Tuerk C, MacDougal S, Gold L
Department of Molecular, Cellular and Developmental Biology, University of Colorado, Boulder 80309.
Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):6988-92. doi: 10.1073/pnas.89.15.6988.
High-affinity ligands of the reverse transcriptase of human immunodeficiency virus type 1 (HIV-1) were isolated by the SELEX procedure (systematic evolution of ligands by exponential enrichment) from RNA populations randomized at 32 positions. Analysis of these ligands revealed a pseudoknot consensus with primary sequence bias at some positions. We demonstrated that at least one of the ligands inhibits cDNA synthesis by HIV reverse transcriptase but fails to inhibit other reverse transcriptases. These experiments highlight the power of SELEX to yield highly specific ligands that reduce the activity of target proteins. Such ligands may provide therapeutic reagents for viral and other diseases.
通过SELEX程序(指数富集配体系统进化)从32个位置随机化的RNA群体中分离出了人类免疫缺陷病毒1型(HIV-1)逆转录酶的高亲和力配体。对这些配体的分析揭示了一个在某些位置具有一级序列偏向性的假结共有序列。我们证明,这些配体中至少有一个可抑制HIV逆转录酶的cDNA合成,但不能抑制其他逆转录酶。这些实验突出了SELEX产生可降低靶蛋白活性的高度特异性配体的能力。此类配体可能为病毒及其他疾病提供治疗试剂。