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Literature DB >> 24881566

Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).

Steven M Sparks¹, Grace Chen², Jon L Collins³, Dana Danger³, Steven T Dock³, Channa Jayawickreme², Stephen Jenkinson⁴, Christopher Laudeman⁴, M Anthony Leesnitzer², Xi Liang³, Patrick Maloney⁴, David C McCoy⁴, David Moncol², Vincent Rash², Thomas Rimele², Padmaja Vulimiri², James M Way³, Sean Ross³.

Abstract

The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.

Entities: Chemical Gene

Keywords: FFA4; Free fatty acid receptor 4; Free fatty acid receptor 4 agonist; Free fatty acid receptor 4 antagonist; GPR120

Mesh：

Substances：

Year: 2014 PMID： 24881566 DOI： 10.1016/j.bmcl.2014.05.012

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

27 in total

1. Linoleic acid induces migration and invasion through FFAR4- and PI3K-/Akt-dependent pathway in MDA-MB-231 breast cancer cells.

Authors: Nathalia Serna-Marquez; Ricardo Diaz-Aragon; Emmanuel Reyes-Uribe; Pedro Cortes-Reynosa; Eduardo Perez Salazar
Journal: Med Oncol Date: 2017-04-29 Impact factor: 3.064

2. Free-fatty acid receptor-4 (FFA4) modulates ROS generation and COX-2 expression via the C-terminal β-arrestin phosphosensor in Raw 264.7 macrophages.

Authors: Ameneh Cheshmehkani; Ilya S Senatorov; Jyothi Dhuguru; Ola Ghoneim; Nader H Moniri
Journal: Biochem Pharmacol Date: 2017-09-21 Impact factor: 5.858

3. Functional expression of the free fatty acids receptor-1 and -4 (FFA1/GPR40 and FFA4/GPR120) in bovine endometrial cells.

Authors: Pamela Valenzuela; Stefanie Teuber; Carolina Manosalva; Pablo Alarcón; Carlos D Figueroa; Marcelo Ratto; Rafael A Burgos; Maria A Hidalgo
Journal: Vet Res Commun Date: 2019-06-11 Impact factor: 2.459

4. Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.

Authors: Xuqing Zhang; Chaozhong Cai; Zhihua Sui; Mark Macielag; Yuanping Wang; Wen Yan; Arthur Suckow; Hong Hua; Austin Bell; Peter Haug; Wilma Clapper; Celia Jenkinson; Joseph Gunnet; James Leonard; William V Murray
Journal: ACS Med Chem Lett Date: 2017-07-27 Impact factor: 4.345

Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).

1. Linoleic acid induces migration and invasion through FFAR4- and PI3K-/Akt-dependent pathway in MDA-MB-231 breast cancer cells.

2. Free-fatty acid receptor-4 (FFA4) modulates ROS generation and COX-2 expression via the C-terminal β-arrestin phosphosensor in Raw 264.7 macrophages.

3. Functional expression of the free fatty acids receptor-1 and -4 (FFA1/GPR40 and FFA4/GPR120) in bovine endometrial cells.

4. Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.

Review 5. Signaling through Free Fatty Acid Receptor 4 Attenuates Cardiometabolic Disease.

Review 6. The role of free-fatty acid receptor-4 (FFA4) in human cancers and cancer cell lines.

7. GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.

Review 8. Anti-Atherosclerotic Potential of Free Fatty Acid Receptor 4 (FFAR4).

9. GPR120 signaling controls amyloid-β degrading activity of matrix metalloproteinases.

Review 10. Long Chain Fatty Acids as Modulators of Immune Cells Function: Contribution of FFA1 and FFA4 Receptors.