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• W2000798857 abstract "DAG-lactones afford a synthetically accessible, high affinity platform for probing structure activity relationships at the C1 regulatory domain of protein kinase C (PKC). Given the central role of PKC isoforms in cellular signaling, along with their differential biological activities, a critical objective is the design of isoform selective ligands. Here, we report the synthesis of a series of DAG-lactones varying in their side chains, with a particular focus on linoleic acid derivatives. We evaluated their selectivity for PKC epsilon versus PKC alpha both under standard lipid conditions (100% phosphatidylserine, PS) as well as in the presence of a nuclear membrane mimetic lipid mixture (NML). We find that selectivity for PKC epsilon versus PKC alpha tended to be enhanced in the presence of the nuclear membrane mimetic lipid mixture and, for our lead compound, report a selectivity of 32-fold." @default.
• W2000798857 created "2016-06-24" @default.
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• W2000798857 date "2015-01-01" @default.
• W2000798857 modified "2023-10-18" @default.
• W2000798857 title "Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones)" @default.
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• W2000798857 doi "https://doi.org/10.1016/j.ejmech.2014.11.025" @default.
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