Cloned (Comment) | Organism |
---|---|
expression of wild-type enzyme and mutant enzymes I132A, I132M, I135A, I135M, N136A, N137A, E138A, E138K, T139A, T139V or P140A in Escherichia coli | Human immunodeficiency virus 1 |
Protein Variants | Comment | Organism |
---|---|---|
I132A | mutation confers low-level resistance to nevirapine and delavirdine | Human immunodeficiency virus 1 |
I132M | mutation confers high-level resistance to nevirapine and delavirdine (more than 10fold) and low-level resistance (about 2fold) to efavirenz | Human immunodeficiency virus 1 |
I135A | mutation confers high level resistance to nevirapine and delavirdine, but not to efavirenz | Human immunodeficiency virus 1 |
I135M | mutation confers low-level resistance (about 2fold) to nevirapine, delavirdine and efavirenz | Human immunodeficiency virus 1 |
N136A | mutant enzyme with very low reverse transcriptase activity | Human immunodeficiency virus 1 |
N137A | mutation confers no resistance to nevirapine, delavirdine and efavirenz | Human immunodeficiency virus 1 |
P140A | mutant enzyme with very low reverse transcriptase activity | Human immunodeficiency virus 1 |
T139A | mutant enzyme with very low reverse transcriptase activity | Human immunodeficiency virus 1 |
T139V | mutation confers no resistance to nevirapine, delavirdine and efavirenz | Human immunodeficiency virus 1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3'-azido-2',3'-dideoxythymidine-5'-triphosphate | - |
Human immunodeficiency virus 1 | |
3'-dideoxythymidine triphosphate | - |
Human immunodeficiency virus 1 | |
d4T-TP | - |
Human immunodeficiency virus 1 | |
Delavirdine | - |
Human immunodeficiency virus 1 | |
efavirenz | - |
Human immunodeficiency virus 1 | |
nevirapine | - |
Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | P03366 | - |
- |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00002 | - |
mutant enzyme I132A | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00003 | - |
mutant enzyme E138A | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00003 | - |
mutant enzyme I132M | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00004 | - |
mutant enzyme I135A | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00006 | - |
mutant enzyme I132M | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.00006 | - |
mutant enzyme I135M | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00006 | - |
mutant enzyme N137A | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00006 | - |
mutant enzyme T139V | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00006 | - |
wild-type enzyme | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00007 | - |
mutant enzyme E138K | Human immunodeficiency virus 1 | 3'-azido-2',3'-dideoxythymidine-5'-triphosphate | |
0.00007 | - |
mutant enzyme I132A | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.00008 | - |
mutant enzyme I135A | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.000087 | - |
mutant enzyme N137A | Human immunodeficiency virus 1 | efavirenz | |
0.00009 | - |
mutant enzyme E138A | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.00009 | - |
mutant enzyme I132A | Human immunodeficiency virus 1 | efavirenz | |
0.00009 | - |
mutant enzyme I135M | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.0000942 | - |
wild-type enzyme | Human immunodeficiency virus 1 | efavirenz | |
0.0001 | - |
mutant enzyme E138K | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.0001 | - |
mutant enzyme N137A | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.0001 | - |
mutant enzyme T139V | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.0001 | - |
wild-type enzyme | Human immunodeficiency virus 1 | 3'-dideoxythymidine triphosphate | |
0.000113 | - |
mutant enzyme T139V | Human immunodeficiency virus 1 | efavirenz | |
0.00012 | - |
mutant enzyme I132M | Human immunodeficiency virus 1 | d4T-TP | |
0.00013 | - |
mutant enzyme I132A | Human immunodeficiency virus 1 | d4T-TP | |
0.00014 | - |
mutant enzyme T139V | Human immunodeficiency virus 1 | d4T-TP | |
0.00016 | - |
mutant enzyme E138A | Human immunodeficiency virus 1 | d4T-TP | |
0.00016 | - |
mutant enzyme E138K | Human immunodeficiency virus 1 | d4T-TP | |
0.00016 | - |
mutant enzyme I135A | Human immunodeficiency virus 1 | d4T-TP | |
0.00017 | - |
mutant enzyme I135M | Human immunodeficiency virus 1 | d4T-TP | |
0.00018 | - |
mutant enzyme N137A | Human immunodeficiency virus 1 | d4T-TP | |
0.000188 | - |
mutant enzyme E138A | Human immunodeficiency virus 1 | efavirenz | |
0.000188 | - |
mutant enzyme I135A | Human immunodeficiency virus 1 | efavirenz | |
0.000197 | - |
mutant enzyme I135M | Human immunodeficiency virus 1 | efavirenz | |
0.0002 | - |
wild-type enzyme | Human immunodeficiency virus 1 | d4T-TP | |
0.000216 | - |
mutant enzyme E138K | Human immunodeficiency virus 1 | efavirenz | |
0.000432 | - |
mutant enzyme I132M | Human immunodeficiency virus 1 | efavirenz | |
0.00152 | - |
mutant enzyme N137A | Human immunodeficiency virus 1 | Delavirdine | |
0.00218 | - |
wild-type enzyme | Human immunodeficiency virus 1 | Delavirdine | |
0.00261 | - |
mutant enzyme T139V | Human immunodeficiency virus 1 | Delavirdine | |
0.00392 | - |
mutant enzyme I135M | Human immunodeficiency virus 1 | Delavirdine | |
0.0065 | - |
mutant enzyme N137A | Human immunodeficiency virus 1 | nevirapine | |
0.0072 | - |
wild-type enzyme | Human immunodeficiency virus 1 | nevirapine | |
0.00762 | - |
mutant enzyme E138A | Human immunodeficiency virus 1 | Delavirdine | |
0.0087 | - |
mutant enzyme I132A | Human immunodeficiency virus 1 | Delavirdine | |
0.0123 | - |
mutant enzyme T139V | Human immunodeficiency virus 1 | nevirapine | |
0.013 | - |
mutant enzyme E138K | Human immunodeficiency virus 1 | Delavirdine | |
0.0137 | - |
mutant enzyme E138A | Human immunodeficiency virus 1 | nevirapine | |
0.0159 | - |
mutant enzyme E138K | Human immunodeficiency virus 1 | nevirapine | |
0.018 | - |
mutant enzyme I132A | Human immunodeficiency virus 1 | nevirapine | |
0.0302 | - |
mutant enzyme I132M | Human immunodeficiency virus 1 | Delavirdine | |
0.0346 | - |
mutant enzyme I135A | Human immunodeficiency virus 1 | Delavirdine | |
0.0389 | - |
mutant enzyme I135M | Human immunodeficiency virus 1 | nevirapine | |
0.062 | - |
mutant enzyme I132M | Human immunodeficiency virus 1 | nevirapine | |
0.087 | - |
mutant enzyme I135A | Human immunodeficiency virus 1 | nevirapine |