High-throughput screening of human soluble protein tyrosine phosphatase 1B inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1058-1064, 2011.
Artigo
em Chinês
| WPRIM
| ID: wpr-233035
ABSTRACT
To screen potential human soluble protein tyrosine phosphatase 1B (PTP1B) inhibitors, a high-throughput screening (HTS) model in 384-well microplate with total volume of 50 microL was established. Recombinant PTP1B was cloned and expressed in E. coli. with its specific substrate 4-nitrophenyl phosphate disodium salt hexahydrate (PNPP). The HTS model was based on enzyme reaction rate with enhanced sensitivity and specificity (Z' = 0.78). A total of 24,240 samples were screened, among them 80 samples with inhibition greater than 70% were selected for further rescreening. Finally, six compounds with high inhibitory activity were identified, whose IC50 values were 21.58, 18.39, 15.37, 11.92, 37.27, and 36.61 microg x mL(-1), separately. The results indicated that the method was stable, sensitive, reproducible and also suitable for high-throughput screening.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Vanadatos
/
Sensibilidade e Especificidade
/
Concentração Inibidora 50
/
Avaliação Pré-Clínica de Medicamentos
/
Inibidores Enzimáticos
/
Escherichia coli
/
Proteína Tirosina Fosfatase não Receptora Tipo 1
/
Ensaios de Triagem em Larga Escala
/
Metabolismo
Tipo de estudo:
Estudo diagnóstico
/
Estudo de rastreamento
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2011
Tipo de documento:
Artigo
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