Dependence of aptamer activity on opposed terminal extensions : improvement of light-regulation efficiency
- Aptamers that can be regulated with light allow precise control of protein activity in space and time and hence of biological function in general. In a previous study, we showed that the activity of the thrombin-binding aptamer HD1 can be turned off by irradiation using a light activatable "caged" intramolecular antisense-domain. However, the activity of the presented aptamer in its ON state was only mediocre. Here we studied the nature of this loss in activity in detail and found that switching from 5'- to 3'-extensions affords aptamers that are even more potent than the unmodified HD1. In particular we arrived at derivatives that are now more active than the aptamer NU172 that is currently in phase 2 clinical trials as an anticoagulant. As a result, we present light-regulatable aptamers with a superior activity in their ON state and an almost digital ON/OFF behavior upon irradiation.
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| Author: | Maximilian Buff, Florian Schäfer, Bernhard Wulffen, Jens MüllerORCiDGND, Bernd Pötzsch, Alexander HeckelORCiDGND, Günter Mayer |
|---|---|
| URN: | urn:nbn:de:hebis:30-85087 |
| DOI: | https://doi.org/10.1093/nar/gkp1148 |
| ISSN: | 1362-4962 |
| ISSN: | 0305-1048 |
| Pubmed Id: | https://pubmed.ncbi.nlm.nih.gov/20007153 |
| Parent Title (English): | Nucleic acids research |
| Publisher: | Oxford Univ. Press |
| Place of publication: | Oxford |
| Document Type: | Article |
| Language: | English |
| Date of Publication (online): | 2010/11/12 |
| Year of first Publication: | 2009 |
| Publishing Institution: | Universitätsbibliothek Johann Christian Senckenberg |
| Release Date: | 2010/11/12 |
| Tag: | anticoagulants; blood coagulation; coagulation process; thrombin |
| Volume: | 38 |
| Issue: | 6 |
| Page Number: | 8 |
| First Page: | 2111 |
| Last Page: | 2118 |
| Note: | © The Author(s) 2009. Published by Oxford University Press. This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/2.5), which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. |
| Source: | Nucleic Acids Research, vol. 38, no. 6, S. 2111-2118 ; doi: 10.1093/nar/gkp1148 ; First published online: December 8, 2009 |
| HeBIS-PPN: | 230020453 |
| Institutes: | Biochemie, Chemie und Pharmazie / Biochemie und Chemie |
| Dewey Decimal Classification: | 5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie |
| Sammlungen: | Universitätspublikationen |
| Sammlung Biologie / Sondersammelgebiets-Volltexte | |
| Licence (German): |  Creative Commons - Namensnennung-Nicht kommerziell 3.0 |
