Development of HTS model on SERT inhibitors combined biological screening model with HTVS / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1116-1121, 2015.
Artigo
em Chinês
| WPRIM
| ID: wpr-257019
ABSTRACT
In order to improve the efficiency of drug screening on serotonin transporter (SERT) inhibitors, a high-throughput screening (HTS) model is established in RBL-2H3 cells. The RBL-2H3 cells are very similar to the serotonin genetic neuro, in modulation of post-receptor mechanisms and transduction pathway of SERT reactivated. Depending on a fluorescence substrate ASP+ used in detection method of inhibitor rates, it's convenient, quick, accurate and effective, not making the environmental biohazard compared with radioactive experiments. Furthermore, biological screening model combined with computer aided virtual screening technique describing high-throughput virtual screening (HTVS). Bayesian classification method and molecular fingerprint similarity were applied to virtual screening technique, for screening compounds in compound library. Some compounds have been found, and then validated further by biological screening model. Combination of HTS and HTVS improves the efficiency of screening SERT inhibitors.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Linhagem Celular
/
Teorema de Bayes
/
Inibidores Seletivos de Recaptação de Serotonina
/
Avaliação Pré-Clínica de Medicamentos
/
Proteínas da Membrana Plasmática de Transporte de Serotonina
/
Ensaios de Triagem em Larga Escala
/
Metabolismo
/
Modelos Biológicos
Tipo de estudo:
Estudo diagnóstico
/
Estudo prognóstico
/
Estudo de rastreamento
Limite:
Animais
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2015
Tipo de documento:
Artigo
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