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Literature summary for 3.1.13.2 extracted from

  • Hang, J.Q.; Li, Y.; Yang, Y.; Cammack, N.; Mirzadegan, T.; Klumpp, K.
    Substrate-dependent inhibition or stimulation of HIV RNase H activity by non-nucleoside reverse transcriptase inhibitors (NNRTIs) (2007), Biochem. Biophys. Res. Commun., 352, 341-350.
    View publication on PubMed
Search for more literature for 3.1.13.2

Protein Variants

Protein Variants Comment Organism
K103N site-directed mutagenesis, mutation of the nonnucleoside reverse transcriptase inhibitor binding site residue reduces the inhibitory effects of nonnucleoside reverse transcriptase inhibitors Human immunodeficiency virus 1
K103N/Y181C site-directed mutagenesis, mutation of the nonnucleoside reverse transcriptase inhibitor binding site residue reduces the inhibitory effects of nonnucleoside reverse transcriptase inhibitors Human immunodeficiency virus 1
Y181C site-directed mutagenesis, mutation of the nonnucleoside reverse transcriptase inhibitor binding site residue reduces the inhibitory effects of nonnucleoside reverse transcriptase inhibitors Human immunodeficiency virus 1
Y188L site-directed mutagenesis, mutation of the nonnucleoside reverse transcriptase inhibitor binding site residue reduces the inhibitory effects of nonnucleoside reverse transcriptase inhibitors Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
capravirine a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity Human immunodeficiency virus 1
efavirenz a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity Human immunodeficiency virus 1
GW8248 a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity Human immunodeficiency virus 1
additional information nonnucleoside reverse transcriptase inhibitors, i.e. NNRTIs, binding to the polymerase domain of HIV-RT interferes with RNase H activity through a long-range effect, which is affected by the structure of the RNA:DNA hybrid substrate, but is independent of NNRTI compound structure and nucleic acid substrate sequence Human immunodeficiency virus 1
nevirapine a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity Human immunodeficiency virus 1
TMC-125 a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity Human immunodeficiency virus 1

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
 i.e. HIV-1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DNA-RNA hybrid + H2O recessed 5'-end RNA substrates CGK1 annealed from RNA R1, i.e. 5'-GAAUACUCAAGCUAUGCAUC-3', and DNA D1, i.e. 5'-GATGCATAGCTTGAGTATTCTATAGTGAGTCGTATTAA-3', substrate labeling with fluorescein at the 3' end and with dabcyl at the 5' end Human immunodeficiency virus 1 ?
-
 ?
additional information HIV reverse transcriptase, HIV-RT, contains two distinct protein domains catalyzing DNA polymerase and RNase H activities Human immunodeficiency virus 1 ?
-
 ?

Subunits

Subunits Comment Organism
More the HIV RNase H domain comprises amino acid residues 427-562 of the reverse transcriptase Human immunodeficiency virus 1

Synonyms

Synonyms Comment Organism
RNase H
-
 Human immunodeficiency virus 1

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at Human immunodeficiency virus 1

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information inhibition kinetics, wild-type and mutant enzymes, overview Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000045
-
 pH 8.0, 22°C, wild-type enzyme Human immunodeficiency virus 1 efavirenz
0.0000076
-
 pH 8.0, 22°C, wild-type enzyme Human immunodeficiency virus 1 GW8248
0.0000084
-
 pH 8.0, 22°C, wild-type enzyme Human immunodeficiency virus 1 capravirine
0.0000106
-
 pH 8.0, 22°C, mutant K103N Human immunodeficiency virus 1 GW8248
0.0000108
-
 pH 8.0, 22°C, mutant Y188L Human immunodeficiency virus 1 GW8248
0.0000109
-
 pH 8.0, 22°C, mutant Y181C Human immunodeficiency virus 1 efavirenz
0.000011
-
 pH 8.0, 22°C, mutant K103N Human immunodeficiency virus 1 capravirine
0.0000121
-
 pH 8.0, 22°C, mutant Y181C Human immunodeficiency virus 1 GW8248
0.0000206
-
 pH 8.0, 22°C, mutant Y181C Human immunodeficiency virus 1 capravirine
0.0000233
-
 pH 8.0, 22°C, mutant Y188L Human immunodeficiency virus 1 capravirine
0.0000238
-
 pH 8.0, 22°C, mutant K103N/Y181C Human immunodeficiency virus 1 GW8248
0.0000281
-
 pH 8.0, 22°C, mutant K103N Human immunodeficiency virus 1 efavirenz
0.0000471
-
 pH 8.0, 22°C, mutant K103N Human immunodeficiency virus 1 TMC-125
0.0000493
-
 pH 8.0, 22°C, mutant Y188L Human immunodeficiency virus 1 efavirenz
0.0000588
-
 pH 8.0, 22°C, wild-type enzyme Human immunodeficiency virus 1 TMC-125
0.0000637
-
 pH 8.0, 22°C, mutant K103N/Y181C Human immunodeficiency virus 1 efavirenz
0.000091
-
 pH 8.0, 22°C, mutant K103N/Y181C Human immunodeficiency virus 1 capravirine
0.000098
-
 pH 8.0, 22°C, mutant Y188L Human immunodeficiency virus 1 TMC-125
0.0001034
-
 pH 8.0, 22°C, mutant Y181C Human immunodeficiency virus 1 TMC-125
0.000147
-
 pH 8.0, 22°C, mutant K103N/Y181C Human immunodeficiency virus 1 TMC-125
0.000216
-
 pH 8.0, 22°C, wild-type enzyme Human immunodeficiency virus 1 nevirapine
0.01
-
 above, pH 8.0, 22°C, mutants K103N, Y181C, Y188L, and K103N/Y181C Human immunodeficiency virus 1 nevirapine