EC Number   |
Protein Variants |
Reference |
|---|
   3.4.23.47 | D25N |
inactive mutant forms a dimer |
710496 |
| 3.4.23.47 | DELTA96-99 |
dimer interface mutations such as a deletion of the C-terminal residues 96-99 (PR21-95), drastically increase the Kd. Deletion mutant consists predominantly of folded monomers. Addition of 2fold excess active-site inhibitor does not promote dimerization |
710496 |
| 3.4.23.47 | E37K |
mutation significantly retards autoproteolytic cleavage during expression. Mutant shows a higher dimer dissociation constant, Kd, compared to wild-type. Km and kcat values for substrate Lys-Ala-Arg-Val-Nle-(4-nitrophenylalanine)-Glu-Ala-Nle comparable to wild-type |
710496 |
| 3.4.23.47 | I32V |
site-directed mutagenesis, mutation analogous to wild-type HIV-1 protease sequence (EC 3.4.23.16). The mutation increases the susceptibility of HIV-2 to multiple protease inhibitors |
754549 |
| 3.4.23.47 | I50V |
IC50 (mM): value above 10 (amprenavir), 0.000072 (idinavir), 0.000132 (nelfinavir), 0.000316 (tipranavir), 0.000203 (lopinavir) |
677596 |
| 3.4.23.47 | I54M |
IC50 (mM): value above 10 (amprenavir), 0.000236 (idinavir), 0.000624 (nelfinavir), 0.001106 (tipranavir), 0.000481 (lopinavir) |
677596 |
| 3.4.23.47 | I54M |
mutant is resistant toward HIV-2 protease inhibitor lopinavir and saquinavir in yeast |
682827 |
| 3.4.23.47 | I54M/I84V |
IC50 (mM): value above 10 (amprenavir), 0.000388 (idinavir), 0.001747 (nelfinavir), 0.002028 (tipranavir), 0.000375 (lopinavir) |
677596 |
| 3.4.23.47 | I54M/L90M |
IC50 (mM): value above 10 (amprenavir), 0.001112 (idinavir), 0.002564 (nelfinavir), 0.000145 (tipranavir), 0.000524 (lopinavir) |
677596 |
| 3.4.23.47 | I54M/L99F |
IC50 (mM): value above 10 (amprenavir), 0.000825 (idinavir), 0.002241 (nelfinavir), 0.002908 (tipranavir), 0.000414 (lopinavir) |
677596 |
