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Bioorg Med Chem Lett. 2010 Feb 1;20(3):950-3. doi: 10.1016/j.bmcl.2009.12.068. Epub 2009 Dec 23.

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

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1
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
DOI:
10.1016/j.bmcl.2009.12.068
[Indexed for MEDLINE]
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