Chemistry:GSK137647A

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GSK137647A (also called GSK137647) is an experimental drug which acts as a highly selective and moderately potent agonist for the free fatty acid receptor FFAR4 (GPR120).[1] It has antiinflammatory effects[2] and has been used to research the role of FFAR4 in various processes such as diabetes,[3][4] ulcerative colitis,[5] maintenance of bone density,[6] and cancer.[7]

References

  1. ↑ "Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)". Bioorganic & Medicinal Chemistry Letters 24 (14): 3100–3103. July 2014. doi:10.1016/j.bmcl.2014.05.012. PMID 24881566. 
  2. ↑ "GPR120/FFAR4 stimulation attenuates airway remodeling and suppresses IL-4- and IL-13-induced airway epithelial injury via inhibition of STAT6 and Akt". Biomedicine & Pharmacotherapy 168. December 2023. doi:10.1016/j.biopha.2023.115774. PMID 37924784. 
  3. ↑ "Insulinotropic effects of GPR120 agonists are altered in obese diabetic and obese non-diabetic states". Clinical Science 131 (3): 247–260. February 2017. doi:10.1042/CS20160545. PMID 27980130. 
  4. ↑ "Pharmacological potential of novel agonists for FFAR4 on islet and enteroendocrine cell function and glucose homeostasis". European Journal of Pharmaceutical Sciences 142. January 2020. doi:10.1016/j.ejps.2019.105104. PMID 31669388. https://pure.ulster.ac.uk/en/publications/pharmacological-potential-of-novel-agonists-for-ffar4-on-islet-an. 
  5. ↑ "Activation of free fatty acid receptors, FFAR1 and FFAR4, ameliorates ulcerative colitis by promote fatty acid metabolism and mediate macrophage polarization". International Immunopharmacology 130. March 2024. doi:10.1016/j.intimp.2024.111778. PMID 38432147. 
  6. ↑ "Effect of GSK-137647A, the first non-carboxylic FFA4 agonist, on the osteogenic and adipogenic differentiation of bone mesenchymal stem cells in db/db mice". The Journal of Pharmacy and Pharmacology 72 (3): 461–469. March 2020. doi:10.1111/jphp.13217. PMID 31858612. 
  7. ↑ "Synthetic free fatty acid receptor (FFAR) 2 agonist 4-CMTB and FFAR4 agonist GSK13764 inhibit colon cancer cell growth and migration and regulate FFARs expression in in vitro and in vivo models of colorectal cancer". Pharmacological Reports 76 (6): 1403–1414. December 2024. doi:10.1007/s43440-024-00667-5. PMID 39432182. 



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