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Issue 8, 2010
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Oligoproline helices as structurally defined scaffolds for oligomeric G protein-coupled receptor ligands

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Abstract

Oligoprolines (OPs) are used as rigid backbone scaffolds for the design of oligomeric ligands that target specific G protein-coupled receptors. The OPs were designed to vary in length, the position and number of the ligand-functionalized residues incorporated. For all synthesized compounds a typical PP type II helix was evidenced by circular dichroism indicating that decoration of the helix with large ligands did not affect the helical conformation. Pharmacological evaluation revealed that oligomerization of an agonist with the use of an oligoproline scaffold showed an increase in potency when compared to the monomeric counterparts.

Graphical abstract: Oligoproline helices as structurally defined scaffolds for oligomeric G protein-coupled receptor ligands

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Publication details

The article was received on 10 Nov 2009, accepted on 21 Jan 2010 and first published on 22 Feb 2010


Article type: Paper
DOI: 10.1039/B923556F
Citation: Org. Biomol. Chem., 2010,8, 1881-1884
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    Oligoproline helices as structurally defined scaffolds for oligomeric G protein-coupled receptor ligands

    K. M. Bonger, V. V. Kapoerchan, G. M. Grotenbreg, C. J. van Koppen, C. M. Timmers, G. A. van der Marel and H. S. Overkleeft, Org. Biomol. Chem., 2010, 8, 1881
    DOI: 10.1039/B923556F

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