[Aptamers in the Treatment of Bacterial Infections: Problems and Prospects].

N A Zeninskaya, A V Kolesnikov, A K Ryabko, I G Shemyakin, I A Dyatlov, A V Kozyr
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引用次数: 1

Abstract

Aptamers are short single-stranded oligonucleotides which are selected via targeted chemical evolution in vitro to bind a molecular target of interest. The aptamer selection technology is designated as SELEX (Systematic evolution of ligands by exponential enrichment). SELEX enables isolation of oligonucleotide aptamers binding a wide range of targets of interest with little respect for their nature and molecular weight. A number of applications of aptamer selection were developed ranging from biosensor technologies to antitumor drug discovery. First aptamer-based pharmaceutical (Macugen) was approved by FDA for clinical use in 2004, and since then more than ten aptamer-based drugs undergo various phases of clinical trials. From the medicinal chemist’s point of view, aptamers represent a new class of molecules suitable for the development of new therapeutics. Due to the stability, relative synthesis simplicity, and development of advanced strategies of target specific molecular selection, aptamers attract increased attention of drug discovery community. Difficulties of the development of next-generation antibiotics basing on the conventional basis of combinatorial chemistry and high-throughput screening have also amplified the interest to aptamer-based therapeutic candidates. The present article reviews the investigations focused on the development of antibacterial aptamers and discusses the potential and current limitations of the use of this type of therapeutic molecules.

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适体在细菌感染治疗中的应用:问题与展望
适配体是短单链寡核苷酸,通过体外靶向化学进化选择结合感兴趣的分子靶标。适体选择技术被命名为SELEX(配体的系统进化由指数富集)。SELEX能够分离寡核苷酸适配体,结合广泛的感兴趣的目标,很少尊重其性质和分子量。从生物传感器技术到抗肿瘤药物的发现,适体选择的许多应用都得到了发展。2004年,第一个基于适配体的药物(Macugen)被FDA批准用于临床使用,从那时起,十多种基于适配体的药物经历了不同阶段的临床试验。从药物化学家的角度来看,适体代表了一类适合开发新疗法的新分子。适配体由于其稳定性、相对简单的合成以及先进的靶向分子选择策略的发展,越来越受到药物发现界的关注。基于组合化学和高通量筛选的传统基础开发下一代抗生素的困难也扩大了对基于适配体的治疗候选药物的兴趣。本文综述了抗菌适体的研究进展,并讨论了这类治疗分子的潜力和目前的局限性。
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来源期刊
CiteScore
1.50
自引率
0.00%
发文量
31
期刊最新文献
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