Selective placement of an aliphatic â-alanine (â) residue paired side-by-side with either a pyrrole (Py) or imidazole (Im) aromatic amino acid is found to compensate for sequence composition effects for recognition of the minor groove of DNA by hairpin pyrrole-imidazole polyamides. A series of polyamides were prepared which contain pyrrole and imidazole aromatic amino acids, as well as γ-aminob...

Microwave synthesis was utilized to rapidly build Py-Im polyamides in high yields and purity using Boc-protection chemistry on Kaiser oxime resin. A representative polyamide targeting the 5'-WGWWCW-3' (W = A or T) subset of the consensus Androgen and Glucocorticoid Response Elements was synthesized in 56% yield after 20 linear steps and HPLC purification. It was confirmed by Mosher amide deriva...

Disclosed is an inhibitor of the expression of CTGF gene, which comprises a pyrrole-imidazole polyamide. The pyrrole-imidazole polyamide has an N-methylpyrrole unit (hereinafter, referred to as “Py”), an N-methylimidazole unit (hereinafter, referred to as “Im”) and a ϝ-aminobutanoic acid unit. In the pyrrole-imidazole polyamide, the region of the ϝ-aminobutanoic acid unit is folded to form an U...

Nowadays, “green” is a hot topic almost everywhere, from retailers to universities to industries; and achieving a green status has become a universal aim. However, polymers are commonly considered not to be “green”, being associated with massive energy consumption and severe pollution problems (for example, the “Plastic Soup”) as a public stereotype. To achieve green polymers, three elements sh...