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Protolichesterinic acid derivatives: α-methylene-γ-lactones as potent dual activators of PPARγ and Nrf2 transcriptional factors.

Abstract : PPARγ and Nrf2 are important transcriptional factors involved in many signaling pathways, especially in the anti-infectious response of macrophages. Compounds bearing a Michael acceptor moiety are well known to activate such transcriptional factors, we thus evaluated the potency of α,β-unsaturated lactones synthesized using fluorous phase organic synthesis. Compounds were first screened for their cytotoxicity in order to select lactones for PPARγ and Nrf2 activation evaluation. Among them, two α-methylene-γ-lactones were identified as potent dual activators of PPARγ and Nrf2 in macrophages.
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https://hal-univ-rennes1.archives-ouvertes.fr/hal-01114513
Contributor : Laurent Jonchère <>
Submitted on : Monday, February 9, 2015 - 3:16:51 PM
Last modification on : Thursday, March 5, 2020 - 2:06:31 PM

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Anne-Cécile Le Lamer, Hélène Authier, Isabelle Rouaud, Agnès Coste, Joël Boustie, et al.. Protolichesterinic acid derivatives: α-methylene-γ-lactones as potent dual activators of PPARγ and Nrf2 transcriptional factors.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (16), pp.3819-22. ⟨10.1016/j.bmcl.2014.06.062⟩. ⟨hal-01114513⟩

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