Abstract
Many potent DNA aptamers are known to contain a G-quadruplex (G4) core. Structures and applications of the majority of such aptamers have been reviewed previously. The present review focuses on the design and optimization of G4 aptamers. General features of bioactive G4s are analyzed, and the main strategies for construction of aptamers with desired properties and topologies, including modular assembly, control of an aptamer folding and some others, are outlined. Chemical modification as a method for post-SELEX G4 aptamer optimization is also discussed, and the effects of loop and core modifications are compared. Particular attention is paid to the emerging trends, such as the development of genomic G4- inspired aptamers and the combinatorial approaches which aim to find a balance between rational design and selection.
Keywords: Aptamers, chemical modification, combinatorial approaches, drug design, G-quadruplexes, structure-activity relationship.
Mini-Reviews in Medicinal Chemistry
Title:G4 Aptamers: Trends in Structural Design
Volume: 16 Issue: 16
Author(s): Anna Varizhuk, Nikolay Ilyinsky, Igor Smirnov and Galina Pozmogova
Affiliation:
Keywords: Aptamers, chemical modification, combinatorial approaches, drug design, G-quadruplexes, structure-activity relationship.
Abstract: Many potent DNA aptamers are known to contain a G-quadruplex (G4) core. Structures and applications of the majority of such aptamers have been reviewed previously. The present review focuses on the design and optimization of G4 aptamers. General features of bioactive G4s are analyzed, and the main strategies for construction of aptamers with desired properties and topologies, including modular assembly, control of an aptamer folding and some others, are outlined. Chemical modification as a method for post-SELEX G4 aptamer optimization is also discussed, and the effects of loop and core modifications are compared. Particular attention is paid to the emerging trends, such as the development of genomic G4- inspired aptamers and the combinatorial approaches which aim to find a balance between rational design and selection.
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Varizhuk Anna, Ilyinsky Nikolay, Smirnov Igor and Pozmogova Galina, G4 Aptamers: Trends in Structural Design, Mini-Reviews in Medicinal Chemistry 2016; 16 (16) . https://dx.doi.org/10.2174/1389557516666160321114715
DOI https://dx.doi.org/10.2174/1389557516666160321114715 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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