SAR study of a novel triene-ansamycin group compound, quinotrierixin, and related compounds, as inhibitors of ER stress-induced XBP1 activation.
J Antibiot (Tokyo)
; 61(5): 303-11, 2008 May.
Article
em En
| MEDLINE
| ID: mdl-18653996
ABSTRACT
In the course of screening for an inhibitor of ER stress-induced XBP1 activation, we isolated a new member of the triene-ansamycin group compound, quinotrierixin, from a culture broth of Streptomyces sp. PAE37. Quinotrierixin inhibited thapsigargin-induced XBP1 activation in HeLa cells with an IC50 of 0.067 microM. We found that other triene-ansamycin group compounds such as demethyltrienomycin A and mycotrienin I also inhibited ER stress-induced XBP1 activation. Moreover, we performed SAR study of twelve triene-ansamycin group compounds. The study showed that OH group at C-13 was crucial, and CH3 group at C-14 would be important for the XBP1 inhibitory activity.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Streptomyces
/
Fatores de Transcrição
/
Rifabutina
/
Proteínas de Ligação a DNA
/
Antibacterianos
Limite:
Humans
Idioma:
En
Revista:
J Antibiot (Tokyo)
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Japão