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TUG-891

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TUG-891
Identifiers
  • 3-[4-[[5-fluoro-2-(4-methylphenyl)phenyl]methoxy]phenyl]propanoic acid
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC23H21FO3
Molar mass364.416 g·mol−1
3D model (JSmol)
  • CC1=CC=C(C=C1)C2=C(C=C(C=C2)F)COC3=CC=C(C=C3)CCC(=O)O
  • InChI=1S/C23H21FO3/c1-16-2-7-18(8-3-16)22-12-9-20(24)14-19(22)15-27-21-10-4-17(5-11-21)6-13-23(25)26/h2-5,7-12,14H,6,13,15H2,1H3,(H,25,26)
  • Key:LPGBXHWIQNZEJB-UHFFFAOYSA-N

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

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  1. ^ Hudson BD, Shimpukade B, Mackenzie AE, Butcher AJ, Pediani JD, Christiansen E, et al. (November 2013). "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. doi:10.1124/mol.113.087783. PMC 3807074. PMID 23979972.
  2. ^ Cornall LM, Mathai ML, Hryciw DH, McAinch AJ (May 2014). "GPR120 agonism as a countermeasure against metabolic diseases". Drug Discovery Today. 19 (5): 670–679. doi:10.1016/j.drudis.2013.11.021. PMID 24315954.
  3. ^ Hansen SV, Ulven T (2016). "Pharmacological Tool Compounds for the Free Fatty Acid Receptor 4 (FFA4/GPR120)". Handbook of Experimental Pharmacology. 236: 33–56. doi:10.1007/164_2016_60. ISBN 978-3-319-50692-0. PMID 27807695.
  4. ^ Schilperoort M, van Dam AD, Hoeke G, Shabalina IG, Okolo A, Hanyaloglu AC, et al. (March 2018). "The GPR120 agonist TUG-891 promotes metabolic health by stimulating mitochondrial respiration in brown fat". EMBO Molecular Medicine. 10 (3). doi:10.15252/emmm.201708047. PMC 5840546. PMID 29343498.
  5. ^ Senatorov IS, Moniri NH (April 2018). "The role of free-fatty acid receptor-4 (FFA4) in human cancers and cancer cell lines". Biochemical Pharmacology. 150: 170–180. doi:10.1016/j.bcp.2018.02.011. PMC 5866782. PMID 29452095.
  6. ^ Murtaza B, Hichami A, Khan AS, Shimpukade B, Ulven T, Ozdener MH, et al. (February 2020). "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. doi:10.1194/jlr.RA119000142. PMC 6997603. PMID 31806728.
  7. ^ Christian M (August 2020). "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. doi:10.1113/EP087877. PMC 8650997. PMID 32144819.
  8. ^ Kiepura A, Stachyra K, Olszanecki R (April 2021). "Anti-Atherosclerotic Potential of Free Fatty Acid Receptor 4 (FFAR4)". Biomedicines. 9 (5): 467. doi:10.3390/biomedicines9050467. PMC 8146529. PMID 33923318.
  9. ^ Wang HX, Liu C, Li YY, Cao Y, Zhao L, Zhao YJ, et al. (October 2023). "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. doi:10.4103/1673-5374.369116. PMC 10328290. PMID 37056148.
  10. ^ Ji G, Guo Q, Xue Q, Kong R, Wang S, Lei K, et al. (November 2021). "Novel GPR120 Agonists with Improved Pharmacokinetic Profiles for the Treatment of Type 2 Diabetes". Molecules. 26 (22). Basel, Switzerland: 6907. doi:10.3390/molecules26226907. PMC 8624523. PMID 34833999.
  11. ^ Carullo G, Mazzotta S, Vega-Holm M, Iglesias-Guerra F, Vega-Pérez JM, Aiello F, et al. (April 2021). "GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery". Journal of Medicinal Chemistry. 64 (8): 4312–4332. doi:10.1021/acs.jmedchem.0c01002. PMC 8154576. PMID 33843223.
  12. ^ Wang X, Li X, Wei S, Wang M, Xu Y, Hu W, et al. (December 2022). "Discovery of Novel and Selective G-Protein Coupled Receptor 120 (GPR120) Agonists for the Treatment of Type 2 Diabetes Mellitus". Molecules. 27 (24). Basel, Switzerland: 9018. doi:10.3390/molecules27249018. PMC 9781217. PMID 36558150.
  13. ^ Li X, Zhang X, Xie X, Dong T, Lv C, Guan R, et al. (October 2024). "Novel Phenoxyalkanoic Acid Derivatives as Free Fatty Acid Receptor 4 Agonists for Treating Type 2 Diabetes Mellitus". International Journal of Molecular Sciences. 25 (21): 11476. doi:10.3390/ijms252111476. PMC 11547093. PMID 39519029.
  14. ^ Jhinjharia D, Kaushik AC, Sahi S (January 2025). "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. doi:10.1080/07391102.2023.2280707. PMID 37978906.
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