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Issue 28, 2015
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Triblock peptide–linker–lipid molecular design improves potency of peptide ligands targeting family B G protein-coupled receptors

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Abstract

Two peptide–linker–lipid constructs were designed and prepared which target the parathyroid hormone 1 receptor, a family B G protein-coupled receptor. Both show increased agonist activity in a cell-based assay. The lipid moiety enables the formation of micelle-like nanostructures, which is shown to hinder proteolytic digestion and is expected to reduce renal clearance.

Graphical abstract: Triblock peptide–linker–lipid molecular design improves potency of peptide ligands targeting family B G protein-coupled receptors

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The article was received on 13 Jan 2015, accepted on 18 Feb 2015 and first published on 18 Feb 2015


Article type: Communication
DOI: 10.1039/C5CC00301F
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Citation: Chem. Commun., 2015,51, 6157-6160

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    Triblock peptide–linker–lipid molecular design improves potency of peptide ligands targeting family B G protein-coupled receptors

    Y. Liu, Y. Cai, W. Liu, X. Li, E. Rhoades and E. C. Y. Yan, Chem. Commun., 2015, 51, 6157
    DOI: 10.1039/C5CC00301F

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