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Literature summary for 3.1.13.2 extracted from

  • Beilhartz, G.L.; Wendeler, M.; Baichoo, N.; Rausch, J.; Le Grice, S.; Goette, M.
    HIV-1 Reverse Transcriptase Can Simultaneously Engage Its DNA/RNA Substrate at Both DNA Polymerase and RNase H Active Sites: Implications for RNase H Inhibition (2009), J. Mol. Biol., 388, 462-474.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
Y5014-(phenylcarbonyl)-L-Phe inserting a benzophenone into the RNase H primer grip (p66501BpF/p51 reverse transcriptase) creates an enzyme that is resistant to beta-thujaplicinol at inhibitor concentrations as high as 300 microM Human immunodeficiency virus 1
Y5014-azido-L-Phe nonnatural amino acid substitution introducing an azido function Human immunodeficiency virus 1
Y501F site-directed mutagenesis. IC50 for beta-thujaplicinol is comparable to wild-type value Human immunodeficiency virus 1
Y501W site-directed mutagenesis. IC50 for beta-thujaplicinol is comparable to wild-type value Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
beta-thujaplicinol
-
Human immunodeficiency virus 1
Phosphonoformic acid inhibits both the polymerase and the RNase H activities Human immunodeficiency virus 1

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ binding of beta-thujaplicinol requires divalent metal ions Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DNA-RNA hybrid + H2O
-
Human immunodeficiency virus 1 ?
-
?

Synonyms

Synonyms Comment Organism
ribonuclease H
-
Human immunodeficiency virus 1
RNase H HIV-1 reverse transcriptase possesses DNA polymerase and RNase H activities Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
Y5014-(phenylcarbonyl)-L-Phe mutant, the IC50 value is above 300 microM Human immunodeficiency virus 1 additional information
0.000308
-
wild-type Human immunodeficiency virus 1 beta-thujaplicinol
0.000356
-
Y501W mutant Human immunodeficiency virus 1 beta-thujaplicinol
0.000386
-
Y5014-azido-L-Phe mutant Human immunodeficiency virus 1 beta-thujaplicinol
0.00047
-
Y501F mutant Human immunodeficiency virus 1 beta-thujaplicinol