Author/Authors :
Brenda L. Palucki، نويسنده , , Scott D. Feighner، نويسنده , , Sheng-Shung Pong، نويسنده , , Karen Kulju McKee، نويسنده , , Donna L. Hreniuk، نويسنده , , Carina Tan، نويسنده , , Andrew D. Howard، نويسنده , , Lex H. Y. Van der Ploeg، نويسنده , , Arthur A. Patchett، نويسنده , , Ravi P. Nargund، نويسنده ,
Abstract :
A series of small molecules derived from MK-0677, a potent synthetic GHS, mimicking the N-terminal Gly-Ser-O-(n-octanoyl)- -Ser-Phe segment of ghrelin was synthesized and tested in a binding and in a functional assay measuring intracellular calcium elevation in HEK-293 cells expressing hGHSR1a. Replacement of Phe in this tetrapeptide with a spiro(indoline-3,4′-piperidine) group, Gly-Ser with 2-aminoisobutyric acid, and O-(n-octanoyl)- -Ser with O-benzyl- -Ser provided synthetic GHS agonists with similar functional potency as ghrelin.
