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Synthesis and properties of triplex-forming oligonucleotides containing 2′-O-(2-methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2010-07-10 , DOI: 10.1016/j.bmc.2010.07.005
Chenguang Lou 1 , Qiang Xiao , Lavinia Brennan , Mark E Light , Nuria Vergara-Irigaray , Elizabeth M Atkinson , Lindy M Holden-Dye , Keith R Fox , Tom Brown
Affiliation  

2′-O-(2-Methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine phosphoramidite (MEPU) has been synthesized from d-ribose and 5-iodouracil and incorporated into triplex-forming oligonucleotides (TFOs) by automated solid-phase oligonucleotide synthesis. The TFOs gave very high triplex stability with their target duplexes as measured by ultraviolet/fluorescence melting and DNase I footprinting. The incorporation of MEPU into TFOs renders them resistant to degradation by serum nucleases.



中文翻译:

含2'-O-(2-甲氧基乙基)-5-(3-氨基丙基-1-炔基)-尿苷的三链形成寡核苷酸的合成及性质

2' - O- (2-甲氧基乙基)-5-(3-氨基丙-1-炔基)-尿苷亚磷酰胺 (MEPU) 已由d-核糖和 5-碘尿嘧啶合成,并通过自动固相寡核苷酸合成。通过紫外/荧光熔解和 DNase I 足迹测定,TFO 对其目标双链体具有非常高的三链体稳定性。MEPU 与 TFO 的结合使它们能够抵抗血清核酸酶的降解。

更新日期:2010-07-10
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