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Literature summary for 3.1.26.13 extracted from

  • Corona, A.; Di Leva, F.S.; Thierry, S.; Pescatori, L.; Cuzzucoli Crucitti, G.; Subra, F.; Delelis, O.; Esposito, F.; Rigogliuso, G.; Costi, R.; Cosconati, S.; Novellino, E.; Di Santo, R.; Tramontano, E.
    Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by diketo acid derivatives (2014), Antimicrob. Agents Chemother., 58, 6101-6110.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
N474A the mutant shows about 40fold reduced kcat value compared to the wild type enzyme Human immunodeficiency virus 1
Q475A the mutant shows about 10fold reduced kcat value compared to the wild type enzyme Human immunodeficiency virus 1
R448A the mutant shows about 3fold reduced kcat value compared to the wild type enzyme Human immunodeficiency virus 1
R557A the mutant shows about 5fold reduced kcat value compared to the wild type enzyme Human immunodeficiency virus 1
Y501A the mutant shows about 400fold reduced kcat valuecompared to the wild type enzyme Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
(5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
Human immunodeficiency virus 1
(5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
Human immunodeficiency virus 1
(5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
Human immunodeficiency virus 1
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
Human immunodeficiency virus 1
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
-
Human immunodeficiency virus 1
(5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
-
Human immunodeficiency virus 1
beta-thujaplicinol
-
Human immunodeficiency virus 1
ethyl (5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
Human immunodeficiency virus 1
ethyl (5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate selectively inhibits RNase H activity in the low micromolar range Human immunodeficiency virus 1
ethyl (5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
Human immunodeficiency virus 1
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
Human immunodeficiency virus 1
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
-
Human immunodeficiency virus 1
ethyl (5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
-
Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000029
-
RNA-DNA hybrid mutant enzyme Y501A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.00003
-
RNA-DNA hybrid mutant enzyme N474A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.000041
-
RNA-DNA hybrid mutant enzyme R557A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.000085
-
RNA-DNA hybrid mutant enzyme R448A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.0001
-
RNA-DNA hybrid mutant enzyme Q475A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.000126
-
RNA-DNA hybrid wild type enzyme, at pH 7.8 and 37°C 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.
RNA-DNA hybrid + H2O 5'-GTTTTCTTTTCCCCCCTGAC-3'-fluorescein/5'-CAAAAGAAAAGGGGGGACUG-3'-dabcyl Human immunodeficiency virus 1 ?
-
?

Synonyms

Synonyms Comment Organism
RNase H
-
Human immunodeficiency virus 1

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.004
-
RNA-DNA hybrid mutant enzyme Y501A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.04
-
RNA-DNA hybrid mutant enzyme N474A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.18
-
RNA-DNA hybrid mutant enzyme Q475A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.42
-
RNA-DNA hybrid mutant enzyme R557A, at pH 7.8 and 37°C Human immunodeficiency virus 1
0.73
-
RNA-DNA hybrid mutant enzyme R448A, at pH 7.8 and 37°C Human immunodeficiency virus 1
1.9
-
RNA-DNA hybrid wild type enzyme, at pH 7.8 and 37°C Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00007
-
mutant enzyme Y501A, at pH 7.8 and 37°C Human immunodeficiency virus 1 beta-thujaplicinol
0.00009
-
mutant enzyme N474A, at pH 7.8 and 37°C Human immunodeficiency virus 1 beta-thujaplicinol
0.00015
-
mutant enzyme R448A, at pH 7.8 and 37°C Human immunodeficiency virus 1 beta-thujaplicinol
0.00019
-
mutant enzyme Q475A, at pH 7.8 and 37°C Human immunodeficiency virus 1 beta-thujaplicinol
0.00022
-
mutant enzyme R557A, at pH 7.8 and 37°C Human immunodeficiency virus 1 beta-thujaplicinol
0.0063
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 ethyl (5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
0.0073
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 ethyl (5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
0.0077
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 (5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
0.008
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 ethyl (5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
0.0082
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 ethyl (5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
0.0086
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
0.0112
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
0.0161
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
0.0192
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 (5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
0.0193
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 (5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
0.028
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
0.087
-
at pH 7.8 and 37°C Human immunodeficiency virus 1 (5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid