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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

G4 Aptamers: Trends in Structural Design

Author(s): Anna Varizhuk, Nikolay Ilyinsky, Igor Smirnov and Galina Pozmogova

Volume 16, Issue 16, 2016

Page: [1321 - 1329] Pages: 9

DOI: 10.2174/1389557516666160321114715

open access plus


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.

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