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.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Breast Neoplasms / diagnostic imaging
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Breast Neoplasms / metabolism*
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Cell Line
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Cell Line, Tumor
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Drug Design*
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Female
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Heterocyclic Compounds, 1-Ring / chemical synthesis*
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Heterocyclic Compounds, 1-Ring / metabolism*
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Humans
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Neuropeptide Y / analogs & derivatives*
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Neuropeptide Y / metabolism*
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Radionuclide Imaging
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Radiopharmaceuticals / chemical synthesis
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Receptors, Neuropeptide Y / analysis
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Receptors, Neuropeptide Y / metabolism*
Substances
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DOTA4 compound
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Heterocyclic Compounds, 1-Ring
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Neuropeptide Y
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Radiopharmaceuticals
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Receptors, Neuropeptide Y
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neuropeptide Y-Y1 receptor