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