Issue 22, 2006

SELEX and dynamic combinatorial chemistry interplay for the selection of conjugated RNA aptamers

Abstract

SELEX (for Systematic Evolution of Ligands by Exponential enrichment) has proven to be extraordinarily powerful for the isolation of DNA or RNA aptamers that bind with high affinity and specificity to a wide range of molecular targets. However, the modest chemical functionality of nucleic acids poses some limits on the versatility of aptamers as binders and catalysts. To further improve the properties of aptamers, additional chemical diversity must be introduced. The design of chemical modifications is not a trivial task. Recently, dynamic combinatorial chemistry (DCC) has been introduced as an alternative to traditional combinatorial chemistry. DCC employs equilibrium shifting to effect molecular evolution of a dynamic combinatorial library of molecules. Herein, we describe an original process that combines DCC and SELEX for the in vitro selection of modified aptamers which are conjugated to chemically diverse small-molecules. Its successful application for the selection of small-molecule conjugated RNA aptamers that bind tightly to the transactivation-response (TAR) element of HIV-1 is presented.

Graphical abstract: SELEX and dynamic combinatorial chemistry interplay for the selection of conjugated RNA aptamers

Article information

Article type
Paper
Submitted
28 Jul 2006
Accepted
20 Sep 2006
First published
06 Oct 2006

Org. Biomol. Chem., 2006,4, 4082-4088

SELEX and dynamic combinatorial chemistry interplay for the selection of conjugated RNA aptamers

A. Bugaut, J. Toulmé and B. Rayner, Org. Biomol. Chem., 2006, 4, 4082 DOI: 10.1039/B610890C

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