Ghrelin O-Acyltransferase Assays and Inhibition

Martin S. Taylor, Yousang Hwang, Po Yuan Hsiao, Jef D. Boeke, Philip A. Cole

    Research output: Chapter in Book/Report/Conference proceedingChapter

    Abstract

    Ghrelin O-acyltransferase (GOAT) is responsible for catalyzing the attachment of the eight-carbon fatty acid octanoyl to the Ser3 side chain of the peptide ghrelin to generate the active form of this metabolic hormone. As such, GOAT is viewed as a potential therapeutic target for the treatment of obesity and diabetes mellitus. Here, we review recent progress in the development of cell and in vitro assays to measure GOAT action and the identification of several synthetic GOAT inhibitors. In particular, we discuss the design, synthesis, and characterization of the bisubstrate analog GO-CoA-Tat and its ability to modulate weight and blood glucose in mice. We also highlight current challenges and future research directions in our biomedical understanding of this fascinating ghrelin processing enzyme.

    Original languageEnglish (US)
    Title of host publicationMethods in Enzymology
    PublisherAcademic Press Inc.
    Pages205-228
    Number of pages24
    DOIs
    StatePublished - Jan 2012

    Publication series

    NameMethods in Enzymology
    Volume514
    ISSN (Print)0076-6879
    ISSN (Electronic)1557-7988

    Keywords

    • bisubstrate
    • design
    • ELISA
    • inhibitor
    • mechanism
    • metabolism
    • octanoyl-CoA
    • peptide
    • synthetic compound
    • weight

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Biology

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