Screening and identification of the upregulators of ATP-binding cassette transporter A1 / 药学学报
Acta Pharmaceutica Sinica
; (12): 446-451, 2012.
Article
en Zh
| WPRIM
| ID: wpr-323021
Biblioteca responsable:
WPRO
ABSTRACT
ATP-binding cassette transporter A1 (ABCA1) promotes cholesterol and phospholipid efflux from cells to lipid-poor apolipoprotein A-I (apoA-I), and plays a key role in the initial steps of the whole process of reverse cholesterol transport (RCT). Upregulation of ABCA1 is beneficial for atherosclerosis (AS) prevention and/or therapy, which indicated that ABCA1 was a target for anti-AS drug development. In the previous study, a high-throughput screening method was established using ABCA1p-LUC HepG2 cell line to find the upregulators of ABCA1. In the present study, compound 2030421B was found using this method, with EC50 of 0.50 microg x mL(-1). The compound was further identified as an upregulator of ABCA1 expression by real-time quantitative reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting analysis. Studies also showed that the 2030421B could induce apoA-I-mediated cholesterol efflux and inhibit lipids uptake into mouse peritoneal macrophages RAW264.7.
Texto completo:
1
Base de datos:
WPRIM
Asunto principal:
Farmacología
/
Benzaldehídos
/
Transporte Biológico
/
ARN Mensajero
/
Estructura Molecular
/
Regulación hacia Arriba
/
Células Cultivadas
/
Química
/
Colesterol
/
Apolipoproteína A-I
Tipo de estudio:
Diagnostic_studies
/
Screening_studies
Límite:
Animals
/
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2012
Tipo del documento:
Article