Abstract
Novel bisimidazole-containing peptidomimetic molecules, which can efficiently cleave RNA in the absence of divalent metal ions have been synthesized. The thymidine 5'-monophosphate derivatives modified with these peptidomimetics have been obtained on CPG (controlled pore glass) using a solid phase azide-alkyne cycloaddition. The ability of all synthesized derivatives to cleave RNA has been demonstrated by a solid-phase screening method. The resulting conjugates have provided a 20–100% cleavage of the RNA target in 18 hours. The results allow us to consider the described strategy as a useful approach for the rapid selection of potentially promising peptidomimetic molecules in order to synthesize reactive constructs on their basis.
Original language | English |
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Pages (from-to) | 813-824 |
Number of pages | 12 |
Journal | Russian Journal of Bioorganic Chemistry |
Volume | 45 |
Issue number | 6 |
DOIs | |
Publication status | Published - 1 Nov 2019 |
Keywords
- artificial nucleases
- azide-alkyne cycloaddition
- CPG
- imidazole
- RNA cleavage
- solid-phase screening
- DESIGN
- CLICK CHEMISTRY
- LIGATION
- CYCLOADDITION
- NUCLEOSIDE
- PEPTIDES
- SEQUENCE-SPECIFIC CLEAVAGE
- IMIDAZOLE
- ANTISENSE OLIGONUCLEOTIDES
- RIBONUCLEASE