Synthesis of neurotensin(8-13)-phosphopeptide heterodimers via click chemistry

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3306-9. doi: 10.1016/j.bmcl.2010.04.038. Epub 2010 Apr 14.


Two neurotensin(8-13)-containing peptide heterodimers were prepared via copper(I)-mediated click chemistry. The resulting peptide dimers could be obtained in 28-31% yield after HPLC purification. Neurotensin(8-13)-containing peptide dimers were used in an in vitro binding assay to determine binding affinity towards the neurotensin receptor-1 (NTR1). The determined IC(50) values of 8.3 microM and 0.7 microM indicate only very low binding affinity of the neurotensin(8-13)-containing peptide heterodimers towards the NTR1.

MeSH terms

  • Chromatography, High Pressure Liquid
  • Dimerization
  • Neurotensin / chemistry*
  • Peptide Fragments / chemistry*
  • Phosphopeptides / chemical synthesis*
  • Phosphopeptides / chemistry


  • Peptide Fragments
  • Phosphopeptides
  • Neurotensin
  • neurotensin (8-13)