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- Basic Research
- GPR40 Agonism Modulates Inflammatory Reactions in Vascular Endothelial Cells
- Joo Won Kim, Eun Roh, Kyung Mook Choi, Hye Jin Yoo, Hwan-Jin Hwang, Sei Hyun Baik
- Diabetes Metab J. 2022;46(3):506-511. Published online January 24, 2022
- DOI: https://doi.org/10.4093/dmj.2021.0092
- 6,097 View
- 250 Download
- 12 Web of Science
- 12 Crossref
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Abstract
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ePub - Endothelial dysfunction is strongly linked with inflammatory responses, which can impact cardiovascular disease. Recently, G protein-coupled receptor 40 (GPR40) has been investigated as a modulator of metabolic stress; however, the function of GPR40 in vascular endothelial cells has not been reported. We analyzed whether treatment of GPR40-specific agonists modulated the inflammatory responses in human umbilical vein endothelial cells (HUVECs). Treatment with LY2922470, a GPR40 agonist, significantly reduced lipopolysaccharide (LPS)-mediated nuclear factor-kappa B (NF-κB) phosphorylation and movement into the nucleus from the cytosol. However, treatment with another GPR40 agonist, TAK875, did not inhibit LPS-induced NF-κB activation. LPS treatment induced expression of adhesion molecules vascular cell adhesion molecule-1 (VCAM-1) and intercellular adhesion molecule-1 (ICAM-1) and attachment of THP-1 cells to HUVECs, which were all decreased by LY2922470 but not TAK875. Our results showed that ligand-dependent agonism of GPR40 is a promising therapeutic target for overcoming inflammatory reactions in the endothelium.
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Citations
Citations to this article as recorded by
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Cell Reports.2024; 43(10): 114858. CrossRef - Recent Developments in Drug Design of Oral Synthetic Free Fatty Acid Receptor 1 Agonists
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Drug Design, Development and Therapy.2024; Volume 18: 5961. CrossRef - GPR40 deficiency worsens metabolic syndrome‐associated periodontitis in mice
Yanchun Li, Zhongyang Lu, Cameron L. Kirkwood, Keith L. Kirkwood, Stephen A. Wank, Ai‐Jun Li, Maria F. Lopes‐Virella, Yan Huang
Journal of Periodontal Research.2023; 58(3): 575. CrossRef - Signaling pathways and intervention for therapy of type 2 diabetes mellitus
Rong Cao, Huimin Tian, Yu Zhang, Geng Liu, Haixia Xu, Guocheng Rao, Yan Tian, Xianghui Fu
MedComm.2023;[Epub] CrossRef - G Protein-Coupled Receptor 40 Agonist LY2922470 Alleviates Ischemic-Stroke-Induced Acute Brain Injury and Functional Alterations in Mice
Yingyu Lu, Wanlu Zhou, Qinghua Cui, Chunmei Cui
International Journal of Molecular Sciences.2023; 24(15): 12244. CrossRef - AM1638, a GPR40-Full Agonist, Inhibited Palmitate- Induced ROS Production and Endoplasmic Reticulum Stress, Enhancing HUVEC Viability in an NRF2-Dependent Manner
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Endocrinology and Metabolism.2023; 38(6): 760. CrossRef - Learn from failures and stay hopeful to GPR40, a GPCR target with robust efficacy, for therapy of metabolic disorders
Hong-Ping Guan, Yusheng Xiong
Frontiers in Pharmacology.2022;[Epub] CrossRef
- Synthetic GPR40/FFAR1 agonists: An exhaustive survey on the most recent chemical classes and their structure-activity relationships
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