Molecular Design of a Pyrrole–Imidazole Hairpin Polyamides for Effective DNA Alkylation

Chemical and Biological Explorations of the Family of CC-1065 and the Duocarmycin Natural Products

“…The synthesis of CPI and CBI analogues (Fig. 32) incorporating large imidazole/pyrrole polyamide chains for binding double stranded DNA which can target G-C base pairs has been reported [81][82][83][84][85]. The incorporation of a vinyl linker between the alkylating and minor groove binding agents was again shown to be important for efficient DNA alkylation [75].…”

Development of a molecule-recognized promoter DNA sequence for inhibition of HER2 expression

“…Polyamide was synthesized, according to the method described earlier. 26 Next, we performed a direct binding assay using Biacore2000 (GE Healthcare Ltd, Little Chalfont, UK) to see whether PI polyamide-HER2 binds to a target sequence consisting of double-strand oligonucleotides containing the HTF-binding site. We confirmed that PI polyamide-HER2 shows an approximately 10-times higher preference for binding to a complementary DNA sequence, including the HTF-binding sites than those for binding to mutated DNA (Table 1).…”

Modulation of the EMT/MET process by pyrrole–imidazole polyamide targeting human transforming growth factor-β1

“…PI polyamides were synthesized according to previously described methods (Bando et al, 2002). We designed both a PI polyamide that binds to the DNA sequence of the near FSE2 site (-1383 to -1376 nucleotides upstream of the transcription initiation point) of the promoter region of the human TGF-β1 gene (Suppl.…”