Synthesis of neurotensin(8-13)-phosphopeptide heterodimers via click chemistry.
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.
Richter
Susan
S
Institute of Radiopharmacy, Forschungszentrum Dresden-Rossendorf e.V., Bautzner Landstrasse 400, 01328 Dresden, Germany.
Ramenda
Theres
T
Bergmann
Ralf
R
Kniess
T
T
Steinbach
Joerg
J
Pietzsch
Jens
J
Wuest
Frank
F
D002851:Chromatography, High Pressure Liquid; D019281:Dimerization; D009496:Neurotensin / Q000737:chemistry*; D010446:Peptide Fragments / Q000737:chemistry*; D010748:Phosphopeptides / Q000138:chemical synthesis* / Q000737:chemistry
D010446:Peptide Fragments; D010748:Phosphopeptides; D009496:Neurotensin; C054381:neurotensin (8-13)