Synthesis of a Coumarin-Based PPARγ Fluorescence Probe for Competitive Binding Assay
Peroxisome proliferator-activated receptor γ (PPARγ) is a molecular target of metabolic syndrome and inflammatory disease. PPARγ is an important nuclear receptor and numerous PPARγ ligands were developed to date; thus, efficient assay methods are important. Here, we investigated the incorporation of...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-04-01
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| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/22/8/4034 |
| Summary: | Peroxisome proliferator-activated receptor γ (PPARγ) is a molecular target of metabolic syndrome and inflammatory disease. PPARγ is an important nuclear receptor and numerous PPARγ ligands were developed to date; thus, efficient assay methods are important. Here, we investigated the incorporation of 7-diethylamino coumarin into the PPARγ agonist rosiglitazone and used the compound in a binding assay for PPARγ. PPARγ-ligand-incorporated 7-methoxycoumarin, <b>1</b>, showed weak fluorescence intensity in a previous report. We synthesized PPARγ-ligand-incorporating coumarin, <b>2</b>, in this report, and it enhanced the fluorescence intensity. The PPARγ ligand <b>2</b> maintained the rosiglitazone activity. The obtained partial agonist <b>6</b> appeared to act through a novel mechanism. The fluorescence intensity of <b>2</b> and <b>6</b> increased by binding to the ligand binding domain (LBD) of PPARγ and the affinity of reported PPARγ ligands were evaluated using the probe. |
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| ISSN: | 1661-6596 1422-0067 |