Creation of functional recognition molecules for chemical modification of gene expression

Artificial molecules that exhibit specific recognition of duplex DNA have attracted great interest because of their potential application in the manipulation of gene expression. Specific chemical reactions to the target base within the predetermined site would secure selective inhibition at either translation or transcription reactions. A more interesting application would be to alter the reacted base structure to induce a point mutation. In our study, we have focused our efforts on: 1) development of new cross-linking molecules with high efficiency as well as high selectivity; 2) establishment of a new molecular basis for the formation of nonnatural triplexes; and 3) synthetic approaches to the new minor groove binders. This paper summarizes our recent results using two new functional molecules: 2-amino-6-vinylpurine derivatives as new cross-linking agents; and W-shaped nucleic acid analogues as new recognition molecules for the formation of nonnatural-type triplexes.