Structure‐Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2

ChemMedChem ◽  
2021 ◽  
Author(s):  
Anders Højgaard Hansen ◽  
Henriette B. Christensen ◽  
Sunil K. Pandey ◽  
Eugenia Sergeev ◽  
Alice Valentini ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Free Fatty Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Acid Receptor ◽  
Structure Activity ◽  
Free Fatty Acid Receptor ◽  
Potent Antagonist ◽  
Fatty Acid Receptor

Design, synthesis and structure–activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker

2017 ◽  
Vol 25 (8) ◽  
pp. 2445-2450 ◽  
Author(s):  
Jianyong Yang ◽  
Zheng Li ◽  
Huilan Li ◽  
Chunxia Liu ◽  
Nasi Wang ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Free Fatty Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Design Synthesis ◽  
Acid Receptor ◽  
Structure Activity ◽  
Free Fatty Acid Receptor ◽  
Fatty Acid Receptor

scholarly journals Structure–Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators

2020 ◽  
Vol 63 (7) ◽  
pp. 3577-3595
Author(s):  
Elisabeth Rexen Ulven ◽  
Tezz Quon ◽  
Eugenia Sergeev ◽  
Natasja Barki ◽  
Matjaz Brvar ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Free Fatty Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Acid Receptor ◽  
Structure Activity ◽  
Free Fatty Acid Receptor ◽  
Fatty Acid Receptor

scholarly journals The Free Fatty Acid Receptor G Protein-coupled Receptor 40 (GPR40) Protects from Bone Loss through Inhibition of Osteoclast Differentiation

2013 ◽  
Vol 288 (9) ◽  
pp. 6542-6551 ◽  
Author(s):  
Fabien Wauquier ◽  
Claire Philippe ◽  
Laurent Léotoing ◽  
Sylvie Mercier ◽  
Marie-Jeanne Davicco ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Free Fatty Acid ◽  
Bone Loss ◽  
G Protein ◽  
Osteoclast Differentiation ◽  
G Protein Coupled Receptor ◽  
Acid Receptor ◽  
Free Fatty Acid Receptor ◽  
G Protein Coupled ◽  
Fatty Acid Receptor

Expression of free fatty acid receptor GPR40 in the neurogenic niche of adult monkey hippocampus

Hippocampus ◽  
2008 ◽  
Vol 18 (3) ◽  
pp. 326-333 ◽  
Author(s):  
Dexuan Ma ◽  
Li Lu ◽  
Nadezhda B. Boneva ◽  
Shogo Warashina ◽  
Desislav B. Kaplamadzhiev ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Free Fatty Acid ◽  
Acid Receptor ◽  
Neurogenic Niche ◽  
Free Fatty Acid Receptor ◽  
Fatty Acid Receptor

scholarly journals Regulation of Free Fatty Acid Receptor 4 on Inflammatory Gene Induced by LPS in Large Yellow Croaker (Larimichthys crocea)

2021 ◽  
Vol 12 ◽  
Author(s):  
Mengjiao Wu ◽  
Qingfei Li ◽  
Kangsen Mai ◽  
Qinghui Ai
Keyword(s):  
Fatty Acid ◽  
Free Fatty Acid ◽  
Mrna Expression ◽  
Head Kidney ◽  
Large Yellow Croaker ◽  
Larimichthys Crocea ◽  
Inflammatory Genes ◽  
Acid Receptor ◽  
Free Fatty Acid Receptor ◽  
Fatty Acid Receptor

Free fatty acid receptor 4 (FFAR4) plays a key role in regulating the inflammatory response in mammals. The present study aimed to investigate the function of large yellow croaker FFAR4 on inflammation. In the present study, ffar4 was widely expressed in 10 tissues of large yellow croaker including gill, head kidney and spleen. Further studies showed that treatment of head kidney macrophages with agonists (TUG891 or GSK137647A) or overexpression of ffar4 reduced the mRNA expression of pro-inflammatory genes induced by LPS, and increased the expression of pparγ. Treatment of macrophages with antagonist AH7614 increased the mRNA expression of pro-inflammatory genes induced by LPS, and decreased the mRNA expression of pparγ. In order to verify the immunomodulatory effect of PPARγ, PPARγ was overexpressed in macrophages which significantly reduced the mRNA expression of pro-inflammatory genes il6, il1β, il8, tnfα and cox2. Moreover, results of dual-luciferase assays showed that PPARγ downregulated the transcriptional activity of il6 and il1β promoters. In conclusion, FFAR4 showed anti-inflammatory effects on LPS-induced inflammation in large yellow croaker.

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