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 | 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 | Comment | Organism | Structure |
---|---|---|---|
K+ | - |
Human immunodeficiency virus 1 | |
Mg2+ | - |
Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
i.e. HIV-1 | - |
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 | Comment | Organism |
---|---|---|
More | the HIV RNase H domain comprises amino acid residues 427-562 of the reverse transcriptase | Human immunodeficiency virus 1 |
Synonyms | Comment | Organism |
---|---|---|
RNase H | - |
Human immunodeficiency virus 1 |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
22 | - |
assay at | Human immunodeficiency virus 1 |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Human immunodeficiency virus 1 |
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 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 |