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Literature summary for 3.1.13.2 extracted from

  • Wendeler, M.; Lee, H.F.; Bermingham, A.; Miller, J.T.; Chertov, O.; Bona, M.K.; Baichoo, N.S.; Ehteshami, M.; Beutler, J.; OKeefe, B.R.; Goette, M.; Kvaratskhelia, M.; Le Grice, S.
    Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity (2008), ACS Chem. Biol., 3, 635-644.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.13.2

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Human immunodeficiency virus 1

Protein Variants

Protein Variants Comment Organism
Y501Az-F p-azido-L-phenylalanine (Az-F), site-directed mutagenesis, sensitivity of HIV-1 reverse transcriptase Tyr501 variants to NSC727447 inhibition tested Human immunodeficiency virus 1
Y501Bp-F p-benzoyl-L-phenylalanine, site-directed mutagenesis, sensitivity of HIV-1 reverse transcriptase Tyr501 variants to NSC727447 inhibition tested Human immunodeficiency virus 1
Y501F site-directed mutagenesis, sensitivity of HIV-1 reverse transcriptase Tyr501 variants to NSC727447 inhibition tested Human immunodeficiency virus 1
Y501W site-directed mutagenesis, sensitivity of HIV-1 reverse transcriptase Tyr501 variants to NSC727447 inhibition tested Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide NSC727447 Human immunodeficiency virus 1
2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide NSC727447 Human immunodeficiency virus 2
beta-thujaplicinol
-
 Human immunodeficiency virus 1
beta-thujaplicinol
-
 Human immunodeficiency virus 2
manicol
-
 Human immunodeficiency virus 1
manicol
-
 Human immunodeficiency virus 2
N-[3-(aminocarbonyl)-4,5-dimethyl-2-thienyl]-2-furancarboxamide NSC727448 Human immunodeficiency virus 1
N-[3-(aminocarbonyl)-4,5-dimethyl-2-thienyl]-2-furancarboxamide NSC727448 Human immunodeficiency virus 2

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-
Human immunodeficiency virus 2
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Human immunodeficiency virus 1

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information RNaseH assays are performed using an 18-nucleotide 3'-fluorescein-labeled RNA annealed to a complementary 18-nucleotide 5'-dabcyl-conjugated DNA. The increase in fluorescence as a result of RNase H hydrolysis is monitored with a Spectramax Gemini EM fluorescence spectrometer Human immunodeficiency virus 1 ?
-
 ?

Synonyms

Synonyms Comment Organism
reverse transcriptase-associated ribonuclease H
-
 Human immunodeficiency virus 1
reverse transcriptase-associated ribonuclease H
-
 Human immunodeficiency virus 2
ribonuclease H
-
 Human immunodeficiency virus 1
ribonuclease H
-
 Human immunodeficiency virus 2
RNase H domain of reverse transcriptase Human immunodeficiency virus 1
RNase H domain of reverse transcriptase Human immunodeficiency virus 2

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.002
-
 pH 8.0, 37°C Human immunodeficiency virus 1 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
0.0025
-
 pH 8.0, 37°C Human immunodeficiency virus 2 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
0.0032
-
 pH 8.0, 37°C Human immunodeficiency virus 1 N-[3-(aminocarbonyl)-4,5-dimethyl-2-thienyl]-2-furancarboxamide
0.005
-
 pH 8.0, 37°C Human immunodeficiency virus 2 N-[3-(aminocarbonyl)-4,5-dimethyl-2-thienyl]-2-furancarboxamide
0.0066
-
 wild-type, pH 8.0, 37°C Human immunodeficiency virus 1 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
0.02
-
 Y501F mutant, pH 8.0, 37°C Human immunodeficiency virus 1 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
0.0706
-
 Y501W mutant, pH 8.0, 37°C Human immunodeficiency virus 1 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
0.0896
-
 Y501Az-F mutant, pH 8.0, 37°C Human immunodeficiency virus 1 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
0.1967
-
 Y501Bp-F mutant, pH 8.0, 37°C Human immunodeficiency virus 1 2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide