Ghrelin O-acyltransferase assays and inhibition.

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

    Research output: Contribution to journalReview article


    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)
    Pages (from-to)205-228
    Number of pages24
    JournalMethods in enzymology
    StatePublished - 2012

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Biology

    Fingerprint Dive into the research topics of 'Ghrelin O-acyltransferase assays and inhibition.'. Together they form a unique fingerprint.

  • Cite this

    Taylor, M. S., Hwang, Y., Hsiao, P. Y., Boeke, J. D., & Cole, P. A. (2012). Ghrelin O-acyltransferase assays and inhibition. Methods in enzymology, 514, 205-228.