Design and Synthesis of Peptide YY Analogues with C-terminal Backbone Amide-to-Ester Modifications.
Basic Information
ID: ALA3098032
Journal: ACS Med Chem Lett
Title: Design and Synthesis of Peptide YY Analogues with C-terminal Backbone Amide-to-Ester Modifications.
Authors: Albertsen L, Andersen JJ, Paulsson JF, Thomsen JK, Norrild JC, Strømgaard K.
Abstract: Peptide YY (PYY) is a gut hormone that activates the G protein-coupled neuropeptide Y (NPY) receptors, and because of its appetite reducing actions, it is evaluated as an antiobesity drug candidate. The C-terminal tail of PYY is crucial for activation of the NPY receptors. Here, we describe the design and preparation of a series of PYY(3-36) depsipeptide analogues, in which backbone amide-to-ester modifications were systematically introduced in the C-terminal. Functional NPY receptor assays and circular dichroism revealed that the ψ(CONH) bonds at positions 30-31 and 33-34 are particularly important for receptor interaction and that the latter is implicated in Y2 receptor selectivity.
CiteXplore: 24900634
DOI: 10.1021/ml400335g
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