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 | 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 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 | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
- |
- |
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 | Comment | Organism |
---|---|---|
RNase H | - |
Human immunodeficiency virus 1 |
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 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 |