Figure 1.

Design and synthesis of activators. (A) The synthetic activator consisting of an activation domain (AD), a dimerization or linker domain (LD), and a DNA binding domain (DBD) complexed with the cognate palindromic DNA site of the hairpin polyamide-peptide conjugate. (B) The synthesis of polyamide 1 was accomplished according to established protocols. (a) Treatment of 1 with thiolane-2,5-dione followed by benzyl bromide provided thioester 2 in good yield (53%). (b) Combination of thioester 2 with each peptide in denaturing buffer then provided the targeted conjugates via the native ligation reaction.