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In this paper,a series of peptide-siRNA conjugates with phosphodiester unit as the linker targeting to Cdc2 gene were synthesized by solid phase stepwise strategy.The conjugation of peptides at either 3’-terminus of siCdc2 bring no change to the classical A-form of RNA duplex,but slightly compromise the thermodynamic stability.Peptide conjugation at the 3’-terminus of sense strand could improve the serum stability obviously,however,the opposite peptide conjugation at the 3’-terminus of antisense strand shows no such influence.According to the results of artificial silencing activity assay system,peptide conjugation at 3’-terminus of antisense strand slightly weakens the silencing activity of siCdc2.But sense strand peptide conjugation exhibits similar silencing activity as native siCdc2,meanwhile,it could mitigate the unwanted off-target effect of sense strand targeting to its own mRNA.
In this paper, a series of peptide-siRNA conjugates with phosphodiester unit as the linker targeting to Cdc2 gene were synthesized by solid phase stepwise strategy. The conjugation of peptides at either 3’-terminus of siCdc2 bring no change to the classical A-form of RNA duplex, but slightly compromise the thermodynamic stability. Peptide conjugation at the 3’-terminus of sense strand could improve the serum stability obviously, however, the opposite peptide conjugation at the 3’-terminus of antisense strand shows no such influence. According to this to the results of artificial silencing activity assay system, peptide conjugation at 3’-terminus of antisense strand slightly weakens the silencing activity of siCdc2.But sense strand peptide conjugation exhibiting similar silencing activity as native siCdc2, meanwhile, it could mitigate the unwanted off- target effect of sense strand targeting to its own mRNA.