- search hit 1 of 1
Antagonists of the miRNA-Argonaute 2 Protein Complex
- microRNAs (miRNAs) have been identified as high-value drug targets. A widely applied strategy in miRNA inhibition is the use of antisense agents. However, it has been shown that oligonucleotides are poorly cell permeable because of their complex chemical structure and due to their negatively charged backbone. Consequently, the general application of oligonucleotides in therapy is limited. Since miRNAs’ functions are executed exclusively by the Argonaute 2 protein, we therefore describe a protocol for the design of a novel miRNA inhibitor class: antagonists of the miRNA-Argonaute 2 protein complex, so-called anti-miR-AGOs, that not only block the crucial binding site of the target miRNA but also bind to the protein’s active site. Due to their lower molecular weight and, thus, more drug-like chemical structure, the novel inhibitor class may show better pharmacokinetic properties than reported oligonucleotide inhibitors, enabling them for potential therapeutic use.
Author details: | Marco F. SchmidtORCiDGND, Oliver KorbORCiD, Chris Abell |
---|---|
DOI: | https://doi.org/10.1007/978-1-4939-6563-2_17 |
ISBN: | 978-1-4939-6563-2 |
ISBN: | 978-1-4939-6561-8 |
ISBN: | 978-1-4939-8236-3 |
ISSN: | 1064-3745 |
ISSN: | 1940-6029 |
Pubmed ID: | https://pubmed.ncbi.nlm.nih.gov/27924487 |
Title of parent work (English): | Drug Target miRNA: Methods and Protocols |
Subtitle (English): | Anti-miR-AGOs |
Publisher: | Springer |
Place of publishing: | New York |
Publication type: | Article |
Language: | English |
Date of first publication: | 2016/12/07 |
Publication year: | 2017 |
Release date: | 2022/09/23 |
Tag: | Drug design; miRNA inhibitors; miRNA seed region; miRNA-Argonaute 2 protein complex; microRNA |
Volume: | 1517 |
Number of pages: | 11 |
First page: | 239 |
Last Page: | 249 |
Organizational units: | Mathematisch-Naturwissenschaftliche Fakultät / Institut für Chemie |
DDC classification: | 5 Naturwissenschaften und Mathematik / 54 Chemie / 540 Chemie und zugeordnete Wissenschaften |
6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit | |
Peer review: | Referiert |