Nanjunda Rupesh, Wilson W David
Department of Chemistry, Georgia State University, Atlanta, Georgia, USA.
Curr Protoc Nucleic Acid Chem. 2012 Dec;Chapter 8:Unit8.8. doi: 10.1002/0471142700.nc0808s51.
Compounds that bind in the DNA minor groove have provided critical information on DNA molecular recognition, have found extensive uses in biotechnology, and are providing clinically useful drugs against diseases as diverse as cancer and sleeping sickness. This review focuses on the development of clinically useful heterocyclic diamidine minor groove binders. These compounds have shown us that the classical model for minor groove binding in AT DNA sequences must be expanded in several ways: compounds with nonstandard shapes can bind strongly to the groove, water can be directly incorporated into the minor groove complex in an interfacial interaction, and the compounds can form cooperative stacked dimers to recognize GC and mixed AT/GC base pair sequences.
结合于DNA小沟的化合物为DNA分子识别提供了关键信息，在生物技术领域有广泛应用，并且正在提供针对癌症和昏睡病等多种疾病的临床有用药物。本综述聚焦于临床有用的杂环二脒小沟结合剂的发展。这些化合物向我们表明，AT DNA序列中小沟结合的经典模型必须在几个方面加以扩展：具有非标准形状的化合物可与小沟强烈结合，水可通过界面相互作用直接纳入小沟复合物中，并且这些化合物可形成协同堆积二聚体以识别GC以及混合的AT/GC碱基对序列。
