Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Eur J Med Chem ; 51: 184-92, 2012 May.
Artigo em Inglês | MEDLINE | ID: mdl-22424612

RESUMO

The chemokine receptor CXCR7 is an atypical G protein-coupled receptor as it preferentially signals through the ß-arrestin pathway rather than through G proteins. CXCR7 is thought to be of importance in cancer and the development of CXCR7-targeting ligands is of huge importance to further elucidate the pharmacology and the therapeutic potential of CXCR7. In the present study, we synthesized 24 derivatives based on a compound scaffold patented by Chemocentryx and obtained CXCR7 ligands with pK(i) values ranging from 5.3 to 8.1. SAR studies were supported by computational 3D Fingerprint studies, revealing several important affinity descriptors. Two key compounds (29 and 30, VUF11207 and VUF11403) were found to be high-potency ligands that induce recruitment of ß-arrestin2 and subsequent internalization of CXCR7, making them important tool compounds in future CXCR7 research.


Assuntos
Amidas/química , Técnicas de Química Sintética , Modelos Moleculares , Receptores CXCR/agonistas , Estireno/química , Estireno/farmacologia , Células HEK293 , Humanos , Conformação Molecular , Relação Quantitativa Estrutura-Atividade , Estireno/síntese química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...