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Literature summary for 3.1.26.13 extracted from

  • Ngoutane Mfopa, A.; Corona, A.; Eloh, K.; Tramontano, E.; Frau, A.; Boyom, F.F.; Caboni, P.; Tocco, G.
    Uvaria angolensis as a promising source of inhibitors of HIV-1 RT-associated RNA-dependent DNA polymerase and RNase H functions (2018), Nat. Prod. Res., 32, 640-647 .
    View publication on PubMed

Application

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

Inhibitors

Inhibitors Comment Organism Structure
6-[1-(4-fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester i.e. RDS1643, RNase H inhibitor Human immunodeficiency virus 1
EDTA
-
Human immunodeficiency virus 1
additional information extracts of Uvaria angolensis from tropical zone of Cameroon (Mount Kalla in Yaounde City) are a promising source of inhibitors of HIV-1 reverse transcriptase-associated RNA-dependent DNA polymerase (RDDP) and HIV-1 RNase H functions. Usage of stem bark methanol extract that inhibits both HIV-1 RNase H function and RDDP activity with IC50 values of 0.001 mg/ml and 0.00062 mg/ml, respectively, and, after been fractionated with different solvents, its solid residue shows an IC50 of 0.00010 mg/ml and of 0.00023 mg/ml against RNase H and RDDP, respectively. Methanol and water extracts from leaves and twigs, are also effective but much less than stem bark extracts. Determination of cytotoxicity Human immunodeficiency virus 1
RDS1643 RNase H inhibitor 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
-

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Human immunodeficiency virus 1

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
assay at Human immunodeficiency virus 1

General Information

General Information Comment Organism
physiological function HIV-1 reverse trancriptase (RT) is a key multifunctional enzyme which combines an RNA-dependent DNA polymerase activity (RDDP) and a ribonuclease H (RNase H) function, both essential for the viral genome replication Human immunodeficiency virus 1