Spiro(indoline-3,4′-piperidine) growth hormone secretagogues as ghrelin mimetics

Add time:09/29/2019    Source:infona.pl

A series of small molecules derived from MK-0677, a potent synthetic GHS, mimicking the N-terminal Gly-Ser-O-(n-octanoyl)-l-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)-l-Ser with O-benzyl-d-Ser provided synthetic GHS agonists with similar functional potency as ghrelin.

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