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Literature summary extracted from

  • Ntemgwa, M.; Brenner, B.G.; Oliveira, M.; Moisi, D.; Wainberg, M.A.
    Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors (2007), Antimicrob. Agents Chemother., 51, 604-610.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.4.23.47 medicine the role of natural polymorphisms in the PR gene on the time to the development of resistance to proteinase inhibitors using an HIV-2 tissue culture model are examined. Natural polymorphisms in HIV-2 facilitate the selection of proteinase inhibitor resistance Human immunodeficiency virus 2

Protein Variants

EC Number Protein Variants Comment Organism
3.4.23.47 I50V IC50 (mM): value above 10 (amprenavir), 0.000072 (idinavir), 0.000132 (nelfinavir), 0.000316 (tipranavir), 0.000203 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I54M IC50 (mM): value above 10 (amprenavir), 0.000236 (idinavir), 0.000624 (nelfinavir), 0.001106 (tipranavir), 0.000481 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I54M/I84V IC50 (mM): value above 10 (amprenavir), 0.000388 (idinavir), 0.001747 (nelfinavir), 0.002028 (tipranavir), 0.000375 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I54M/L90M IC50 (mM): value above 10 (amprenavir), 0.001112 (idinavir), 0.002564 (nelfinavir), 0.000145 (tipranavir), 0.000524 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I54M/L99F IC50 (mM): value above 10 (amprenavir), 0.000825 (idinavir), 0.002241 (nelfinavir), 0.002908 (tipranavir), 0.000414 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I82F IC50 (mM): 0.000965 (amprenavir), 0.000544 (idinavir), 0.000244 (nelfinavir), 0.000306 (tipranavir), 0.000145 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I82L IC50 (mM): 0.000528 (amprenavir), 0.000064 (idinavir), 0.000106 (nelfinavir), 0.00016 (tipranavir), 0.000075 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 I82L/L99F IC50 (mM): 0.000098 (amprenavir), 0.000143 (idinavir), 0.000961 (nelfinavir), 0.000524 (tipranavir), 0.000496 (lopinavir) Human immunodeficiency virus 2
3.4.23.47 additional information within 10 to 15 weeks of serial passage, three major mutations: I54M, I82F, and L90M arise in HIV-2 viral cultures exposed to amprenavir, nelfinavir, indinavir, whereas I82L is selected with tripranavir. After 25 weeks, other cultures develop I50V and I84V mutations. The acquisition of the I54M, I84V, L90M, and L99F mutations result in multi-PI-resistant viruses, conferring 10fold to more than 100fold resistance Human immunodeficiency virus 2

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.47 amprenavir
-
 Human immunodeficiency virus 2
3.4.23.47 indinavir
-
 Human immunodeficiency virus 2
3.4.23.47 lopinavir
-
 Human immunodeficiency virus 2
3.4.23.47 nelfinavir
-
 Human immunodeficiency virus 2
3.4.23.47 tipranavir
-
 Human immunodeficiency virus 2

Organism

EC Number Organism UniProt Comment Textmining
3.4.23.47 Human immunodeficiency virus 2
-
-
-

Synonyms

EC Number Synonyms Comment Organism
3.4.23.47 PR
-
 Human immunodeficiency virus 2

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.23.47 0.000004
-
 wild-type Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000016
-
 wild-type Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000064
-
 wild-type Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.000064
-
 mutant I82L Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000072
-
 mutant I50V Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000075
-
 mutant I82L Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000098
-
 mutant V62A/L99F Human immunodeficiency virus 2 amprenavir
3.4.23.47 0.000106
-
 mutant I82L Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.000132
-
 mutant I50V Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.000143
-
 mutant V62A/L99F Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000145
-
 mutant I54M/L90M Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.000145
-
 mutant I82F Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.00016
-
 wild-type Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.000203
-
 mutant I50V Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000236
-
 mutant I54M Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000244
-
 mutant I82F Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.000306
-
 mutant I82F Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.000316
-
 mutant I50V Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.000375
-
 mutant I54M/L84V Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000388
-
 mutant I54M/L84V Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000414
-
 mutant I54M/L99F Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.00044
-
 wild-type Human immunodeficiency virus 2 amprenavir
3.4.23.47 0.000481
-
 mutant I54M Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000496
-
 mutant V62A/L99F Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000524
-
 mutant I54M/L90M Human immunodeficiency virus 2 lopinavir
3.4.23.47 0.000524
-
 mutant V62A/L99F Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.000528
-
 mutant I82L Human immunodeficiency virus 2 amprenavir
3.4.23.47 0.000544
-
 mutant I82F Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000624
-
 mutant I54M Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.000825
-
 mutant I54M/L99F Human immunodeficiency virus 2 indinavir
3.4.23.47 0.000961
-
 mutant V62A/L99F Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.000965
-
 mutant I82F Human immunodeficiency virus 2 amprenavir
3.4.23.47 0.001106
-
 mutant I54M Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.001112
-
 mutant I54M/L90M Human immunodeficiency virus 2 indinavir
3.4.23.47 0.001747
-
 mutant I54M/L84V Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.002028
-
 mutant I54M/L84V Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.002241
-
 mutant I54M/L99F Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.002564
-
 mutant I54M/L90M Human immunodeficiency virus 2 nelfinavir
3.4.23.47 0.002908
-
 mutant I54M/L99F Human immunodeficiency virus 2 tipranavir
3.4.23.47 0.004436
-
 mutant I82L Human immunodeficiency virus 2 tipranavir
3.4.23.47 1
-
 mutant I50V, value above 10 Human immunodeficiency virus 2 amprenavir
3.4.23.47 1
-
 mutant I54M/L84V: value above 10 Human immunodeficiency virus 2 amprenavir
3.4.23.47 1
-
 mutant I54M/L90M: value above 10 Human immunodeficiency virus 2 amprenavir
3.4.23.47 1
-
 mutant I54M/L99F: value above 10 Human immunodeficiency virus 2 amprenavir
3.4.23.47 1
-
 mutant I54M: value above 10 Human immunodeficiency virus 2 amprenavir