Bioorg Med Chem Lett. 2010 Feb 1;20(3):950-3. Epub 2009 Dec 23.

[Lys(DOTA)4]BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.

Guérin B, Dumulon-Perreault V, Tremblay MC, Ait-Mohand S, Fournier P, Dubuc C, Authier S, Bénard F.

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Department of Nuclear Medicine and Radiobiology, Centre d'Imagerie Moléculaire de Sherbrooke, Université de Sherbrooke, Québec, Canada. brigitte.guerin2@USherbrooke.ca

Abstract

We substituted a truncated neuropeptide Y (NPY) analog, [Pro(30), Tyr(32), Leu(34)]NPY(28-36)NH(2) also called BVD15, at various positions with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7-10-tetraacetic acid) and evaluated the effect of the coupling position with the binding affinity for NPY Y(1) receptors (NPY1R). Our data suggest that [Lys(DOTA)(4)]BVD15 (K(i)=63+/-25 nM vs. K(i)=39+/-34 nM for BVD15) is a potent NPY analog suitable for radiolabeling with metallo positron emitters for PET imaging of breast cancer.

PMID:: 20042335; [PubMed - indexed for MEDLINE]

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