Key result
Increasing the positive charge in the RNA-binding domain of chemical ribonucleases from +2 to +4 resulted in a significant growth in ribonuclease activity against an HIV-1 RNA fragment.
Increasing the positive charge of chemical ribonucleases enhances their ability to cleave HIV-1 RNA fragments.
May guide antiviral ribonuclease design; leaves open translation to in vivo HIV efficacy.
The effect of the total positive charge in the RNA-binding domain of chemical ribonucleases that are conjugates of bisquaternary salts of diazabicyclo[2.2.2]octane and imidazol on the cleavage of an HIV-1 RNA fragment was studied. An increase in the positive charge from +2 to +4 was shown to result in a significant growth in the ribonuclease activity. Possible mechanisms of the interactions between structural moieties of chemical ribonucleases and RNA that enable an effective catalysis of the cleavage of phosphodiester bonds are discussed.
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Tamkovich et al. (2007) studied this question. Chemical ribonucleases with increased positive charge in the RNA-binding domain was evaluated on Cleavage of an HIV-1 RNA fragment. Increasing the positive charge in the RNA-binding domain of chemical ribonucleases from +2 to +4 resulted in a significant growth in ribonuclease activity against an HIV-1 RNA fragment.
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