Protein Variants | Comment | Organism |
---|---|---|
K103N | mutation shows only moderate effects on either polymerase or RNAse H inhibitory potencies of GW8248 and TMC-125. IC50 for nevirapine is strongly enhanced. 1.6fold decrease in IC50-value for capravirine, 18.8fold increase in IC50-value for efavirenz | Human immunodeficiency virus 1 |
K103N/Y181C | mutation shows only moderate effects on either polymerase or RNAse H inhibitory potencies of GW8248 and TMC-125. IC50 for nevirapine is strongly enhanced. 1.3fold increase in IC50-value for capravirine, 21.8fold increase in IC50-value for efavirenz | Human immunodeficiency virus 1 |
Y181C | mutation shows only moderate effects on either polymerase or RNAse H inhibitory potencies of GW8248 and TMC-125. IC50 for nevirapine is strongly enhanced. 2.1fold increase in IC50-value for capravirine, IC50 for efavirenz is nearly identical to wild-type value | Human immunodeficiency virus 1 |
Y188L | mutation shows only moderate effects on either polymerase or RNAse H inhibitory potencies of GW8248 and TMC-125. IC50 for nevirapine is strongly enhanced. 47.8fold increase in IC50-value for capravirine, 58fold increase in IC50-value for efavirenz | Human immunodeficiency virus 1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
capravirine | HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition | Human immunodeficiency virus 1 | |
efavirenz | HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition | Human immunodeficiency virus 1 | |
GW8248 | HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition | Human immunodeficiency virus 1 | |
nevirapine | HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition | Human immunodeficiency virus 1 | |
TMC-125 | HIV reverse transcriptase contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Inhibits 5'-RNA directed HIV RNase H activity of reverse transcriptase. Potency of RNase H inhibition correlats with the respective potencies of DNA polymerase inhibition | Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
- |
- |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000037 | - |
mutant enzyme Y181C | Human immunodeficiency virus 1 | efavirenz | |
0.0000039 | - |
wild-type enzyme | Human immunodeficiency virus 1 | efavirenz | |
0.0000046 | - |
mutant enzyme K103N | Human immunodeficiency virus 1 | GW8248 | |
0.0000051 | - |
mutant enzyme K103N/Y181C | Human immunodeficiency virus 1 | GW8248 | |
0.0000054 | - |
mutant enzyme K103N | Human immunodeficiency virus 1 | capravirine | |
0.0000059 | - |
mutant enzyme Y181C | Human immunodeficiency virus 1 | GW8248 | |
0.0000082 | - |
wild-type enzyme | Human immunodeficiency virus 1 | GW8248 | |
0.0000086 | - |
wild-type enzyme | Human immunodeficiency virus 1 | capravirine | |
0.0000112 | - |
mutant enzyme K103N/Y181C | Human immunodeficiency virus 1 | capravirine | |
0.0000126 | - |
mutant enzyme K103N | Human immunodeficiency virus 1 | TMC-125 | |
0.0000183 | - |
mutant enzyme Y181C | Human immunodeficiency virus 1 | capravirine | |
0.0000209 | - |
mutant enzyme Y181C | Human immunodeficiency virus 1 | TMC-125 | |
0.0000245 | - |
wild-type enzyme | Human immunodeficiency virus 1 | TMC-125 | |
0.0000324 | - |
mutant enzyme K103N/Y181C | Human immunodeficiency virus 1 | TMC-125 | |
0.0000647 | - |
mutant enzyme Y188L | Human immunodeficiency virus 1 | TMC-125 | |
0.0000679 | - |
mutant enzyme Y188L | Human immunodeficiency virus 1 | GW8248 | |
0.0000734 | - |
mutant enzyme K103N | Human immunodeficiency virus 1 | efavirenz | |
0.0000849 | - |
mutant enzyme K103N/Y181C | Human immunodeficiency virus 1 | efavirenz | |
0.000228 | - |
mutant enzyme Y188L | Human immunodeficiency virus 1 | efavirenz | |
0.000411 | - |
mutant enzyme Y188L | Human immunodeficiency virus 1 | capravirine | |
0.002217 | - |
wild-type enzyme | Human immunodeficiency virus 1 | nevirapine |