we studied its regulation by the BA receptor Takeda G protein coupled receptor (TGR5), which promotes hepatoprotection against BA overload ...
Valeska Bidault-Jourdainne, Grégory Merlen, Mathilde Glénisson, Isabelle Doignon, Isabelle Garcin, Noémie Péan, Raphael Boisgard, José Ursic-Bedoya, Matteo Serino, Christoph Ullmer, Lydie Humbert, Ahmed Abdelrafee, Nicolas Golse, Eric Vibert, Jean-Charles Duclos-Vallée, Dominique Rainteau, Thierry Tordjmann   +16 more
doaj   +2 more sources

Bile salt receptor TGR5 is highly expressed in esophageal adenocarcinoma and precancerous lesions with significantly worse overall survival and gender differences

Clinical and Experimental Gastroenterology, 2017
Chunhong Pang,1,2 Amy LaLonde,3 Tony E Godfrey,4 Jianwen Que,5,6 Jun Sun,7 Tong Tong Wu,3 Zhongren Zhou2 1Department of Pathology, China-Japan Friendship Hospital, 2Department of Pathology and Laboratory Medicine, 3Department of Biostatistics and ...
Pang CH, LaLonde A, Godfrey TE, Que J, Sun J, Wu TT, Zhou ZR   +6 more
doaj   +1 more source

Intestinal peroxisome proliferator‐activated receptor α‐fatty acid‐binding protein 1 axis modulates nonalcoholic steatohepatitis

Hepatology, EarlyView., 2022
Abstract Background and Aims Peroxisome proliferator‐activated receptor α (PPARα) regulates fatty acid transport and catabolism in liver. However, the role of intestinal PPARα in lipid homeostasis is largely unknown. Here, intestinal PPARα was examined for its modulation of obesity and NASH. Approach and Results Intestinal PPARα was activated and fatty
Tingting Yan, Yuhong Luo, Nana Yan, Keisuke Hamada, Nan Zhao, Yangliu Xia, Ping Wang, Changdong Zhao, Dan Qi, Shoumei Yang, Lulu Sun, Jie Cai, Qiong Wang, Changtao Jiang, Oksana Gavrilova, Kristopher W. Krausz, Daxesh P. Patel, Xiaoting Yu, Xuan Wu, Haiping Hao, Weiwei Liu, Aijuan Qu, Frank J. Gonzalez   +22 more
wiley   +1 more source

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, EarlyView., 2022
CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli, Silvia Marchianò, Cristina di Giorgio, Rosalinda Roselli, Martina Bordoni, Rachele Bellini, Bianca Fiorillo, Valentina Sepe, Bruno Catalanotti, Chiara Cassiano, Maria Chiara Monti, Eleonora Distrutti, Angela Zampella, Stefano Fiorucci   +13 more
wiley   +1 more source

Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5^H88Y Mutant Mice

Takeda G protein-coupled receptor 5 (TGR5) is a promising target for treating metabolic syndrome and inflammatory diseases. Herein, we identified a new series of betulinic acid derivatives as potent TGR5 agonists, which show remarkable activity on human (
Min Gu (305818), Xin Xie (311744), Yuan Lan (11291210), Jing Li (10611), Ning Zhuo (3089652), Ying Yun (7460177), Jianpeng Yin (2112994), Fajun Nan (1426045), Shimeng Guo (818772), Huanan Liu (10644772), Min Wang (21070), Xiaoying Liang (552537), Chenlu Zhang (508309)   +12 more
core   +6 more sources

Role of TGR5 in Bile Acid Metabolism [PDF]

, 2011
TGR5 is a G protein-coupled bile acid receptor present in various tissues in the body. Its agonism increases energy expenditure and lowers blood glucose. Thus, it is an attractive drug target for treating human metabolic disease.
Li, Tingting
core   +3 more sources

New synthetic bile acid analogue agonists of FXR and TGR5 receptors: Analytical methodologies for the study of their physico-chemical properties, pharmacokinetic activity and metabolism. [PDF]

, 2013
This thesis reports an integrated analytical approach for the study of physicochemical and biological properties of new synthetic bile acid (BA) analogues agonists of FXR and TGR5 receptors.
Colliva, Carolina <1981>
core   +1 more source