Abstract: Small molecule ghrelin O-acyltransferase inhibitors found using an assay to detect ghrelin O-acyltransferase activity using an acrylodan-labeled peptide mimic of ghrelin that provides for high-throughput screening for ghrelin O-acyltransferase inhibitors and detection via high performance liquid chromatography. The newly discovered class of synthetic triterpenoids efficiently inhibits ghrelin acylation by GOAT and function as covalent reversible inhibitors of GOAT. In cell studies, the most potent members of this family of compounds efficiently block ghrelin acylation at submicromolar concentrations and offer a foundation for continued development and evaluation of novel hGOAT inhibitors as therapeutics targeting disorders such obesity, type II diabetes, gastroparesis, and Prader-Willi syndrome.

Abstract: Grhelin O-acyltransferase inhibitors using a triazole linkage to incorporate aromatic and alkyl substituents to mimic the natural octanoyl group attached to ghrelin. Inhibitors include a triazole portion, an alkyl linker, and a hydrophobic aromatic group on a side chain. The hydrophobic aromatic group may include various length alkyl linkers.

Abstract: An assay to detect ghrelin O-acyltransferase activity using an acrylodan-labeled peptide mimic of ghrelin that provides for high-throughput screening for ghrelin O-acyltransferase inhibitors and detection via high performance liquid chromatography. Alternatively, the assay for ghrelin acylation may be based on a synthetic peptide substrate that mimics the N-terminal sequence of ghrelin and has an environmentally-sensitive fluorophore attached to its C-terminal amino acid through chemoselective ligation.

Abstract: Grhelin O-acyltransferase inhibitors using a triazole linkage to incorporate aromatic and alkyl substituents to mimic the natural octanoyl group attached to ghrelin. Inhibitors include a triazole portion, an alkyl linker, and a hydrophobic aromatic group on a side chain. The hydrophobic aromatic group may include various length alkyl linkers.

Abstract: An assay to detect ghrelin O-acyltransferase activity using an acrylodan-labeled peptide mimic of ghrelin that provides for high-throughput screening for ghrelin O-acyltransferase inhibitors and detection via high performance liquid chromatography. Alternatively, the assay for ghrelin acylation may be based on a synthetic peptide substrate that mimics the N-terminal sequence of ghrelin and has an environmentally-sensitive fluorophore attached to its C-terminal amino acid through chemoselective ligation.