Division of Natural & Applied Sciences and Department of Chemistry, Hope College, 35 East 12th Street, Holland, MI 49423, USA.
Biochem Biophys Res Commun. 2011 Jan 21;404(3):848-52. doi: 10.1016/j.bbrc.2010.12.073. Epub 2010 Dec 23.
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 × 10(8)M(-1) for diamino 2, which is ∼4 times higher than 5.4 × 10(7)M(-1) for its monoamino analogue 1.
合成了一种正交定位的二氨基/二阳离子聚酰胺 f-IPI 2。它具有增强的结合亲和力,并且表现出与其单氨基/单阳离子类似物 f-IPI 1 相当的序列特异性。来自 CD 和 DNase I 足迹研究的结果证实了聚酰胺 1 和 2 对同源序列 5'-ACGCGT-3'的小沟结合和选择性。SPR 研究提供了它们的结合常数:二氨基 2 的为 2.4×10(8)M(-1),约为其单氨基类似物 1 的 5.4×10(7)M(-1)的 4 倍。