Scheme 1.
Photoregulation of antisense activity with light-removable PEG groups. A. A PEGylated antisense agent binds to the mRNA target sequence, which recruits RNase H to the mRNA:DNA duplex leading to the degradation of the mRNA and thus gene silencing. B. A PhotoPEG-antisense is cleaved upon UV irradiation, leaving the DNA-based antisense agent susceptible to degradation by exonucleases, thereby allowing the translation of the mRNA and gene expression.
