Establishment of a molecular platform for screening thalidomide derivatives with potential high anti-tumor activities
10.13220/j.cnki.jipr.2015.02.012
- Author:
Hai-Ning HUANG
1
Author Information
1. Cardiovascular Drug Research Center, Tianjin Institute of Health and Environmental Medicine
- Publication Type:Journal Article
- Keywords:
Cereblon (CRBN);
Drug screening;
Ikaros family zinc finger protein 1(lKZF1);
Thalidomide derivatives
- From:
Journal of International Pharmaceutical Research
2015;42(2):189-193
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To establish a molecular platform for screening thalidomide derivatives with potential high anti-tumor activities. Methods: Human cereblonvCRBN) and Ikaros family zinc finger protein l(IKZF1) cDNA were amplified and cloned into pXJ40-myc and pcDNA3-FLAG vectors respectively. Then the two constructs were transfected into 293T cells and the anti-tumor activities of thalidomide and its derivatives were reflected by their effects on the binding between CRBN and IKZF1 proteins. Results: Both CRBN and IKZF1 were successfully expressed in 293T cells. Thalidomide and two of its derivatives were found to enhance the interaction between CRBN and IKZF1 significantly. Conclusion: A molecular platform was successfully established for screening thalidomide derivatives with potential high anti-tumor activities and two thalidomide derivatives could potentiate the binding between CRBN and IKZF1. suggesting that they possess potential anti-tumor activities.
