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Structure and nuclease resistance of 2',4'-constrained 2'-O-methoxyethyl (cMOE) and 2-O-ethyl (cEt) modified DNAs

机译:2',4'约束的2'-O-甲氧基乙基(cMOE)和2-O-乙基(cEt)修饰的DNA的结构和核酸酶抗性

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摘要

Combining the structural elements of the second generation 2'-O-methoxyethyl (MOE) and locked nucleic acid (LNA) antisense oligonucleotide (AON) modifications yielded the highly nuclease resistant 2',4'-constrained MOE and ethyl bicyclic nucleic acids (cMOE and cEt BNA, respectively). Crystal structures of DNAs with cMOE or cEt BNA residues reveal their conformational preferences. Comparisons with MOE and LNA structures allow insights into their favourable properties for AON applications.
机译:结合第二代2'-O-甲氧基乙基(MOE)和锁定核酸(LNA)反义寡核苷酸(AON)修饰的结构元件,产生了高度耐核酸酶的2',4'约束型MOE和乙基双环核酸(cMOE和cEt BNA)。具有cMOE或cEt BNA残基的DNA的晶体结构揭示了其构象偏好。通过与MOE和LNA结构进行比较,可以深入了解其对AON应用的有利特性。

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  • 来源
    《Chemical Communications》 |2012年第66期|p.8195-8197|共3页
  • 作者单位

    Department of Biochemistry, Vanderbilt University School ofMedicine, Nashville, TN 37232, USA;

    Department of Medicinal Chemistry, Isis Pharmaceuticals Inc.,2855 Gazelle Court, Carlsbad, CA 92010, USA;

    Department of Medicinal Chemistry, Isis Pharmaceuticals Inc.,2855 Gazelle Court, Carlsbad, CA 92010, USA;

    Department of Medicinal Chemistry, Isis Pharmaceuticals Inc.,2855 Gazelle Court, Carlsbad, CA 92010, USA;

    Department of Medicinal Chemistry, Isis Pharmaceuticals Inc.,2855 Gazelle Court, Carlsbad, CA 92010, USA;

    Department of Medicinal Chemistry, Isis Pharmaceuticals Inc.,2855 Gazelle Court, Carlsbad, CA 92010, USA;

    Department of Biochemistry, Vanderbilt University School ofMedicine, Nashville, TN 37232, USA;

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  • 入库时间 2022-08-17 13:20:58

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