Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a drug target | Human immunodeficiency virus 1 |
Protein Variants | Comment | Organism |
---|---|---|
K103N | site-directed mutagenesis, the DNA polymerase function of the enzyme is sensitive to alizarine inhibitors like the wild-type enzyme | Human immunodeficiency virus 1 |
Y181C | site-directed mutagenesis, the DNA polymerase function of the enzyme is insensitive to alizarine inhibitors | Human immunodeficiency virus 1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1,2-bis(2-oxopropoxy)anthracene-9,10-dione | - |
Human immunodeficiency virus 1 | |
1,2-bis[(3-oxobutan-2-yl)oxy]anthracene-9,10-dione | - |
Human immunodeficiency virus 1 | |
2-[2-(4-bromophenyl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
2-[2-(biphenyl-4-yl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-2-(2-oxo-2-phenylethoxy)-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-2-(2-oxopropoxy)-9,10-dihydroanthracen-1-yl acetate | noncompetitive inhibitor, KNA-53 inhibits the RNase H function and is inactive on the polymerase function of enzyme mutant Y181C | Human immunodeficiency virus 1 | |
9,10-dioxo-2-(prop-2-en-1-yloxy)-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-2-(prop-2-yn-1-yloxy)-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-2-[(2-oxopentan-3-yl)oxy]-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-2-[(3-oxobutan-2-yl)oxy]-9,10-dihydroanthracen-1-yl acetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl diacetate | - |
Human immunodeficiency virus 1 | |
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate | noncompetitive inhibitor | Human immunodeficiency virus 1 | |
alizarin | - |
Human immunodeficiency virus 1 | |
efavirenz | - |
Human immunodeficiency virus 1 | |
additional information | alizarine derivatives as dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases, molecular docking and molecular dynamic simulation, overview | Human immunodeficiency virus 1 |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Human immunodeficiency virus 1 |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
deoxynucleoside triphosphate + DNAn | Human immunodeficiency virus 1 | - |
diphosphate + DNAn+1 | - |
? | |
additional information | Human immunodeficiency virus 1 | the viral DNA polymerase activity can be both RNA and DNA dependent, see also EC 2.7.7.7 | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
deoxynucleoside triphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
additional information | the viral DNA polymerase activity can be both RNA and DNA dependent, see also EC 2.7.7.7 | Human immunodeficiency virus 1 | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
DNA polymerase | - |
Human immunodeficiency virus 1 |
HIV-1 reverse transcriptase | - |
Human immunodeficiency virus 1 |
HIV-1 RT | - |
Human immunodeficiency virus 1 |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000003 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | efavirenz | |
0.005 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[2-(4-bromophenyl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate | |
0.006 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[2-(biphenyl-4-yl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate | |
0.012 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate | |
0.014 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 1,2-bis(2-oxopropoxy)anthracene-9,10-dione | |
0.06 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-2-(2-oxo-2-phenylethoxy)-9,10-dihydroanthracen-1-yl acetate | |
0.061 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-2-[(3-oxobutan-2-yl)oxy]-9,10-dihydroanthracen-1-yl acetate | |
0.079 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | alizarin | |
0.082 | - |
pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-2-(prop-2-en-1-yloxy)-9,10-dihydroanthracen-1-yl acetate | |
0.1 | - |
above, pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-2-(prop-2-yn-1-yloxy)-9,10-dihydroanthracen-1-yl acetate | |
0.1 | - |
above, pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-9,10-dihydroanthracene-1,2-diyl diacetate | |
0.1 | - |
above, pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-2-(2-oxopropoxy)-9,10-dihydroanthracen-1-yl acetate | |
0.1 | - |
above, pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 9,10-dioxo-2-[(2-oxopentan-3-yl)oxy]-9,10-dihydroanthracen-1-yl acetate | |
0.1 | - |
above, pH and temperature not specified in the publication | Human immunodeficiency virus 1 | 1,2-bis[(3-oxobutan-2-yl)oxy]anthracene-9,10-dione |
General Information | Comment | Organism |
---|---|---|
physiological function | HIV-1 reverse transcriptase has two associated activities, DNA polymerase and RNase H, both essential for viral replication | Human immunodeficiency virus 1 |