University of Bonn, Life & Medical Sciences Institute, Bonn, Germany.
Hamostaseologie. 2011 Nov;31(4):258-63. doi: 10.5482/ha-1156.
Nucleic acid based aptamers are single-stranded oligonucleotide ligands isolated from random libraries by an in-vitro selection procedure. Through the formation of unique three-dimensional structures, aptamers are able to selectively interact with a variety of target molecules and are therefore also promising candidates for the development of anticoagulant drugs. While thrombin represents the most prominent enzymatic target in this field, also aptamers directed against other coagulation proteins and proteases have been identified with some currently being tested in clinical trials. In this review, we summarize recent developments in the design and evaluation of aptamers for anticoagulant therapy and research.
基于核酸的适体是通过体外选择程序从随机文库中分离出的单链寡核苷酸配体。通过形成独特的三维结构,适体能选择性地与多种靶分子相互作用,因此也是开发抗凝药物的有前途的候选物。虽然凝血酶是该领域最突出的酶靶标,但也已经鉴定出针对其他凝血蛋白和蛋白酶的适体,其中一些目前正在临床试验中进行测试。在这篇综述中,我们总结了用于抗凝治疗和研究的适体设计和评估的最新进展。