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STEREOCHEMICAL CONTROL OF THE DNA BINDING AFFINITY, SEQUENCE SPECIFICITY, AND ORIENTATION-PREFERENCE OF CHIRAL HAIRPIN POLYAMIDES IN THE MINOR GROOVE
STEREOCHEMICAL CONTROL OF THE DNA BINDING AFFINITY, SEQUENCE SPECIFICITY, AND ORIENTATION-PREFERENCE OF CHIRAL HAIRPIN POLYAMIDES IN THE MINOR GROOVE
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机译:小沟中手性发夹状聚酰胺的DNA结合亲和力,序列特异性和方向偏好的立体化学控制
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摘要
This invention provides improved polyamides comprising a hairpin loop derived from gamma-aminobutyric acid which bind to the minor groove of a promoter regions of a DNA sequence. Binding of the polyamide to the DNA sequence of the promoter region inhibits expression of the requisite gene. The improvement relates to the use of R-2,4-diaminobutyric acid and derivatives of the 2-amino group to form the hairpin loop. The improved asymmetric hairpin provides for tighter binding of the polyamides to the minor groove of DNA and additionally provides an amine function for derivatizing polyamides by, for example, forming amide linkages. Such derivatives may serve to attach detectable labels to the polyamide.
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