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

We substituted a truncated neuropeptide Y (NPY) analog, [Pro30, Tyr32, Leu34]NPY(28-36)NH2 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 Y1 receptors (NPY1R). Our data suggest that [Lys(DOTA)4]BVD15 (Ki = 63 ± 25 nM vs. Ki = 39 ± 34 nM for BVD15) is a potent NPY analog suitable for radiolabeling with metallo positron emitters for PET imaging of breast cancer.

Graphical abstract[Lys(DOTA)4]BVD15, a potent NPY Y1 analog suitable for radiolabeling with metallo positron emitters for PET imaging of breast cancer.Figure optionsDownload full-size imageDownload as PowerPoint slide