Structure-function studies on the new growth hormone-releasing peptide, ghrelin: minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a
作者： Maria A. Bednarek , Scott D. Feighner , Sheng-Shung Pong , Karen Kulju McKee , Donna L. Hreniuk
DOI: 10.1021/JM0001727
关键词: Growth hormone secretagogue 、 Biochemistry 、 Receptor 、 Growth hormone secretagogue receptor 、 Chemistry 、 Endocrinology 、 Peptide hormone 、 Internal medicine 、 Ghrelin 、 Ghrelin O-acyltransferase 、 Secretagogue 、 Agonist
摘要: The recently discovered growth hormone secretagogue, ghrelin, is a potent agonist at the human secretagogue receptor 1a (hGHSR1a). To elucidate structural features of this peptide necessary for efficient binding to and activation receptor, several analogues ghrelin with various aliphatic or aromatic groups in side chain residue 3, short peptides derived from were prepared tested assay an measuring intracellular calcium elevation HEK-293 cells expressing hGHSR1a. Bulky hydrophobic 3 turned out be essential maximum activity. Also, encompassing first 4 5 residues found functionally activate hGHSR1a about as efficiently full-length ghrelin. Thus entire sequence not activity: Gly-Ser-Ser(n-octanoyl)-Phe segment appears constitute "active core" required potency
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