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Reviews

Patented TGR5 modulators: a review (2006 – present)

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Pages 1399-1414 | Published online: 06 Oct 2012

Keep up to date with the latest research on this topic with citation updates for this article.

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Rakesh Sahu, Rakhi Mishra & Chandana Majee. (2020) An insight into primary biliary cholangitis and its recent advances in treatment: semi-synthetic analogs to combat ursodeoxycholic-acid resistance. Expert Review of Gastroenterology & Hepatology 14:10, pages 985-998.
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Hannah M Eggink, Maarten R Soeters & Thijs WH Pols. (2014) TGR5 ligands as potential therapeutics in inflammatory diseases. International Journal of Interferon, Cytokine and Mediator Research 6, pages 27-38.
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Saurin Raval. (2013) Compound and compositions as TGR5 agonists: WO2012082947. Expert Opinion on Therapeutic Patents 23:4, pages 531-536.
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Articles from other publishers (40)

Emiliano Rosatelli, Andrea Carotti, Bruno Cerra, Francesca De Franco, Daniela Passeri, Roberto Pellicciari & Antimo Gioiello. (2023) Chemical exploration of TGR5 functional hot-spots: Synthesis and structure-activity relationships of C7- and C23-Substituted cholic acid derivatives. European Journal of Medicinal Chemistry 261, pages 115851.
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Sylvain Picon, Rajaa Boulahjar, Vanessa Hoguet, Morgane Baron, Isabelle Duplan, Emmanuelle Vallez, Nathalie Hennuyer, Julie Dumont, Véronique Touche, Emilie Dorchies, Manuel Lasalle, Amandine Descat, Catherine Piveteau, Alexandre Biela, Ludovic Chaput, Bruno O. Villoutreix, Emmanuelle Lipka, Emmanuel Sevin, Maxime Culot, Fabien Gosselet, Sophie Lestavel, Pascal Roussel, Rebecca Deprez-Poulain, Florence Leroux, Bart Staels, Benoit Deprez, Anne Tailleux & Julie Charton. (2023) Discovery, Structure–Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5. Journal of Medicinal Chemistry 66:17, pages 11732-11760.
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Yan Li, Jingjing Sun, Xiao Wang, Zhijie Luo, Xuemei Shao, Yingxiu Li, Qirong Cao, Shuai Zhao, Mingcheng Qian & Xin Chen. (2023) Discovery and biological evaluation of cholic acid derivatives as potent TGR5 positive allosteric modulators. Bioorganic & Medicinal Chemistry 92, pages 117418.
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Kenneth C. P. Cheung, Jiao Ma, Rodrigo Azevedo Loiola, Xingxuan Chen & Wei Jia. (2023) Bile acid‐activated receptors in innate and adaptive immunity: targeted drugs and biological agents. European Journal of Immunology 53:8.
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Elizabeth M. Ure, Lawrence D. Harris, Scott A. Cameron, Alex Weymouth-Wilson, Richard H. Furneaux, Janet L. Pitman, Simon. F. Hinkley & Andreas Luxenburger. (2022) Synthesis of 12β-methyl-18- nor -avicholic acid analogues as potential TGR5 agonists . Organic & Biomolecular Chemistry 20:17, pages 3511-3527.
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Shizhen Zhao, Le Wang, Jie Wang, Chenwei Wang, Shaowei Zheng, Yajie Fu, Yunfu Li, Wei-Dong Chen, Ruifang Hou, Dongbin Yang & Yan-Dong Wang. (2022) Design, synthesis and evaluation of 3-phenoxypyrazine-2-carboxamide derivatives as potent TGR5 agonists. RSC Advances 12:6, pages 3618-3629.
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Mingjie Fan, Yangmeng Wang, Lihua Jin, Zhipeng Fang, Jiangling Peng, Jui Tu, Yanjun Liu, Eryun Zhang, Senlin Xu, Xiaoqian Liu, Yuqing Huo, Zhaoli Sun, Xiaojuan Chao, Wen-Xing Ding, Qingfeng Yan & Wendong Huang. (2022) Bile Acid–Mediated Activation of Brown Fat Protects From Alcohol-Induced Steatosis and Liver Injury in Mice. Cellular and Molecular Gastroenterology and Hepatology 13:3, pages 809-826.
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Sachiho Miyata, Yuji Kawashima, Miku Sakai, Masaya Matsubayashi, Keisuke Motoki, Yui Miyajima, Yousuke Watanabe, Noriko Chikamatsu, Tetsuya Taniguchi & Ryukou Tokuyama. (2021) Discovery, optimization, and evaluation of non-bile acid FXR/TGR5 dual agonists. Scientific Reports 11:1.
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Piero Portincasa, Agostino Di Ciaula, Gabriella Garruti, Mirco Vacca, Maria De Angelis & David Q.-H. Wang. (2020) Bile Acids and GPBAR-1: Dynamic Interaction Involving Genes, Environment and Gut Microbiome. Nutrients 12:12, pages 3709.
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Simona De Marino, Claudia Finamore, Michele Biagioli, Adriana Carino, Silvia Marchianò, Rosalinda Roselli, Cristina Di Giorgio, Martina Bordoni, Francesco Saverio Di Leva, Ettore Novellino, Chiara Cassiano, Vittorio Limongelli, Angela Zampella, Carmen Festa & Stefano Fiorucci. (2020) GPBAR1 Activation by C6-Substituted Hyodeoxycholane Analogues Protect against Colitis. ACS Medicinal Chemistry Letters 11:5, pages 818-824.
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Grégory Merlen, Valeska Bidault‐Jourdainne, Nicolas Kahale, Mathilde Glenisson, José Ursic‐Bedoya, Isabelle Doignon, Isabelle Garcin, Lydie Humbert, Dominique Rainteau & Thierry Tordjmann. (2020) Hepatoprotective impact of the bile acid receptor TGR5. Liver International 40:5, pages 1005-1015.
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Mari Lilith Lund, Giovanni Sorrentino, Kristoffer Lihme Egerod, Chantal Kroone, Brynjulf Mortensen, Filip Krag Knop, Frank ReimannFiona M. Gribble, Daniel J. Drucker, Eelco J.P. de Koning, Kristina Schoonjans, Fredrik Bäckhed, Thue W. Schwartz & Natalia Petersen. (2020) L-Cell Differentiation Is Induced by Bile Acids Through GPBAR1 and Paracrine GLP-1 and Serotonin Signaling. Diabetes 69:4, pages 614-623.
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Lu Zhang, Xianjun Fu, Ting Gui, Tianqi Wang, Zhenguo Wang, Gerd A. Kullak-Ublick & Zhibo Gai. (2019) Effects of Farnesiferol B on Ischemia-Reperfusion-Induced Renal Damage, Inflammation, and NF-κB Signaling. International Journal of Molecular Sciences 20:24, pages 6280.
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Slavica Lazarević, Maja Đanić, Svetlana Goločorbin-Kon, Hani Al-Salami & Momir Mikov. (2019) Semisynthetic bile acids: a new therapeutic option for metabolic syndrome. Pharmacological Research 146, pages 104333.
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Joanne M. Donkers, Reinout L.P. Roscam Abbing & Stan F.J. van de Graaf. (2019) Developments in bile salt based therapies: A critical overview. Biochemical Pharmacology 161, pages 1-13.
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Francesco Saverio Di Leva, Daniele Di Marino & Vittorio Limongelli. 2019. Bile Acids and Their Receptors. Bile Acids and Their Receptors 111 136 .
Juan P. Arab, Saul J. Karpen, Paul A. Dawson, Marco Arrese & Michael Trauner. (2016) Bile acids and nonalcoholic fatty liver disease: Molecular insights and therapeutic perspectives. Hepatology 65:1, pages 350-362.
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Roberto Pellicciari, Daniela Passeri, Francesca De Franco, Serena Mostarda, Paolo Filipponi, Carolina Colliva, Raffaella Maria Gadaleta, Placido Franco, Andrea Carotti, Antonio Macchiarulo, Aldo Roda, Antonio Moschetta & Antimo Gioiello. (2016) Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders. Journal of Medicinal Chemistry 59:19, pages 9201-9214.
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Yanping Xu. (2016) Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases. Journal of Medicinal Chemistry 59:14, pages 6553-6579.
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R. J. Hodge & D. J. Nunez. (2016) Therapeutic potential of T akeda‐ G ‐protein‐receptor‐5 ( TGR5 ) agonists. H ope or hype? . Diabetes, Obesity and Metabolism 18:5, pages 439-443.
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Christina Lamers, Daniel Merk, Matthias Gabler, Daniel Flesch, Astrid Kaiser & Manfred Schubert-Zsilavecz. (2016) SAR studies on FXR modulators led to the discovery of the first combined FXR antagonistic/TGR5 agonistic compound. Future Medicinal Chemistry 8:2, pages 133-148.
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Sameer Agarwal, Amit Patil, Umesh Aware, Prashant Deshmukh, Brijesh Darji, Santosh Sasane, Kalapatapu V. V. M. Sairam, Priyanka Priyadarsiny, Poonam Giri, Harilal Patel, Suresh Giri, Mukul Jain & Ranjit C. Desai. (2015) Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist. ACS Medicinal Chemistry Letters 7:1, pages 51-55.
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Bruno Cerra, Serena Mostarda, Chiara Custodi, Antonio Macchiarulo & Antimo Gioiello. (2016) Integrating multicomponent flow synthesis and computational approaches for the generation of a tetrahydroquinoline compound based library. MedChemComm 7:3, pages 439-446.
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Alessia Perino & Kristina Schoonjans. (2015) TGR5 and Immunometabolism: Insights from Physiology and Pharmacology. Trends in Pharmacological Sciences 36:12, pages 847-857.
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Christoph G.W. Gertzen, Lina Spomer, Sander H.J. Smits, Dieter Häussinger, Verena Keitel & Holger Gohlke. (2015) Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists. European Journal of Medicinal Chemistry 104, pages 57-72.
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Chen Zhou, Fangxia Zou, Yungen Xu, Luyong Zhang & Xiaoming Zha. (2015) Identification of new non-steroidal TGR5 agonists using virtual screening with combined pharmacophore models. Medicinal Chemistry Research 24:6, pages 2561-2572.
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Klemens Högenauer, Luca Arista, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche, Rochdi Bouhelal, Deborah G. Nguyen, B. Ganesh Bhat, Layla Raad, Celine Rauld & José M. Carballido. (2014) G-Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5) Agonists Reduce the Production of Proinflammatory Cytokines and Stabilize the Alternative Macrophage Phenotype. Journal of Medicinal Chemistry 57:24, pages 10343-10354.
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Aldo Roda, Roberto Pellicciari, Antimo Gioiello, Flavia Neri, Cecilia Camborata, Daniela Passeri, Francesca De Franco, Silvia Spinozzi, Carolina Colliva, Luciano Adorini, Marco Montagnani & Rita Aldini. (2014) Semisynthetic Bile Acid FXR and TGR5 Agonists: Physicochemical Properties, Pharmacokinetics, and Metabolism in the Rat. Journal of Pharmacology and Experimental Therapeutics 350:1, pages 56-68.
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Nuruddeen D. Lewis, Lori A. Patnaude, Josephine Pelletier, Donald J. Souza, Susan M. Lukas, F. James King, Jonathan D. Hill, Dimitria E. Stefanopoulos, Kelli Ryan, Sudha Desai, Donna Skow, Stefan G. Kauschke, Andre Broermann, Daniel Kuzmich, Christian Harcken, Eugene R. Hickey & Louise K. Modis. (2014) A GPBAR1 (TGR5) Small Molecule Agonist Shows Specific Inhibitory Effects on Myeloid Cell Activation In Vitro and Reduces Experimental Autoimmune Encephalitis (EAE) In Vivo. PLoS ONE 9:6, pages e100883.
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Sujith Rajan, Abhishek Gupta, Muheeb Beg, Kripa Shankar, Ankita Srivastava, Salil Varshney, Durgesh Kumar & Anil Nilkanth Gaikwad. (2014) Adipocyte transdifferentiation and its molecular targets. Differentiation 87:5, pages 183-192.
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Dean P. Phillips, Wenqi Gao, Yang Yang, Guobao Zhang, Isabelle K. Lerario, Thomas L. Lau, Jiqing Jiang, Xia Wang, Deborah G. Nguyen, B. Ganesh Bhat, Carol Trotter, Heather Sullivan, Gustav Welzel, Jannine Landry, Yali Chen, Sean B. Joseph, Chun Li, W. Perry Gordon, Wendy Richmond, Kevin Johnson, Angela Bretz, Badry Bursulaya, Shifeng Pan, Peter McNamara & H. Martin Seidel. (2014) Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure–Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy. Journal of Medicinal Chemistry 57:8, pages 3263-3282.
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Thijs W.H. Pols. (2014) TGR5 in inflammation and cardiovascular disease. Biochemical Society Transactions 42:2, pages 244-249.
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Henri Duboc, Yvette Taché & Alan F. Hofmann. (2014) The bile acid TGR5 membrane receptor: From basic research to clinical application. Digestive and Liver Disease 46:4, pages 302-312.
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T Lieu, G Jayaweera & N W Bunnett. (2014) GPBA : a GPCR for bile acids and an emerging therapeutic target for disorders of digestion and sensation . British Journal of Pharmacology 171:5, pages 1156-1166.
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Serena Mostarda, Paolo Filipponi, Roccaldo Sardella, Francesco Venturoni, Benedetto Natalini, Roberto Pellicciari & Antimo Gioiello. (2014) Glucuronidation of bile acids under flow conditions: design of experiments and Koenigs–Knorr reaction optimization. Org. Biomol. Chem. 12:47, pages 9592-9600.
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Benedetto Natalini, Roccaldo Sardella, Antimo Gioiello, Federica Ianni, Alessandro Di Michele & Maura Marinozzi. (2014) Determination of bile salt critical micellization concentration on the road to drug discovery. Journal of Pharmaceutical and Biomedical Analysis 87, pages 62-81.
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Massimiliano Tognolini, Matteo Incerti, Daniele Pala, Simonetta Russo, Riccardo Castelli, Iftiin Hassan‐Mohamed, Carmine Giorgio & Alessio Lodola. (2013) Target Hopping as a Useful Tool for the Identification of Novel EphA2 Protein–Protein Antagonists. ChemMedChem 9:1, pages 67-72.
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Antonio Macchiarulo, Antimo Gioiello, Charles Thomas, Thijs W. H. Pols, Roberto Nuti, Cristina Ferrari, Nicola Giacchè, Francesca De Franco, Mark Pruzanski, Johan Auwerx, Kristina Schoonjans & Roberto Pellicciari. (2013) Probing the Binding Site of Bile Acids in TGR5. ACS Medicinal Chemistry Letters 4:12, pages 1158-1162.
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Simonetta Russo, Matteo Incerti, Massimiliano Tognolini, Riccardo Castelli, Daniele Pala, Iftiin Hassan-Mohamed, Carmine Giorgio, Francesca De Franco, Antimo Gioiello, Paola Vicini, Elisabetta Barocelli, Silvia Rivara, Marco Mor & Alessio Lodola. (2013) Synthesis and Structure-Activity Relationships of Amino Acid Conjugates of Cholanic Acid as Antagonists of the EphA2 Receptor. Molecules 18:10, pages 13043-13060.
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Henrietta Dehmlow, Rubén Alvarez Sánchez, Stephan Bachmann, Caterina Bissantz, Fritz Bliss, Karin Conde-Knape, Martin Graf, Rainer E. Martin, Ulrike Obst Sander, Susanne Raab, Hans G.F. Richter, Sabine Sewing, Urs Sprecher, Christoph Ullmer & Patrizio Mattei. (2013) Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists. Bioorganic & Medicinal Chemistry Letters 23:16, pages 4627-4632.
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