Our research activities have focused on the creation of functional molecules that exhibit specific recognition and reaction to the DNA and RNA. The functional oligonucleotides incorporating such intelligent agents would enable chemical modulation of gene expression with high sequence-selectivity at a single nucleoside level. Recent progress in our group includes achievement of highly efficient cross-linking reaction with specificity toward cytosine at the target site. We have applied the new cross-linking agent to antisense inhibition of gene expression in cell. Now, we study about higher functional intelligent molecules for regulation of gene expression. We expect that our research can be expanded to "In Cell Chemistry" in future.