Establishment of a molecular platform for screening thalidomide derivatives with potential high anti-tumor activities / 国际药学研究杂志

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.