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.
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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