Influences of hydrocarbon linkers on the receptor binding affinities of gonadotropin-releasing hormone peptides.
Bioorg Med Chem Lett
; 23(20): 5484-7, 2013 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-24018188
ABSTRACT
Three new DOTA-conjugated GnRH peptides with various hydrocarbon linkers were synthesized to evaluate the influences of the linkers on their receptor binding affinities. The hydrocarbon linker displayed a profound impact on the receptor binding affinities of DOTA-conjugated GnRH peptides. The Aun linker was better than Gaba, Ahx and Aoc linkers in retaining strong receptor binding affinity of the GnRH peptide. DOTA-Aun-(D-Lys(6)-GnRH) displayed 22.8 nM GnRH receptor binding affinity. (111)In-DOTA-Aun-(D-Lys(6)-GnRH) exhibited fast tumor uptake and urinary clearance in MDA-MB-231 human breast cancer-xenografted nude mice. The cellular and biological results provided an insight into the design of new GnRH peptides in the future.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Peptídeos
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Hormônio Liberador de Gonadotropina
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Hidrocarbonetos
Limite:
Animals
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Female
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Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article