Application | Comment | Organism |
---|---|---|
medicine | isolation of mutants from H5N1-infected patients to explain the molecular basis of resistance to oseltamivir. Mutants are resistant to oseltamivir but still strongly inhibited by zanamivir owing to an altered hydrophobic pocket in the active site of the enzyme required for oseltamivir binding | unidentified influenza virus |
Crystallization (Comment) | Organism |
---|---|
wild-type and mutants H274Y, N294S, Y252H in complex with oseltamivir. Mutants are resistant to oseltamivir but still strongly inhibited by zanamivir owing to an altered hydrophobic pocket in the active site of the enzyme required for oseltamivir binding | unidentified influenza virus |
Protein Variants | Comment | Organism |
---|---|---|
H274Y | mutant isolated from patient infected with H5N1. Ratio Ki mutant/Ki wild-type for inhibition by oseltamivir is 265, for inhibition by zanamivir is 1.9, respectively | unidentified influenza virus |
N294S | mutant isolated from patient infected with H5N1. Ratio Ki mutant/Ki wild-type for inhibition by oseltamivir is 81, for inhibition by zanamivir is 7.2, respectively | unidentified influenza virus |
Y252H | mutant isolated from patient infected with H5N1. Ratio Ki mutant/Ki wild-type for inhibition by oseltamivir is 0.1, for inhibition by zanamivir is 1.2, respectively | unidentified influenza virus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
oseltamivir | - |
unidentified influenza virus | |
zanamivir | - |
unidentified influenza virus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0063 | - |
2-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid | wild-type | unidentified influenza virus | |
0.0075 | - |
2-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid | mutant Y252H | unidentified influenza virus | |
0.027 | - |
2-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid | mutant H274Y | unidentified influenza virus | |
0.053 | - |
2-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid | mutant N294S | unidentified influenza virus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
unidentified influenza virus | - |
type H5N1 | - |
unidentified influenza virus H5N1 | - |
type H5N1 | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
2-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid + H2O | - |
unidentified influenza virus | 4-methylumbelliferone + N-acetylneuraminic acid | - |
? | |
2-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid + H2O | - |
unidentified influenza virus H5N1 | 4-methylumbelliferone + N-acetylneuraminic acid | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000001 | - |
zanamivir | wild-type | unidentified influenza virus | |
0.00000032 | - |
oseltamivir | wild-type | unidentified influenza virus |