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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
20
Issue
11
Identifiers
DOI: 10.1016/j.bmcl.2010.04.038
Keywords
  • Click Chemistry
  • Neurotensin Receptor
  • Phosphopeptide
  • Peptide Heterodimer
Disciplines
  • Chemistry

Abstract

Abstract 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 IC50 values of 8.3μM and 0.7μM indicate only very low binding affinity of the neurotensin(8–13)-containing peptide heterodimers towards the NTR1.

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