Journal
BIOCONJUGATE CHEMISTRY
Volume 27, Issue 9, Pages 2166-2175Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.6b00376
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Funding
- CRC for Biomedical Imaging Development (CRC-BID), Australia
- Australian Postgraduate Award scholarship
- Nottingham-Monash PhD program
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Traceable truncated Neuropeptide Y (NPY) analogues with Y-1 receptor (Y1R) affinity and selectivity are highly desirable tools in studying receptor location, regulation, and biological functions. A range of fluorescently labeled analogues of a reported Y1R/Y4R preferring ligand BVD-15 have been prepared and evaluated using high content imaging techniques. One peptide, [Lys(2)(sCy5), Arg(4)]BVD-15, was characterized as an Y1R antagonist with a pK(D) of 7.2 measured by saturation analysis using fluorescent imaging. The peptide showed 8-fold lower affinity for Y4R (pK(D) = 6.2) and was a partial agonist at this receptor. The suitability of [Lys(2)(sCy5), Arg(4)]BVD-15 for Y1R and Y4R competition binding experiments was also demonstrated in intact cells. The nature of the label was shown to be critical with replacement of sCyS by the more hydrophobic Cy5.5 resulting in a switch from Y1R antagonist to Y1R partial agonist.
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