Abstract
The systematic evolution of ligands by exponential enrichment (SELEX) is a combinatorial oligonucleotide library- based in vitro selection approach in which DNA or RNA molecules are selected by their ability to bind their targets with high affinity and specificity, comparable to those of antibodies. Nucleic acids with high affinity for their targets have been selected against a wide variety of compounds, from small molecules, such as ATP, to membrane proteins and even whole organisms. Recently, the use of the SELEX technique was extended to isolate oligonucleotide ligands, also known as aptamers, for a wide range of proteins of importance for therapy and diagnostics, such as growth factors and cell surface antigens. The number of aptamers generated as inhibitors of various target proteins has increased following automatization of the SELEX process. Their diagnostic and therapeutic efficacy can be enhanced by introducing chemical modifications into the oligonucleotides to provide resistance against enzymatic degradation in body fluids. Several aptamers are currently being tested in preclinical and clinical trials, and aptamers are in the process of becoming a new class of therapeutic agents. Recently, the anti-VEGF aptamer pegaptanib received FDA approval for treatment of human ocular vascular disease.
Keywords: SELEX, aptamer, therapeutic agent, high-throughput screening
Combinatorial Chemistry & High Throughput Screening
Title: DNA and RNA Aptamers: From Tools for Basic Research Towards Therapeutic Applications
Volume: 9 Issue: 8
Author(s): Henning Ulrich, Cleber A. Trujillo, Arthur A. Nery, Janaina M. Alves, Paromita Majumder, Rodrigo R. Resende and Antonio H. Martins
Affiliation:
Keywords: SELEX, aptamer, therapeutic agent, high-throughput screening
Abstract: The systematic evolution of ligands by exponential enrichment (SELEX) is a combinatorial oligonucleotide library- based in vitro selection approach in which DNA or RNA molecules are selected by their ability to bind their targets with high affinity and specificity, comparable to those of antibodies. Nucleic acids with high affinity for their targets have been selected against a wide variety of compounds, from small molecules, such as ATP, to membrane proteins and even whole organisms. Recently, the use of the SELEX technique was extended to isolate oligonucleotide ligands, also known as aptamers, for a wide range of proteins of importance for therapy and diagnostics, such as growth factors and cell surface antigens. The number of aptamers generated as inhibitors of various target proteins has increased following automatization of the SELEX process. Their diagnostic and therapeutic efficacy can be enhanced by introducing chemical modifications into the oligonucleotides to provide resistance against enzymatic degradation in body fluids. Several aptamers are currently being tested in preclinical and clinical trials, and aptamers are in the process of becoming a new class of therapeutic agents. Recently, the anti-VEGF aptamer pegaptanib received FDA approval for treatment of human ocular vascular disease.
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Cite this article as:
Ulrich Henning, Trujillo A. Cleber, Nery A. Arthur, Alves M. Janaina, Majumder Paromita, Resende R. Rodrigo and Martins H. Antonio, DNA and RNA Aptamers: From Tools for Basic Research Towards Therapeutic Applications, Combinatorial Chemistry & High Throughput Screening 2006; 9 (8) . https://dx.doi.org/10.2174/138620706778249695
DOI https://dx.doi.org/10.2174/138620706778249695 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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