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Paper(s) concerning Rocaglate-Derived-beta-Lactone-5

1 reference(s) found.
Listing paper details in reverse chronological order.
We are grateful to Keith Bradnam for improvment of this script

Title: Remodeling natural products: chemistry and serine hydrolase activity of a rocaglate-derived beta-lactone
Lajkiewicz NJ, Cognetta AB, 3rd, Niphakis MJ, Cravatt BF, Porco JA, Jr.
Ref: Journal of the American Chemical Society, 136:2659, 2014 : PubMed
Abstract


ESTHER: Lajkiewicz_2014_J.Am.Chem.Soc_136_2659
PubMedSearch: Lajkiewicz 2014 J.Am.Chem.Soc 136 2659
PubMedID: 24447064
Gene_locus related to this paper: human-ABHD10, human-ACOT1, human-ACOT2, human-CTSA, human-SCPEP1, mouse-abhda
Inhibitor(s) related to this paper: Rocaglate-Derived-beta-Lactone-5

Abstract

Flavaglines are a class of natural products with potent insecticidal and anticancer activities. beta-Lactones are a privileged structural motif found in both therapeutic agents and chemical probes. Herein, we report the synthesis, unexpected light-driven di-epimerization, and activity-based protein profiling of a novel rocaglate-derived beta-lactone. In addition to in vitro inhibition of the serine hydrolases ABHD10 and ACOT1/2, the most potent beta-lactone enantiomer was also found to inhibit these enzymes, as well as the serine peptidases CTSA and SCPEP1, in PC3 cells.