| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1930788 | Biochemical and Biophysical Research Communications | 2011 | 5 Pages |
An orthogonally positioned diamino/dicationic polyamide f-IPI 2 was synthesized. It has enhanced binding affinity, and it showed comparable sequence specificity to its monoamino/monocationic counterpart f-IPI 1. Results from CD and DNase I footprinting studies confirmed the minor groove binding and selectivity of polyamides 1 and 2 for the cognate sequence 5′-ACGCGT-3′. SPR studies provided their binding constants: 2.4 × 108 M−1 for diamino 2, which is ∼4 times higher than 5.4 × 107 M−1 for its monoamino analogue 1.
Research highlights► A novel pyrrole and imidazole-containing polyamide, diamino f-IPI, is synthesized. ► Diamino f-IPI binds four times more strongly to 5′-ACGCGT-3′ than monoamino f-IPI. ► It binds 5′-ACGCGT-3′ with similar sequence selectivity as monoamino f-IPI. ► Second amino group in diamino f-IPI enhances water solubility. ► It also provides a nucleophilic site for modifications.
