Tethering in RNA: An RNA-Binding Fragment Discovery Tool
Tethering has been extensively used to study small molecule interactions with proteins through reversible disulfide bond forming reactions to cysteine residues. We describe the adaptation of Tethering to the study of small molecule binding to RNA using a thiol-containing adenosine analog (ASH). Amon...
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| Format: | Article |
| Language: | English |
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MDPI AG
2015-03-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/20/3/4148 |
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doaj-7fafe09261c04f1795fc26f9cf7667ff2020-11-24T20:56:01ZengMDPI AGMolecules1420-30492015-03-012034148416110.3390/molecules20034148molecules20034148Tethering in RNA: An RNA-Binding Fragment Discovery ToolKiet Tran0Michelle R. Arkin1Peter A. Beal2Department of Chemistry, University of California, One Shields Ave, Davis, CA 95616, USASmall Molecule Discovery Center, Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94158, USADepartment of Chemistry, University of California, One Shields Ave, Davis, CA 95616, USATethering has been extensively used to study small molecule interactions with proteins through reversible disulfide bond forming reactions to cysteine residues. We describe the adaptation of Tethering to the study of small molecule binding to RNA using a thiol-containing adenosine analog (ASH). Among 30 disulfide-containing small molecules screened for efficient Tethering to ASH-bearing RNAs derived from pre-miR21, a benzotriazole-containing compound showed prominent adduct formation and selectivity for one of the RNAs tested. The results of this screen demonstrate the viability of using thiol-modified nucleic acids to discover molecules with binding affinity and specificity for the purpose of therapeutic compound lead discovery.http://www.mdpi.com/1420-3049/20/3/4148TetheringmiRNAnucleoside analog |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Kiet Tran Michelle R. Arkin Peter A. Beal |
| spellingShingle |
Kiet Tran Michelle R. Arkin Peter A. Beal Tethering in RNA: An RNA-Binding Fragment Discovery Tool Molecules Tethering miRNA nucleoside analog |
| author_facet |
Kiet Tran Michelle R. Arkin Peter A. Beal |
| author_sort |
Kiet Tran |
| title |
Tethering in RNA: An RNA-Binding Fragment Discovery Tool |
| title_short |
Tethering in RNA: An RNA-Binding Fragment Discovery Tool |
| title_full |
Tethering in RNA: An RNA-Binding Fragment Discovery Tool |
| title_fullStr |
Tethering in RNA: An RNA-Binding Fragment Discovery Tool |
| title_full_unstemmed |
Tethering in RNA: An RNA-Binding Fragment Discovery Tool |
| title_sort |
tethering in rna: an rna-binding fragment discovery tool |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2015-03-01 |
| description |
Tethering has been extensively used to study small molecule interactions with proteins through reversible disulfide bond forming reactions to cysteine residues. We describe the adaptation of Tethering to the study of small molecule binding to RNA using a thiol-containing adenosine analog (ASH). Among 30 disulfide-containing small molecules screened for efficient Tethering to ASH-bearing RNAs derived from pre-miR21, a benzotriazole-containing compound showed prominent adduct formation and selectivity for one of the RNAs tested. The results of this screen demonstrate the viability of using thiol-modified nucleic acids to discover molecules with binding affinity and specificity for the purpose of therapeutic compound lead discovery. |
| topic |
Tethering miRNA nucleoside analog |
| url |
http://www.mdpi.com/1420-3049/20/3/4148 |
| work_keys_str_mv |
AT kiettran tetheringinrnaanrnabindingfragmentdiscoverytool AT michellerarkin tetheringinrnaanrnabindingfragmentdiscoverytool AT peterabeal tetheringinrnaanrnabindingfragmentdiscoverytool |
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1716791083479859200 |