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High-throughput screening of human soluble protein tyrosine phosphatase 1B inhibitors / 药学学报
Acta Pharmaceutica Sinica ; (12): 1058-1064, 2011.
Article in Chinese | 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.
Subject(s)
Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Vanadates / Sensitivity and Specificity / Inhibitory Concentration 50 / Drug Evaluation, Preclinical / Enzyme Inhibitors / Escherichia coli / Protein Tyrosine Phosphatase, Non-Receptor Type 1 / High-Throughput Screening Assays / Metabolism Type of study: Diagnostic study / Screening study Limits: Humans Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2011 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Vanadates / Sensitivity and Specificity / Inhibitory Concentration 50 / Drug Evaluation, Preclinical / Enzyme Inhibitors / Escherichia coli / Protein Tyrosine Phosphatase, Non-Receptor Type 1 / High-Throughput Screening Assays / Metabolism Type of study: Diagnostic study / Screening study Limits: Humans Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2011 Type: Article