作为凝血因子IXa可逆抗体的RNA胺酶
Christopher P Rusconi1, Elizabeth Scardino, Juliana Layzer
1Department of Surgery, Program in Combinatorial Therapeutics, Duke University Medical Center, Durham, North Carolina 27710, USA. c.rusconi@cgt.duke.edu
Nature
|September 6, 2002
概括
研究人员开发了一种新的策略,使用核酸制造更安全的抗凝剂. 胺类药物作为抗凝剂,补充性寡核酸类药物作为有效的抗毒剂,可以精确控制药物的作用.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 药理学 药理学是指药理学的学科.
背景情况:
- 治疗剂,特别是抗凝剂,携带诸如出血等不良反应的风险.
- 尽管存在局限性,但由于其可控制的抗毒素 - - 蛋白胺,氨酸被广泛使用.
- 目前还没有一个可通用的策略来设计药物-抗剂对.
研究的目的:
- 通过核酸特性研究药物-解毒剂对的理性设计.
- 开发可通过特定的抗毒剂控制的新型抗凝剂.
主要方法:
- 设计的与蛋白质结合的寡核酸 (亚胺) 向凝血因子IXa.
- 合成了互补的寡核酸以作为胺酶结合抗剂.
- 在人体血中测试了抗凝剂活性和抗毒剂的逆转.
主要成果:
- 向因子IXa的阿普塔默表现出强大的抗凝剂活性.
- 补充的寡核酸有效地逆转了aptamer的抗凝效应.
- 药物抗毒剂系统在健康志愿者和肝素不耐受患者的血中证明有效.
结论:
- 已经建立了一个可通用的策略来设计基于核酸的药物-抗剂对.
- 这种方法使得开发更安全,可调节的抗凝固疗法成为可能.
- 这为创造超越抗凝固的可控制药物系统开辟了道路.
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