一个可编程DNA结合小分子文库的完成。
Completion of a Programmable DNA-Binding Small Molecule Library.
作者信息
Hsu Carey F, Phillips John W, Trauger John W, Farkas Michelle E, Belitsky Jason M, Heckel Alexander, Olenyuk Bogdan Z, Puckett James W, Wang Clay C C, Dervan Peter B
机构信息
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125.
出版信息
Tetrahedron. 2007 Jul 2;63(27):6146-6151. doi: 10.1016/j.tet.2007.03.041.
Hairpin pyrrole-imidazole (Py-Im) polyamides are programmable oligomers that bind the DNA minor groove in a sequence-specific manner with affinities comparable to those of natural DNA-binding proteins. These cell-permeable small molecules have been shown to enter the nuclei of live cells and downregulate endogenous gene expression. We complete here a library of 27 hairpin Py-Im polyamides which bind 7-base-pair sequences of the general form 5'-WWGNNNW-3' (where W = A or T, N = W, G, or C). Their equilibrium association constants (K(a)) range from K(a) = 1×10(8) M(-1) to 4×10(10) M(-1) with good sequence specificity. A table of binding affinities and sequence contexts for this completed 27-member library has been assembled for the benefit of the chemical biology community interested in molecular control of transcription.
发夹状吡咯-咪唑（Py-Im）聚酰胺是可编程的低聚物，它们以序列特异性方式结合DNA小沟，其亲和力与天然DNA结合蛋白相当。这些可穿透细胞的小分子已被证明可进入活细胞的细胞核并下调内源性基因表达。我们在此完成了一个由27种发夹状Py-Im聚酰胺组成的文库，这些聚酰胺结合一般形式为5'-WWGNNNW-3'（其中W = A或T，N = W、G或C）的7个碱基对序列。它们的平衡缔合常数（K(a)）范围为K(a) = 1×10(8) M(-1)至4×10(10) M(-1)，具有良好的序列特异性。为了方便对转录分子控制感兴趣的化学生物学界，已汇编了这个完整的27成员文库的结合亲和力和序列背景表。
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