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Literature summary for 2.7.7.49 extracted from

  • Esposito, F.; Kharlamova, T.; Distinto, S.; Zinzula, L.; Cheng, Y.C.; Dutschman, G.; Floris, G.; Markt, P.; Corona, A.; Tramontano, E.
    Alizarine derivatives as new 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 (2011), FEBS J., 278, 1444-1457.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.7.49

Application

Application Comment Organism
drug development the enzyme is a drug target Human immunodeficiency virus 1

Protein Variants

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

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

Metals/Ions Comment Organism Structure
Mg2+ required Human immunodeficiency virus 1

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

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

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 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

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