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Barnett, B.P.* ; Hwang, Y.* ; Taylor, M.S.* ; Kirchner, H.* ; Pfluger, P.T.* ; Bernard, V.* ; Lin, Y.Y.* ; Bowers, E.M.* ; Mukherjee, C.* ; Song, W.J.* ; Longo, P.A.* ; Leahy, D.J.* ; Hussain, M.A.* ; Tschöp, M.H.* ; Boeke, J.D.* ; Cole, P.A.*

Glucose and weight control in mice with a designed ghrelin O-acyltransferase inhibitor.

Science 330, 1689-1692 (2010)
Postprint DOI PMC
Open Access Green
Ghrelin is a gastric peptide hormone that stimulates weight gain in vertebrates. The biological activities of ghrelin require octanoylation of the peptide on Ser(3), an unusual posttranslational modification that is catalyzed by the enzyme ghrelin O-acyltransferase (GOAT). Here, we describe the design, synthesis, and characterization of GO-CoA-Tat, a peptide-based bisubstrate analog that antagonizes GOAT. GO-CoA-Tat potently inhibits GOAT in vitro, in cultured cells, and in mice. Intraperitoneal administration of GO-CoA-Tat improves glucose tolerance and reduces weight gain in wild-type mice but not in ghrelin-deficient mice, supporting the concept that its beneficial metabolic effects are due specifically to GOAT inhibition. In addition to serving as a research tool for mapping ghrelin actions, GO-CoA-Tat may help pave the way for clinical targeting of GOAT in metabolic diseases.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Sprache englisch
Veröffentlichungsjahr 2010
HGF-Berichtsjahr 2010
ISSN (print) / ISBN 0036-8075
e-ISSN 1095-9203
Zeitschrift Science
Quellenangaben Band: 330, Heft: 6011, Seiten: 1689-1692 Artikelnummer: , Supplement: ,
Verlag American Association for the Advancement of Science (AAAS)
Begutachtungsstatus Peer reviewed
Institut(e) Institute of Diabetes and Obesity (IDO)
POF Topic(s) 30201 - Metabolic Health
Forschungsfeld(er) Helmholtz Diabetes Center
PSP-Element(e) G-502200-001
DOI 10.1126/science.1196154
WOS ID 000285390500070
PubMed ID 21097901
Erfassungsdatum 2010-12-31
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