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Literature summary for 2.7.7.49 extracted from

  • Nissley, D.V.; Radzio, J.; Ambrose, Z.; Sheen, C.W.; Hamamouch, N.; Moore, K.L.; Tachedjian, G.; Sluis-Cremer, N.
    Characterization of novel non-nucleoside reverse transcriptase (RT) inhibitor resistance mutations at residues 132 and 135 in the 51 kDa subunit of HIV-1 RT (2007), Biochem. J., 404, 151-157.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

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

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

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

Organism UniProt Comment Textmining
Human immunodeficiency virus 1 P03366
-
-

IC50 Value

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