Hybrid bombesin analogues: combining an agonist and an antagonist in defined distances for optimized tumor targeting.
J Am Chem Soc
; 135(45): 16793-6, 2013 Nov 13.
Article
em En
| MEDLINE
| ID: mdl-24175716
ABSTRACT
Radiolabeled hybrid ligands with defined distances between an agonist and an antagonist for the gastrin-releasing peptide receptor were found to have excellent tumor-targeting properties. Oligoprolines served as rigid scaffolds that allowed for tailoring distances of 10, 20, and 30 Å between the recognition elements. In vitro and in vivo studies revealed that the hybrid ligand with a distance of 20 Å between the recognition elements exhibits the highest yet observed tumor cell uptake and retention time in prostate cancer cells.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Próstata
/
Bombesina
/
Sistemas de Liberação de Medicamentos
/
Receptores da Bombesina
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
J Am Chem Soc
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Suíça