Toward the Selective Inhibition of G Proteins: Total Synthesis of a Simplified YM-254890 Analog.
Org Lett
; 17(9): 2270-3, 2015 May 01.
Article
em En
| MEDLINE
| ID: mdl-25875152
ABSTRACT
A simplified analog (WU-07047) of the selective Gαq/11 inhibitor YM-254890 has been synthesized, and an initial probe of its activity conducted. In the analog, the two peptide-based linkers in the cyclic YM-254890 have been replaced with hydrocarbon chains. This enables a convergent approach to the synthesis of the analog. Biochemical assays showed that while the simplified analog is not as potent as YM-254890, it does still inhibit Gq.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos Cíclicos
/
Proteínas de Ligação ao GTP
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article