Cytochrome P450 2C9 from Homo sapiens

Enzyme Description

Species
Homo sapiens (human) β†—
Extremophile
No
EC Number
1.14.14.1 β†—

Sequence

Length: 490 amino acids
MDSLVVLVLCLSCLLLLSLWRQSSGRGKLPPGPTPLPVIGNILQIGIKDISKSLTNLSKVYGPVFTLYFGLKPIVVLHGYEAVKEALIDLGEEFSGRGIFPLAERANRGFGIVFSNGKKWKEIRRFSLMTLRNFGMGKRSIEDRVQEEARCLVEELRKTKASPCDPTFILGCAPCNVICSIIFHKRFDYKDQQFLNLMEKLNENIKILSSPWIQICNNFSPIIDYFPGTHNKLLKNVAFMKSYILEKVKEHQESMDMNNPQDFIDCFLMKMEKEKHNQPSEFTIESLENTAVDLFGAGTETTSTTLRYALLLLLKHPEVTAKVQEEIERVIGRNRSPCMQDRSHMPYTDAVVHEVQRYIDLLPTSLPHAVTCDIKFRNYLIPKGTTILISLTSVLHDNKEFPNPEMFDPHHFLDEGGNFKKSKYFMPFSAGKRICVGEALAGMELFLFLTSILQNFNLKSLVDPKNLDTTPVVNGFASVPPFYQLCFIPV
Vanessa GonzΓ‘lez-PΓ©rez et al. (2012) β€” Impact of Organic Solvents on Cytochrome P450 Probe Reactions: Filling the Gap with (S)-Warfarin and Midazolam Hydroxylation
Drug Metabolism and Disposition  Β· doi:10.1124/dmd.112.047134 β†—  Β· Activity - Classical
54 measurements ▼
Database ID
UniProt: P11712 β†—
Sequence Annotation
Inferred - from protein name
Protein Source
Recombinant, host insect cells

Experimental Data (54 measurements)

54 measurements β€” page 1 of 3
Mutation Property Assay Solvent Solvent Volume Aqueous ReferenceWT Reference Measured Value Units Extraction method Data type Solution pH Temperature Substrate(s) Product(s) Cofactor(s) Shaking Comments
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Acetonitrile 0.1 % v/v 100 β€” 76 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Dimethyl Sulfoxide (DMSO) 2 % v/v 100 β€” 23 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Dimethyl Sulfoxide (DMSO) 1 % v/v 100 β€” 41 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Dimethyl Sulfoxide (DMSO) 0.1 % v/v 100 β€” 62 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Acetone 0.1 % v/v 100 β€” 69 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Ethanol 2 % v/v 100 β€” 5 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Acetone 1 % v/v 100 β€” 42 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Ethanol 1 % v/v 100 β€” 20 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Ethanol 0.1 % v/v 100 β€” 59 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Acetone 2 % v/v 100 β€” 22 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Methanol 2 % v/v 100 β€” 18 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Isopropanol 0.1 % v/v 100 β€” 47 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Methanol 1 % v/v 100 β€” 49 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Methanol 0.1 % v/v 100 β€” 79 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Isopropanol 1 % v/v 100 β€” 14 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Acetonitrile 1 % v/v 100 β€” 66 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Isopropanol 2 % v/v 100 β€” 2 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
WT Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Acetonitrile 2 % v/v 100 β€” 62 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
I359L Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Isopropanol 2 % v/v 100 2 4 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
R144C Activity - Classical Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent Isopropanol 2 % v/v 100 2 2 % Digital Continuous 100 mM potassium phosphate buffer 7.4 37Β°C 4 Β΅M (S)-Warfarin (S)-7-Hydroxywarfarin 1 mM NADPH β€” Classical aqueous control (in %)
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Mutations in this dataset (3)

WT R144C I359L

Visualization : Activity β€” Classical

One bar per measurement. Colour = solvent, shade = solvent volume. β€” β€” β€” Reference value. Hover for details.

Mutation Effect

Mutation impact on enzyme stability and function in the presence of organic solvent: comparison of wild-type and mutant values in identical conditions.

Structure

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