Cargando…

Discovery, optimization, and evaluation of non-bile acid FXR/TGR5 dual agonists

Although several potent bile acid Farnesoid X receptor (FXR) and Takeda G-protein-coupled receptor 5 (TGR5, GPBAR1) dual agonists such as INT-767 have been reported, no non-bile acid FXR/TGR5 dual agonist has been investigated to date. Therefore, we attempted to discover potent non-bile acid FXR/TGR...

Descripción completa

Detalles Bibliográficos
Autores principales:	Miyata, Sachiho, Kawashima, Yuji, Sakai, Miku, Matsubayashi, Masaya, Motoki, Keisuke, Miyajima, Yui, Watanabe, Yousuke, Chikamatsu, Noriko, Taniguchi, Tetsuya, Tokuyama, Ryukou
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Nature Publishing Group UK 2021
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8080777/ https://www.ncbi.nlm.nih.gov/pubmed/33911126 http://dx.doi.org/10.1038/s41598-021-88493-0

Ejemplares similares

Hepatic Bile Acid Reuptake in the Rat Depends on Bile Acid Conjugation but Not on Agonistic Properties towards FXR and TGR5
por: Trammell, Samuel A. J., et al.
Publicado: (2020)

Reversal of metabolic disorders by pharmacological activation of bile acid receptors TGR5 and FXR
por: Jadhav, Kavita, et al.
Publicado: (2018)

Activation of the bile acid receptors TGR5 and FXR in the spinal dorsal horn alleviates neuropathic pain
por: Wu, Yuning, et al.
Publicado: (2023)

Hypouricemic agents reduce indoxyl sulfate excretion by inhibiting the renal transporters OAT1/3 and ABCG2
por: Taniguchi, Tetsuya, et al.
Publicado: (2021)

FXR and TGR5 Agonists Ameliorate Liver Injury, Steatosis, and Inflammation After Binge or Prolonged Alcohol Feeding in Mice
por: Iracheta‐Vellve, Arvin, et al.
Publicado: (2018)

The Gut Microbiota as a Therapeutic Target in IBD and Metabolic Disease: A Role for the Bile Acid Receptors FXR and TGR5
por: Baars, Annemarie, et al.
Publicado: (2015)

Blueberry Extract Improves Obesity through Regulation of the Gut Microbiota and Bile Acids via Pathways Involving FXR and TGR5
por: Guo, Jielong, et al.
Publicado: (2019)

FXR/TGR5 mediates inflammasome activation and host resistance to bacterial infection
por: Kang, Ju-Hee, et al.
Publicado: (2021)

Dual Activation of the Bile Acid Nuclear Receptor FXR and G-Protein-Coupled Receptor TGR5 Protects Mice against Atherosclerosis
por: Miyazaki-Anzai, Shinobu, et al.
Publicado: (2014)

Notoginsenoside Ft1 acts as a TGR5 agonist but FXR antagonist to alleviate high fat diet-induced obesity and insulin resistance in mice
por: Ding, Lili, et al.
Publicado: (2021)

Crosstalk between FXR and TGR5 controls glucagon-like peptide 1 secretion to maintain glycemic homeostasis
por: Kim, Hyeonhui, et al.
Publicado: (2018)

Gut microbiota-related bile acid metabolism-FXR/TGR5 axis impacts the response to anti-α4β7-integrin therapy in humanized mice with colitis
por: Han, Bing, et al.
Publicado: (2023)

Central anorexigenic actions of bile acids are mediated by TGR5
por: Perino, Alessia, et al.
Publicado: (2021)

Fatty liver diseases, bile acids, and FXR
por: Zhu, Yan, et al.
Publicado: (2016)

Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists
por: Sepe, Valentina, et al.
Publicado: (2016)

The role of FXR and TGR5 in reversing and preventing progression of Western diet–induced hepatic steatosis, inflammation, and fibrosis in mice
por: Wang, Xiaoxin X., et al.
Publicado: (2022)

Multigenerational impacts of bile exposure are mediated by TGR5 signaling pathways
por: Baptissart, Marine, et al.
Publicado: (2018)

The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
por: Qi, Youchao, et al.
Publicado: (2022)

Novel FXR agonist nelumal A suppresses colitis and inflammation-related colorectal carcinogenesis
por: Miyazaki, Tsuneyuki, et al.
Publicado: (2021)

Effects of Bile Acids and the Bile Acid Receptor FXR Agonist on the Respiratory Rhythm in the In Vitro Brainstem Medulla Slice of Neonatal Sprague-Dawley Rats
por: Zhao, Cong, et al.
Publicado: (2014)

Deciphering the nuclear bile acid receptor FXR paradigm
por: Modica, Salvatore, et al.
Publicado: (2010)

Bile Acids, FXR, and Metabolic Effects of Bariatric Surgery
por: Noel, Olivier F., et al.
Publicado: (2016)

Bile Acids and FXR: Novel Targets for Liver Diseases
por: Stofan, Mary, et al.
Publicado: (2020)

Mutational Characterization of the Bile Acid Receptor TGR5 in Primary Sclerosing Cholangitis
por: Hov, Johannes R., et al.
Publicado: (2010)

Long-term Administration of Nuclear Bile Acid Receptor FXR Agonist Prevents Spontaneous Hepatocarcinogenesis in Abcb4(−/−) Mice
por: Cariello, Marica, et al.
Publicado: (2017)

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non–Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers
por: Badman, Michael K., et al.
Publicado: (2019)

TGR5 agonists induce peripheral and central hypersensitivity to bladder distension
por: Caldwell, Ashlee, et al.
Publicado: (2022)

TGR5 controls bile acid composition and gallbladder function to protect the liver from bile acid overload
por: Bidault-Jourdainne, Valeska, et al.
Publicado: (2020)

Identification of Andrographolide as an Agonist of Bile Acid TGR5 Receptor in a Cell Line to Demonstrate the Reduction in Hyperglycemia in Type-1 Diabetic Rats
por: Li, Yingxiao, et al.
Publicado: (2023)

Proteomics for the discovery of nuclear bile acid receptor FXR targets()
por: Gardmo, Cissi, et al.
Publicado: (2011)

Impact of bile acids on the growth of human cholangiocarcinoma via FXR
por: Dai, Jiaqi, et al.
Publicado: (2011)

Bile acid nuclear receptor FXR and digestive system diseases
por: Ding, Lili, et al.
Publicado: (2015)

Fxr signaling and microbial metabolism of bile salts in the zebrafish intestine
por: Wen, Jia, et al.
Publicado: (2021)

INT-767—A Dual Farnesoid-X Receptor (FXR) and Takeda G Protein-Coupled Receptor-5 (TGR5) Agonist Improves Survival in Rats and Attenuates Intestinal Ischemia Reperfusion Injury
por: Canovai, Emilio, et al.
Publicado: (2023)

Liver Capsule: FXR agonists against liver disease
por: Fuchs, Claudia D., et al.
Publicado: (2016)

Role of the bile acid receptor TGR5 (Gpbar-1) in liver damage and regeneration
por: Keitel, Verena, et al.
Publicado: (2014)

Circulating Bile Acids in Liver Failure Activate TGR5 and Induce Monocyte Dysfunction
por: Leonhardt, Julia, et al.
Publicado: (2021)

Optical control of the nuclear bile acid receptor FXR with a photohormone
por: Morstein, Johannes, et al.
Publicado: (2019)

Bile Acids, Microbiota, and Cystic Fibrosis: Channeling Intestinal FXR Signals
por: McHenry, Scott, et al.
Publicado: (2019)

SUMOylation inhibitors synergize with FXR agonists in combating liver fibrosis
por: Zhou, Jiyu, et al.
Publicado: (2020)

Cannot write session to /tmp/vufind_sessions/sess_tjfbdqacvigqo43e7svkovjcme