The status of Nrf2-based therapeutics： current perspectives and future prospects-中国Betway体育网页登陆

摘要 Thismini-reviewpresentstheauthors'visiononthecurrentstatusandfuturetrendsinthedevelopmentofneuroprotectiveagentsworkingviaactivationofnuclearfactorerythroid2-relatedfactor2(Nrf2),andinparticular,viadisruptionofNrf2-Keaplinteraction.Therearetwoopposite'chemical'mechanismsunderlyingsuchactivation:thefirstoneisanon-specificcovalentmodificationofKeap1thiols,resultinginsideeffectsofvariedseverity,andthesecondoneistheshiftoftheNrf2-Kelch-likeECHassociatedprotein-1(Keap1)bindingequilibriuminthepresenceofacompetitiveandchemicallybenigndisplacementagent.Atthispoint,nodisplacementactivatorsexhibitsufficientbiologicalactivityincomparisonwithcommonNrf2activatorsworkingviaKeaplthiolmodification.Hence,thehopeintherapeuticsisnowlinkedtotheFDAapproveddimethylfumarate,whosederivative,monomethylfumarate,aswedemonstratedrecently,ismuchlesstoxicbutequallybiologicallypotentandanidealcandidateforclinicaltrialsrightnow.AnewlyemergingplayerisanuclearinhibitorofNrf2,BTBdomainandCNChomolog1(Bach1).ThecommerciallydevelopedBachlinhibitorsarecurrentlyunderinvestigationinourlaboratoryshowingpromisingresults.Inourviewpoint,theperfectfuturedrugwillpresentthecombinationofadisplacementactivatorandBachlinhibitortoinsuresafetyandefficiencyofNrf2activation.

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The status of Nrf2-based therapeutics： current perspectives and future prospects

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