基于酵母表达的人二肽基肽酶IV的新型筛选方法及新型抑制剂的发现
A new screening method based on yeast-expressed human dipeptidyl peptidase IV and discovery of novel inhibitors.
作者信息
Hu Chen-Xi, Huang Hui, Zhang Li, Huang You, Shen Zhu-Fang, Cheng Ke-Di, Du Guan-Hua, Zhu Ping
机构信息
Department of Biosynthesis of Natural Products, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing, 100050, China.
出版信息
Biotechnol Lett. 2009 Jul;31(7):979-84. doi: 10.1007/s10529-009-9963-y. Epub 2009 Mar 8.
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 IC(50) of 6.5 microM. 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.
二肽基肽酶（DPP）IV抑制剂为2型糖尿病的治疗提供了一种新策略。人DPP-IV基因从分化的Caco-2细胞中克隆出来，并在毕赤酵母中表达。重组酶被用于一种新的筛选DPP-IV抑制剂的系统。通过高通量筛选，从75000种化合物中鉴定出一种新型化合物（W5188），其IC(50)为6.5微摩尔。如Z'值为0.73和信噪比为6.89所示，该方法对于发现DPP-IV抑制剂具有高度的可重复性和可靠性。
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