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Literature summary for 3.1.26.13 extracted from

  • Billamboz, M.; Bailly, F.; Lion, C.; Touati, N.; Vezin, H.; Calmels, C.; Andreola, M.; Christ, F.; Debyser, Z.; Cotelle, P.
    Magnesium chelating 2-hydroxyisoquinoline-1,3(2H, 4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: Discovery of a novel selective inhibitor of the ribonuclease H function (2011), J. Med. Chem., 54, 1812-1824.
    View publication on PubMed
Search for more literature for 3.1.26.13

Protein Variants

Protein Variants Comment Organism
A128T the mutant strain is resistant to 2-hydroxyisoquinoline-1,3(2H,4H)-dione inhibitors in contrast to the wild-type Moloney murine leukemia virus
G140S/Q148H the mutant strain is resistant to 2-hydroxyisoquinoline-1,3(2H,4H)-dione inhibitors in contrast to the wild-type Moloney murine leukemia virus

Inhibitors

Inhibitors Comment Organism Structure
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-dione shows antiviral activity Moloney murine leukemia virus
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
-
 Moloney murine leukemia virus
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
 Moloney murine leukemia virus
2-hydroxyisoquinoline-1,3(2H,4H)-dione magnesium complex
-
 Moloney murine leukemia virus
beta-thujaplicinol
-
 Moloney murine leukemia virus
diketoacid
-
 Moloney murine leukemia virus
L-708,906
-
 Moloney murine leukemia virus
L-870,810
-
 Moloney murine leukemia virus
additional information magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain, overview. 2-Hydroxyisoquinoline-1,3(2H,4H)-dione forms a 1:1 complex with Mg2+, but a 1:2 complex with Mn2+, Moloney murine leukemia virus
raltegravir
-
 Moloney murine leukemia virus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Moloney murine leukemia virus
additional information the active site of the RNase H function contains four acidic residues, D443, E478, D498, and D549, that likely coordinate two divalent metal ions that are essential for catalysis Moloney murine leukemia virus

Organism

Organism UniProt Comment Textmining
Moloney murine leukemia virus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant enzyme Moloney murine leukemia virus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the active site of the RNase H function contains four acidic residues, D443, E478, D498, and D549, that likely coordinate two divalent metal ions that are essential for catalysis Moloney murine leukemia virus ?
-
 ?

Synonyms

Synonyms Comment Organism
RNase H
-
 Moloney murine leukemia virus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Moloney murine leukemia virus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Moloney murine leukemia virus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000061
-
 pH 8.0, 37°C Moloney murine leukemia virus 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-dione
0.0301
-
 pH 8.0, 37°C Moloney murine leukemia virus 2-hydroxyisoquinoline-1,3(2H,4H)-dione magnesium complex
0.0388
-
 pH 8.0, 37°C Moloney murine leukemia virus 2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
0.0591
-
 pH 8.0, 37°C Moloney murine leukemia virus 2-hydroxyisoquinoline-1,3(2H,4H)-dione

General Information

General Information Comment Organism
malfunction antiviral activity of 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-dione is probably due to the RNase H inhibition Moloney murine leukemia virus