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

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

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.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Breast Neoplasms / diagnostic imaging
  • Breast Neoplasms / metabolism*
  • Cell Line
  • Cell Line, Tumor
  • Drug Design*
  • Female
  • Heterocyclic Compounds, 1-Ring / chemical synthesis*
  • Heterocyclic Compounds, 1-Ring / metabolism*
  • Humans
  • Neuropeptide Y / analogs & derivatives*
  • Neuropeptide Y / metabolism*
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Receptors, Neuropeptide Y / analysis
  • Receptors, Neuropeptide Y / metabolism*

Substances

  • DOTA4 compound
  • Heterocyclic Compounds, 1-Ring
  • Neuropeptide Y
  • Radiopharmaceuticals
  • Receptors, Neuropeptide Y
  • neuropeptide Y-Y1 receptor