Novel high-throughput screen identifies an HIV-1 reverse transcriptase inhibitor with a unique mechanism of action.

@article{Sheen2014NovelHS,
  title={Novel high-throughput screen identifies an HIV-1 reverse transcriptase inhibitor with a unique mechanism of action.},
  author={C C Sheen and Onur Alpt{\"u}rk and Nicolas Sluis-Cremer},
  journal={The Biochemical journal},
  year={2014},
  volume={462 3},
  pages={425-32}
}
HIV-1 resistance to zidovudine [AZT (azidothymidine)] is associated with selection of the mutations M41L, D67N, K70R, L210W, T215F/Y and K219Q/E in RT (reverse transcriptase). These mutations decrease HIV-1 susceptibility to AZT by augmenting RT's ability to excise the chain-terminating AZT-MP (AZT-monophosphate) moiety from the chain-terminated DNA primer. Although AZT-MP excision occurs at the enzyme's polymerase active site, it is mechanistically distinct from the DNA polymerase reaction… CONTINUE READING

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HIV InfectionsMay be treated byZidovudine
HIV-1 resistance to zidovudine [ AZT ( azidothymidine ) ] is associated with selection of the mutations M41L , D67N , K70R , L210W , T215F / Y and K219Q / E in RT ( reverse transcriptase ) .
HIV-1 resistance to zidovudine [ AZT ( azidothymidine ) ] is associated with selection of the mutations M41L , D67N , K70R , L210W , T215F / Y and K219Q / E in RT ( reverse transcriptase ) .
HIV-1 resistance to zidovudine [ AZT ( azidothymidine ) ] is associated with selection of the mutations M41L , D67N , K70R , L210W , T215F / Y and K219Q / E in RT ( reverse transcriptase ) .
Consequently , this activity represents a novel target for drug discovery , and inhibitors that target this activity may increase the efficacy of nucleoside / nucleotide analogues , and may help to delay the onset of drug resistance .
Consequently , this activity represents a novel target for drug discovery , and inhibitors that target this activity may increase the efficacy of nucleoside / nucleotide analogues , and may help to delay the onset of drug resistance .
Consequently , this activity represents a novel target for drug discovery , and inhibitors that target this activity may increase the efficacy of nucleoside / nucleotide analogues , and may help to delay the onset of drug resistance .
Consequently , this activity represents a novel target for drug discovery , and inhibitors that target this activity may increase the efficacy of nucleoside / nucleotide analogues , and may help to delay the onset of drug resistance .
HIV-1 resistance to zidovudine [ AZT ( azidothymidine ) ] is associated with selection of the mutations M41L , D67N , K70R , L210W , T215F / Y and K219Q / E in RT ( reverse transcriptase ) .
HIV-1 resistance to zidovudine [ AZT ( azidothymidine ) ] is associated with selection of the mutations M41L , D67N , K70R , L210W , T215F / Y and K219Q / E in RT ( reverse transcriptase ) .
HIV-1 resistance to zidovudine [ AZT ( azidothymidine ) ] is associated with selection of the mutations M41L , D67N , K70R , L210W , T215F / Y and K219Q / E in RT ( reverse transcriptase ) .
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