In silico modelling of prostacyclin and other lipid mediators to nuclear receptors reveal novel thyroid hormone receptor antagonist properties
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- 作者：Noelia Perez Diaz ; Mire Zloh ; Pryank Patel ; Louise S. Mackenzie ; l.mackenzie2@herts.ac.uk" class="auth_mail" title="E-mail the corresponding author ; louisemackenzie75@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：MLS ; MLS000389544 ; NSAID ; non-steroidal anti-inflammatory drug ; PPARβ/δ ; peroxisome proliferator activated receptor ; PGI2 ; prostacyclin ; PAH ; pulmonary artery hypertension ; T3 ; triiodothyronine ; TRα ; thyroid hormone α receptor ; TRβ ; thyroid hormone β receptor
- 刊名：Prostaglandins and Other Lipid Mediators
- 出版年：2016
- 出版时间：January 2016
- 年：2016
- 卷：122
- 期：Complete
- 页码：18-27
- 全文大小：1978 K
文摘
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In silico screening predicted that PGI2, beraprost, and GW0742 has the potential to bind to thyroid hormone β receptor (TRβ) and TRα.
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Docking analysis predicts that that PGI2, beraprost, and GW0742 binds to residues thought to have allosteric control on the TR ligand binding site.
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Luciferase reporter assays confirmed that beraprost and GW0742 display TRβ and TRα antagonistic properties.
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Beraprost and GW0742 inhibit triiodothyronine (T3) induced vasodilation of rat mesenteric arteries.
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Out data suggests that PGI2, has the ability to affect the long term function of cells through binding to and inactivating TRβ.