Importance of the Proximity and Orientation of Ligand-Linkage to the Design of Cinnamate-GW9662 Hybrid Compounds as Covalent PPARγ Agonists

Importance of the Proximity and Orientation of Ligand-Linkage to the Design of Cinnamate-GW9662 Hybrid Compounds as Covalent PPARγ Agonists

Covalent agonists of PPARγ cause unique receptor conformational changes and behave as selective PPARγ modulators, whereas there are few covalent agonists other than endogenous unsaturated fatty acids metabolites. Previously, we established a cell-based strategy to identify new PPAR...

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Bibliographic Details
Main Authors: Yuki Utsugi, Hirona Kobuchi, Yukio Kawamura, Ahmed Salahelden Aboelhamd Atito, Masaya Nagao, Hiroko Isoda, Yusaku Miyamae
Format: Article
Language:English
Published: MDPI AG 2019-05-01
Series:Molecules
Subjects:
PPARγ
covalent agonist
ligand-linkage
structure-activity relationship
Online Access:https://www.mdpi.com/1420-3049/24/10/2019

Internet

https://www.mdpi.com/1420-3049/24/10/2019

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