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A new screening method based on yeast-expressed human dipeptidyl peptidase IV and discovery of novel inhibitors |
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| Authors: | Chen-Xi Hu Hui Huang Li Zhang You Huang Zhu-Fang Shen Ke-Di Cheng Guan-Hua Du Ping Zhu |
| Affiliation: | (1) Department of Biosynthesis of Natural Products, Institute of Materia Medica, Peking Union Medical College &; Chinese Academy of Medical Sciences, Beijing, 100050, China;(2) Department of Pharmacology, Institute of Materia Medica, Peking Union Medical College &; Chinese Academy of Medical Sciences, Beijing, 100050, China;(3) National Centre for Drug Screening, Institute of Materia Medica, Peking Union Medical College &; Chinese Academy of Medical Sciences, Beijing, 100050, China;(4) Institute and State Key Laboratory of Elemento-organic Chemistry, Nankai University, Tianjin, 300071, China |
| Abstract: | Dipeptidyl peptidase (DPP) IV inhibitors provide a new strategy for the treatment of type 2 diabetes. Human DPP-IV gene was cloned from differentiated Caco-2 cells and expressed in Pichia pastoris. The recombinant enzyme was used in a new system for screening of DPP-IV inhibitors. By high throughput screening, a novel compound (W5188) was identified from 75,000 compounds with an IC50 of 6.5 μM. This method is highly reproducible and reliable for discovery of DPP-IV inhibitors as shown by Z′ value of 0.73 and S/N ratio of 6.89. |
| Keywords: | DPP-IV inhibitor High throughput screening (HTS) Diatetes Recombinant human dipeptidyl peptidase IV (rhDPP-IV) |
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