Establishment of in vitro and cell-based drug screening model for Notch signaling pathway.
- Author:
Qi NIU
;
Fang WU
- Publication Type:Journal Article
- MeSH:
Amyloid Precursor Protein Secretases;
Animals;
Drug Evaluation, Preclinical;
methods;
Humans;
Luciferases;
Mice;
Receptors, Notch;
antagonists & inhibitors;
Signal Transduction
- From:
Acta Pharmaceutica Sinica
2014;49(6):837-842
- CountryChina
- Language:Chinese
-
Abstract:
Notch signal pathway is closely related to the organism's development and a variety of cancers. Current models available for screening modulators of Notch signal pathway all use mouse Notch protein as substrates and those models which use human Notch protein have not been reported. To make the screen results much more reliable, the authors cloned a truncated form of human Notch1 called N100, and built the screening models for the use of it instead of mouse Notch protein. The models included an in vitro screening model based on the purified gamma-secretase enzyme and a cell model using luciferase reporter system. The screening models then have been verified by the known modulators of Notch signal pathway and the IC50 values have been obtained. The verified models can be used to screen modulators of human Notch signaling pathway effectively and it can lay the foundation for finding new modulators of this kind effectively.
