Preclinical Evaluation of Novel 64Cu-Labeled Gastrin-Releasing Peptide Receptor Bioconjugates for PET Imaging of Prostate Cancer

Autor:	Heather M. Hennkens, Rajendra P. Bandari, Antonio Shegani, Pavithra H.A. Kankanamalage, Marina Kuchuk, George Makris, Charles J. Smith
Rok vydání:	2021
Předmět:	Pharmacology chemistry.chemical_classification Biodistribution Organic Chemistry Biomedical Engineering Antagonist Pharmaceutical Science Bioengineering Peptide Ligand (biochemistry) Molecular biology In vitro chemistry Lipophilicity Gastrin-releasing peptide receptor Linker Biotechnology
Zdroj:	Bioconjugate Chemistry. 32:1290-1297
ISSN:	1520-4812 1043-1802
Popis:	We report herein the preclinical evaluation of new [64Cu]Cu-gastrin-releasing peptide receptor (GRPR)-targeting tracers, employing the potent peptide antagonist DPhe-Gln-Trp-Ala-VaI-Gly-His-Sta-Leu-NH2 conjugated to NOTA (in 1) or NODAGA (in 2) chelators via a 6-aminohexanoic acid linker. The Cu-1/2 metalated peptides were synthesized by reacting 1/2 with CuCl2 and were characterized by LC-ESI-MS and HR-ESI-MS. Cu-1/2 exhibited high GRPR-binding affinities with IC50 values
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::6cf2e9606aac540f0ffdc1d9b3dffad1 https://doi.org/10.1021/acs.bioconjchem.0c00656 Zobrazit plný text záznamu