PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 27578964-0 2016 Development of betulinic acid as an agonist of TGR5 receptor using a new in vitro assay. betulinic acid 15-29 G protein-coupled bile acid receptor 1 Homo sapiens 47-51 34406006-2 2021 Herein, we identified a new series of betulinic acid derivatives as potent TGR5 agonists, which show remarkable activity on human (h) and canine (c) TGR5 but exhibit unpromising activity on murine (m) TGR5. betulinic acid 38-52 G protein-coupled bile acid receptor 1 Homo sapiens 75-79 27578964-3 2016 Betulinic acid, a triterpenoid present in the leaves of white birch, has been introduced as a selective TGR5 agonist. betulinic acid 0-14 G protein-coupled bile acid receptor 1 Homo sapiens 104-108 27578964-4 2016 However, direct activation of TGR5 by betulinic acid has not yet been reported. betulinic acid 38-52 G protein-coupled bile acid receptor 1 Homo sapiens 30-34 27578964-9 2016 RESULTS: Betulinic acid dose-dependently increases glucose uptake by CHO-K1 cells transfected with TGR5 only, which can be considered an alternative method instead of radioligand binding assay. betulinic acid 9-23 G protein-coupled bile acid receptor 1 Homo sapiens 99-103 27578964-11 2016 In NCI-H716 cells, which endogenously express TGR5, betulinic acid induces glucagon-like peptide secretion via increasing calcium levels. betulinic acid 52-66 G protein-coupled bile acid receptor 1 Homo sapiens 46-50 27578964-12 2016 However, the actions of betulinic acid were markedly reduced in NCI-H716 cells that received TGR5-silencing treatment. betulinic acid 24-38 G protein-coupled bile acid receptor 1 Homo sapiens 93-97 27578964-13 2016 Therefore, the present study demonstrates the activation of TGR5 by betulinic acid for the first time. betulinic acid 68-82 G protein-coupled bile acid receptor 1 Homo sapiens 60-64 27578964-14 2016 CONCLUSION: Similar to the positive control lithocholic acid, which is the established agonist of TGR5, betulinic acid has been characterized as a useful agonist of TGR5 and can be used to activate TGR5 in the future. betulinic acid 104-118 G protein-coupled bile acid receptor 1 Homo sapiens 98-102 27578964-14 2016 CONCLUSION: Similar to the positive control lithocholic acid, which is the established agonist of TGR5, betulinic acid has been characterized as a useful agonist of TGR5 and can be used to activate TGR5 in the future. betulinic acid 104-118 G protein-coupled bile acid receptor 1 Homo sapiens 165-169 27578964-14 2016 CONCLUSION: Similar to the positive control lithocholic acid, which is the established agonist of TGR5, betulinic acid has been characterized as a useful agonist of TGR5 and can be used to activate TGR5 in the future. betulinic acid 104-118 G protein-coupled bile acid receptor 1 Homo sapiens 165-169 25418122-8 2015 RESULTS: In this study, results show that triggering TGR5 with the specific agonist betulinic acid (BA), and the bile acids CDCA or DCA, activated both the main MAP kinases ERK1/2, p38 and JNK, and the NF-kappaB signaling pathway. betulinic acid 84-98 G protein-coupled bile acid receptor 1 Homo sapiens 53-57 25418122-8 2015 RESULTS: In this study, results show that triggering TGR5 with the specific agonist betulinic acid (BA), and the bile acids CDCA or DCA, activated both the main MAP kinases ERK1/2, p38 and JNK, and the NF-kappaB signaling pathway. betulinic acid 100-102 G protein-coupled bile acid receptor 1 Homo sapiens 53-57 25283506-0 2014 Highly lipophilic 3-epi-betulinic acid derivatives as potent and selective TGR5 agonists with improved cellular efficacy. betulinic acid 18-38 G protein-coupled bile acid receptor 1 Homo sapiens 75-79 25283506-3 2014 Here, we sought to design and synthesize a series of TGR5 agonists derived from the natural product betulinic acid. betulinic acid 100-114 G protein-coupled bile acid receptor 1 Homo sapiens 53-57 25283506-11 2014 CONCLUSION: This study demonstrates that highly lipophilic 3-epi-betulinic acid derivatives can be potent and selective TGR5 agonists with improved cellular efficacy, and our research here provides a new strategy for the design and development of potent TGR5 agonists. betulinic acid 59-79 G protein-coupled bile acid receptor 1 Homo sapiens 120-124 25283506-11 2014 CONCLUSION: This study demonstrates that highly lipophilic 3-epi-betulinic acid derivatives can be potent and selective TGR5 agonists with improved cellular efficacy, and our research here provides a new strategy for the design and development of potent TGR5 agonists. betulinic acid 59-79 G protein-coupled bile acid receptor 1 Homo sapiens 254-258 19911773-0 2010 Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes. betulinic acid 41-55 G protein-coupled bile acid receptor 1 Homo sapiens 79-83