酸和硫酸的固体相化学合成 酸和硫酸的 oligodeoxynucleotides
Douglas J Dellinger1, David M Sheehan, Nanna K Christensen
1Department of Chemistry and Biochemistry, University of Colorado, Boulder, CO 80309-0215, USA.
Journal of the American Chemical Society
|January 23, 2003
概括
通过固相方法合成了新型的酸和酸寡氧核酸. 这些修改后的DNA类似物是稳定的,并刺激RNase H1活动.
科学领域:
- 橄核酸的化学成分
- 药用化学 医学化学
背景情况:
- 在分子生物学和治疗学中,寡氧核酸是至关重要的.
- 开发改性寡核酸可提高稳定性和生物活性.
研究的目的:
- 合成新型酸和酸新型酸.
- 为了评估这些改性DNA类型的稳定性和酶活性.
主要方法:
- 使用新型二胺单体的固体相合成.
- 通过酸修饰自动化DNA合成.
- 通过HPLC进行定量氧化和净化.
- 使用NMR和质谱学进行表征.
主要成果:
- 成功合成了具有>97%合效率的酸和硫酸寡度氧核酸.
- 修改过的寡核酸表明对蛇毒二酶的稳定性.
- 同类药物显示刺激RNase H1活动.
结论:
- 开发的固体相策略使酸和酸修饰的寡核酸能够高效合成.
- 这些新型类似物具有有利的生化特性,包括核酶抵抗和RNase H1相互作用.
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