【摘要】 天然寡核苷酸作为核酸药物有许多缺陷。为了改进药学特性，人们已提出了许多骨架修饰的天然寡核苷酸的替代物，主要包括硫代寡核苷酸、混合骨架寡核苷酸和多肽核苷酸。本文综述了它们的结构特点、稳定性和亲和力。反义寡核苷酸已被用于核医学领域，因此，本文比较了反义治疗药物与反义显像剂的不同点，归纳了不同修饰的寡核苷酸在体内反义显像研究中的药代动力学和生物分布，并对反义显像的前景和目存在的问题进行了探讨。

    关键词 反义寡核苷酸 骨架修饰 硫代寡核苷酸 混合骨架寡核苷酸 多肽核苷酸 反义显像

    Wang Rongfu，Qiu Feng

    Department of Nuclear Medicine，First Hospital，Peking University，Beijing100034.

    【Abstract】 The natural oligonucleotides have manylimitations as drug candidates.To improve the pharmacal properties，dozens of chemical alterations of the phosphodiester-deoxyribose backbone have been proposed，chiefly inˉcluding S-ONs，MBO and PNA.This review expatiates on their chemistry，stability and affinity.Antisense oligonuˉcleotides have been applied in nuclear medicine in recent years.This review compares the differences bwtween the anˉtisense therapeutic drug and antisense imaging agents and summarizes the pharmacokinetics and biodistribution of variˉous modificated alterations in antisense imaging research in vivo.The antisense imaging prospects and obstacle are disˉcussed in this review.

    Key words antisense oligonucleotide backbone modification S-ONs MBO PNA antisense imaging ......