Use of the Fluorescent Nucleoside Analogue Benzo[g]quinazoline 2′-O-Methyl--D-ribofuranoside to Monitor the Binding of the HIV-1 Tat Protein or of Antisense Oligonucleotides to the TAR RNA Stem-Loop
| Autor: | Frédéric Godde, Jean-Jacques Toulmé, Alan G. Weeds, Serge Moreau, Michael J. Gait, Andrey A. Arzumanov |
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| Rok vydání: | 2000 |
| Předmět: |
chemistry.chemical_classification
Nucleoside analogue Organic Chemistry RNA Peptide Stem-loop Biochemistry Catalysis Inorganic Chemistry chemistry.chemical_compound Tar (tobacco residue) chemistry Recognition sequence Drug Discovery Gene expression medicine Quinazoline Physical and Theoretical Chemistry medicine.drug |
| Zdroj: | Helvetica Chimica Acta. 83:1424-1436 |
| ISSN: | 1522-2675 0018-019X |
| DOI: | 10.1002/1522-2675(20000705)83:7<1424::aid-hlca1424>3.0.co;2-d |
| Popis: | The Tat protein is an essential trans-activator of HIV gene expression. It interacts with its RNA recognition sequence, the trans-activation responsive region TAR, as well as cellular factors. These interactions are potential targets for drug discovery against HIV infection. We have developed a new and sensitive assay for the measurement of Tat binding to TAR in solution under equilibrium conditions based on the change of fluorescence of the base analogue benzo[g]quinazoline-2,4(1H,3H)-dione (BgQ) incorporated into the chemically synthesized model TAR stem-loop 2 to which was added Tat-[37-72] peptide (3). The results show that Tat-TAR binding strength is 2 – 3-fold stronger than has previously been determined by mobility-shift analysis. Changes of fluorescence were used also to measure the binding of antisense 2′-O-methyloligonucleotides to TAR 2. |
| Databáze: | OpenAIRE |
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