Establishment of a molecular platform for screening thalidomide derivatives with potential high anti-tumor activities / 国际药学研究杂志
Journal of International Pharmaceutical Research
;
(6): 189-193, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-845676
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Type of study:
Diagnostic study
/
Screening study
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2015
Type:
Article
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