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Literature summary for 3.5.4.B9 extracted from

  • Olson, M.E.; Li, M.; Harris, R.S.; Harki, D.A..
    Small-molecule APOBEC3G DNA cytosine deaminase inhibitors based on a 4-amino-1,2,4-triazole-3-thiol scaffold (2012), ChemMedChem, 8, 112-117.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
C243A/C321A/C356A the mutation has no effect on localization, deamination, oligomerization, or HIV-1 Vif-deficient restriction capabilities. The mutant is only partially resistant to inhibitor MN256.0105, with recovered deamination efficiency of 19% Homo sapiens
C321A the mutation has no effect on localization, deamination, oligomerization, or HIV-1 Vif-deficient restriction capabilities. The mutant is only partially resistant to inhibitor MN256.0105, with recovered deamination efficiency of 21% Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-amino-5-methyl-1,2,4-triazole-3-thiol
-
Homo sapiens
4-[(4-bromobenzylidene)amino]-1,2,4-triazole-3-thiol MN256.0105, 99% inhibition at 0.02 mM Homo sapiens
4-[(4-methoxybenzylidene)amino]-5-methyl-1,2,4-triazole-3-thiol
-
Homo sapiens
additional information not inhibited by 4-amino-1,2,4-triazol-3-ol, 4-amino-5-methyl-1,2,4-triazol-3-ol, 6-(4-methoxyphenyl)-3-methyl-1,2,4-triazolo[3,4-b]-[1,3,4]thiadiazole, and 3-(benzylthio)-5-methyl-1,2,4-triazol-4-amine Homo sapiens
N-(3-thio-5-methyl-1,2,4-triazol-4-yl)benzamide
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ the enzyme contains a catalytic zinc atom Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cytosine in single-stranded viral DNA + H2O Homo sapiens
-
uracil in single-stranded viral DNA + NH3
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cytosine in single-stranded viral DNA + H2O
-
Homo sapiens uracil in single-stranded viral DNA + NH3
-
?

Synonyms

Synonyms Comment Organism
A3G
-
Homo sapiens
APOBEC3G
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0039
-
at pH 7.4 and 37°C Homo sapiens 4-[(4-methoxybenzylidene)amino]-5-methyl-1,2,4-triazole-3-thiol
0.0043
-
at pH 7.4 and 37°C Homo sapiens 4-[(4-bromobenzylidene)amino]-1,2,4-triazole-3-thiol
0.0061
-
at pH 7.4 and 37°C Homo sapiens 4-amino-5-methyl-1,2,4-triazole-3-thiol
0.0082
-
at pH 7.4 and 37°C Homo sapiens N-(3-thio-5-methyl-1,2,4-triazol-4-yl)benzamide

General Information

General Information Comment Organism
physiological function the enzyme is a single-stranded DNA cytosine deaminase that functions in innate immunity against retroviruses and retrotransposons. The enzyme can potently restrict virus infectivity factor-deficient HIV-1 replication by catalyzing excessive levels of G->A hypermutation. Sublethal levels of enzyme-catalyzed mutation may contribute to the high level of HIV-1 fitness and its incurable prognosis Homo sapiens