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Antimicrob Agents Chemother ; 55(10): 4735-41, 2011 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-21768506

RESUMEN

A single polypeptide of the HIV-1 reverse transcriptase that reconstituted Mg(2+)-dependent RNase H activity has been made. Using molecular modeling, the construct was designed to encode the p51 subunit joined by a linker to the thumb (T), connection (C), and RNase H (R) domains of p66. This p51-G-TCR construct was purified from the soluble fraction of an Escherichia coli strain, MIC2067(DE3), lacking endogenous RNase HI and HII. The p51-G-TCR RNase H construct displayed Mg(2+)-dependent activity using a fluorescent nonspecific assay and showed the same cleavage pattern as HIV-1 reverse transcriptase (RT) on substrates that mimic the tRNA removal required for second-strand transfer reactions. The mutant E706Q (E478Q in RT) was purified under similar conditions and was not active. The RNase H of the p51-G-TCR RNase H construct and wild type HIV-1 RT had similar K(m)s for an RNA-DNA hybrid substrate and showed similar inhibition kinetics to two known inhibitors of the HIV-1 RT RNase H.


Asunto(s)
Fármacos Anti-VIH/farmacología , Transcriptasa Inversa del VIH/metabolismo , VIH-1/enzimología , Inhibidores de la Transcriptasa Inversa/farmacología , Ribonucleasa H/metabolismo , Secuencia de Aminoácidos , Secuencia de Bases , Evaluación Preclínica de Medicamentos , Transcriptasa Inversa del VIH/química , Transcriptasa Inversa del VIH/genética , VIH-1/genética , VIH-1/metabolismo , Magnesio/metabolismo , Modelos Moleculares , ARN de Transferencia/genética , Ribonucleasa H/química , Ribonucleasa H/genética , Análisis de Secuencia de ARN
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