Resevrch progress in screening methods of calcineurin inhibitors
10.3867/j.issn.1000-3002.2017.04.011
- VernacularTitle:钙调磷酸酶抑制剂筛选方法的研究进展
- Author:
Xiang XU
;
Zhifeng CUI
;
Dongdong DING
;
Tingheng ZHU
- Keywords:
calcineurin;
inhibitor;
screening methods
- From:
Chinese Journal of Pharmacology and Toxicology
2017;31(4):367-374
- CountryChina
- Language:Chinese
-
Abstract:
Calcineurin inhibitor screening should benefit from the strengths of each method. This paper reviews three calcineurin inhibitor screening methods:yeast positive screening model, yeast reporter gene high through- put screening model and calcineurin activity detection method. We have compared the range of application, advantages and disadvantages of each method, and combined effect of multiple methods. The yeast positive screening model can prevent the false positiveness caused by bacteriostat by using growth zooms instead of inhibition zooms. The yeast reporter gene high through-put screening model is suitable for pilot screening among a wide range of samples and is more efficient than the other methods. The calcineurin activity detection method can directly report the inhibitory ratio to a specific target. This review is expected provide a model-selection reference for the development of novel low-toxic calcineurin inhibitors.
