Article
Insights into PPARγ Phosphorylation and Its Inhibition Mechanism.
Journal of medicinal chemistry - 14 May 2020
Montanari Roberta, Capelli Davide, Yamamoto Keiko, Awaishima Hirono, Nishikata Kimina, Barendregt Arjan, Heck Albert J R, Loiodice Fulvio, Altieri Fabio, Paiardini Alessandro, Grottesi Alessandro, Pirone Luciano, Pedone Emilia, Peiretti Franck, Brunel Jean Michel, Itoh Toshimasa, Pochetti Giorgio
Abstract excerpt
PPARγ represents a key target for the treatment of type 2 diabetes and metabolic syndrome. Synthetic antidiabetic drugs activating PPARγ are accompanied by serious undesirable side effects related to their agonism. In the search for new PPARγ regulators, inhibitors of PPARγ phosphorylation on S245 mediated by CDK5 represent an opportunity for the development of an improved generation of antidiabetic drugs acting...
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