首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >DNA sequence recognition in the minor groove by hairpin pyrrole polyamide-Hoechst 33258 analogue conjugate.
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DNA sequence recognition in the minor groove by hairpin pyrrole polyamide-Hoechst 33258 analogue conjugate.

机译:发夹状吡咯聚酰胺-Hoechst 33258类似物偶联物识别小沟中的DNA序列。

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摘要

A hairpin pyrrole polyamide conjugated to a Hoechst 33258 (Ht) analogue, PyPyPy-gamma-PyPyPy-gamma-Ht, was synthesized on solid-phase by adaptation of an Fmoc technique using a series of PyBOP/HOBt mediated coupling reactions. Sequence selectivity and complex stabilities were characterized by spectrofluorometric titrations and thermal melting studies. The polyamide of the conjugate was observed to bind in a hairpin motif forming 1:1 conjugate:dsDNA complexes. The conjugate is able to recognize nine contiguous A/T bps, discriminating from the sequences containing fewer than nine contiguous A/T bps.
机译:通过使用一系列PyBOP / HOBt介导的偶联反应通过Fmoc技术在固相上合成与Hoechst 33258(Ht)类似物PyPyPy-γ-PyPyPy-γ-Ht共轭的发夹吡咯聚酰胺。序列选择性和复杂的稳定性通过荧光分光光度法滴定和热熔研究进行了表征。观察到缀合物的聚酰胺结合在发夹基序中,形成1:1的缀合物:dsDNA复合物。该缀合物能够识别九个连续的A / T bps,与包含少于九个连续的A / T bps的序列区分开。

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