Bioconjugated chelates based on (methylpyridinyl)tacn: synthesis, 64Cu labeling and in vitro evaluation for prostate cancer targeting - Chimie Electrochimie Moléculaires et Chimie Analytique Accéder directement au contenu
Article Dans Une Revue Metallomics Année : 2022

Bioconjugated chelates based on (methylpyridinyl)tacn: synthesis, 64Cu labeling and in vitro evaluation for prostate cancer targeting

Axia Marlin
  • Fonction : Auteur
Ina Hierlmeier
  • Fonction : Auteur
Amaury Guillou
Mark Bartholomä
  • Fonction : Auteur
Véronique Patinec

Résumé

Abstract Three new bifunctional copper chelators based on the 1,4,7-triazacyclononane (tacn) platform have been synthesized and conjugated to peptide. The first one is constituted of the tacn with two methylpyridinyl and one methylthiazolyl carboxylic acid pendant arms, while, in the second and third ones, the macrocycle is functionalized by three methylpyridinyl groups, with an additional hexynoic acid chain on a carbon of one or two pyridine rings. These three bifunctional chelators have been conjugated to the antagonist JMV594 peptide for targeting the gastrin releasing peptide receptor (GRP-r), which is overexpressed in prostate cancer. The resulting monomeric bioconjugates have shown their efficiency to be radiolabeled with β+ emitter 64Cu, and the hydrophilicity and PC-3 cell internalisation properties of these radiolabeled conjugates have been studied. PC-3 cell binding affinity of mono- and dimeric metal-free and natCu metallated conjugates have been evaluated by IC50 measurements. The results demonstrate the potential of these methylpyridinyl tacn derivatives for radiopharmaceutical applications.

Domaines

Chimie Cancer
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Dates et versions

hal-03697656 , version 1 (17-06-2022)

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Citer

Axia Marlin, Ina Hierlmeier, Amaury Guillou, Mark Bartholomä, Raphaël Tripier, et al.. Bioconjugated chelates based on (methylpyridinyl)tacn: synthesis, 64Cu labeling and in vitro evaluation for prostate cancer targeting. Metallomics, 2022, ⟨10.1093/mtomcs/mfac036⟩. ⟨hal-03697656⟩
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