Chemistry:TUG-891

From HandWiki

TUG-891 is an experimental drug which acts as a potent and selective agonist for the free fatty acid receptor FFAR4 (GPR120). It has antiinflammatory effects and regulates metabolism, gastric peptide release and glucose homeostasis, and has been researched in animal models of conditions such as obesity, diabetes and atherosclerosis, as well as cancer.[1][2][3][4][5][6][7][8][9] TUG-891 was one of the first selective FFAR4 agonists developed and while it is useful for in vitro research, it has poor stability in vivo, and so numerous compounds have been developed with improved properties using TUG-891 as the parent compound.[10][11][12][13][14]

References

  1. ↑ "The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism". Molecular Pharmacology 84 (5): 710–725. November 2013. doi:10.1124/mol.113.087783. PMID 23979972. 
  2. ↑ "GPR120 agonism as a countermeasure against metabolic diseases". Drug Discovery Today 19 (5): 670–679. May 2014. doi:10.1016/j.drudis.2013.11.021. PMID 24315954. 
  3. ↑ "Pharmacological Tool Compounds for the Free Fatty Acid Receptor 4 (FFA4/GPR120)". Handbook of Experimental Pharmacology 236: 33–56. 2016. doi:10.1007/164_2016_60. ISBN 978-3-319-50692-0. PMID 27807695. 
  4. ↑ "The GPR120 agonist TUG-891 promotes metabolic health by stimulating mitochondrial respiration in brown fat". EMBO Molecular Medicine 10 (3). March 2018. doi:10.15252/emmm.201708047. PMID 29343498. 
  5. ↑ "The role of free-fatty acid receptor-4 (FFA4) in human cancers and cancer cell lines". Biochemical Pharmacology 150: 170–180. April 2018. doi:10.1016/j.bcp.2018.02.011. PMID 29452095. 
  6. ↑ "Novel GPR120 agonist TUG891 modulates fat taste perception and preference and activates tongue-brain-gut axis in mice". Journal of Lipid Research 61 (2): 133–142. February 2020. doi:10.1194/jlr.RA119000142. PMID 31806728. 
  7. ↑ "Elucidation of the roles of brown and brite fat genes: GPR120 is a modulator of brown adipose tissue function". Experimental Physiology 105 (8): 1201–1205. August 2020. doi:10.1113/EP087877. PMID 32144819. 
  8. ↑ "Anti-Atherosclerotic Potential of Free Fatty Acid Receptor 4 (FFAR4)". Biomedicines 9 (5): 467. April 2021. doi:10.3390/biomedicines9050467. PMID 33923318. 
  9. ↑ "TUG-891 inhibits neuronal endoplasmic reticulum stress and pyroptosis activation and protects neurons in a mouse model of intraventricular hemorrhage". Neural Regeneration Research 18 (10): 2278–2284. October 2023. doi:10.4103/1673-5374.369116. PMID 37056148. 
  10. ↑ "Novel GPR120 Agonists with Improved Pharmacokinetic Profiles for the Treatment of Type 2 Diabetes". Molecules (Basel, Switzerland) 26 (22): 6907. November 2021. doi:10.3390/molecules26226907. PMID 34833999. 
  11. ↑ "GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery". Journal of Medicinal Chemistry 64 (8): 4312–4332. April 2021. doi:10.1021/acs.jmedchem.0c01002. PMID 33843223. 
  12. ↑ "Discovery of Novel and Selective G-Protein Coupled Receptor 120 (GPR120) Agonists for the Treatment of Type 2 Diabetes Mellitus". Molecules (Basel, Switzerland) 27 (24): 9018. December 2022. doi:10.3390/molecules27249018. PMID 36558150. 
  13. ↑ "Novel Phenoxyalkanoic Acid Derivatives as Free Fatty Acid Receptor 4 Agonists for Treating Type 2 Diabetes Mellitus". International Journal of Molecular Sciences 25 (21). October 2024. doi:10.3390/ijms252111476. PMID 39519029. 
  14. ↑ "A high-throughput structural dynamics approach for identification of potential agonists of FFAR4 for type 2 diabetes mellitus therapy". Journal of Biomolecular Structure & Dynamics 43 (1): 176–196. January 2025. doi:10.1080/07391102.2023.2280707. PMID 37978906. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:TUG-891&oldid=4037741"