Triblock Peptide–linker–lipid Molecular Design Improves Potency Of ...

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From the journal:

Chemical Communications

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

Check for updates Yuting Liu,‡a Yingying Cai,‡a Wei Liu,a Xiao-Han Li,a Elizabeth Rhoadesbc and Elsa C. Y. Yan*a Author affiliations

* Corresponding authors

a Department of Chemistry, Yale University, New Haven, CT 06520, USA E-mail: elsa.yan@yale.edu

b Department of Molecular Biophysics and Biochemistry, Yale University, New Haven, CT 06520, USA

c Department of Physics, Yale University, New Haven, CT 06520, USA

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
  • This article is part of the themed collection: Identification and Optimization of GPCR Ligands in the 21st Century
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Supplementary files

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Article information

DOI https://doi.org/10.1039/C5CC00301F Article type Communication Submitted 13 Jan 2015 Accepted 18 Feb 2015 First published 18 Feb 2015

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Chem. Commun., 2015,51, 6157-6160 BibTex EndNote MEDLINE ProCite ReferenceManager RefWorks RIS

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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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