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Literature summary for 3.1.26.13 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 3.1.26.13

Protein Variants

Protein Variants Comment Organism
K103N site-directed mutagenesis, the mutation does not affect RNase H function Human immunodeficiency virus 1
Y181C site-directed mutagenesis, the mutation does not affect RNase H function Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
1,2-bis(2-oxopropoxy)anthracene-9,10-dione 9% inhibition Human immunodeficiency virus 1
1,2-bis[(3-oxobutan-2-yl)oxy]anthracene-9,10-dione 20% inhibition Human immunodeficiency virus 1
1,2-dihydroxyanthracene-9,10-dione i.e. alizarine, 8% inhibition 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 10% inhibition 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 inhibits the RNase H function and is inactive on the DNA polymerase function 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 12% inhibition Human immunodeficiency virus 1
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate
-
 Human immunodeficiency virus 1
efavirenz
-
 Human immunodeficiency virus 1

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
 HIV-1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the tC5U-p12 hybrid is used as reaction substrate the RNase H activity Human immunodeficiency virus 1 ?
-
 ?

Synonyms

Synonyms Comment Organism
ribonuclease H
-
 Human immunodeficiency virus 1
RNase H
-
 Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information non competitive inhibition kinetics of alizarine derivatives, overview Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.013
-
 pH not specified in the publication, temperature not specified in the publication Human immunodeficiency virus 1 9,10-dioxo-9,10-dihydroanthracene-1,2-diyl dibenzoate
0.021
-
 pH not specified in the publication, 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
0.039
-
 pH not specified in the publication, temperature not specified in the publication Human immunodeficiency virus 1 9,10-dioxo-2-(2-oxo-2-phenylethoxy)-9,10-dihydroanthracen-1-yl acetate
0.1
-
 pH not specified in the publication, 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

General Information

General Information Comment Organism
additional information HIV-1 reverse transcriptase has two associated activities, DNA polymerase and RNase H, both essential for viral replication and validated drug targets Human immunodeficiency virus 1