Design of Stapled Oxyntomodulin Analogs Containing Functionalized Biphenyl Cross-Linkers.
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ABSTRACT: A panel of three lipid-modified, functionalized biphenyl cross-linkers (fBph) were synthesized and subsequently employed in the preparation of the stapled oxyntomodulin (OXM) analogs. In a luciferase-based reporter assay, these stapled OXM analogs showed varying degree of potency in activating GLP-1R and GCGR, presumably due to the disparate effect of the lipid chains on the local environment close to the ligand-receptor binding interface. In particular, the fBph-1 cross-linked peptide with the lipid chain attached to position-3 of the biphenyl cross-linker exhibited the highest dual agonist activity.
SUBMITTER: Tian Y
PROVIDER: S-EPMC6300064 | biostudies-literature | 2019 Jan
REPOSITORIES: biostudies-literature
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