High-throughput screening of human soluble protein tyrosine phosphatase 1B inhibitors / 药学学报
Acta Pharmaceutica Sinica
; (12): 1058-1064, 2011.
Article
ي Zh
| WPRIM
| ID: wpr-233035
المكتبة المسؤولة:
WPRO
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.
النص الكامل:
1
الفهرس:
WPRIM
الموضوع الرئيسي:
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
نوع الدراسة:
Diagnostic_studies
/
Screening_studies
المحددات:
Humans
اللغة:
Zh
مجلة:
Acta Pharmaceutica Sinica
السنة:
2011
نوع:
Article