Cloned (Comment) | Organism |
---|---|
gene UGT2B10, recombinant expressin in HEK-293T cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(-)-nicotine | - |
Homo sapiens | |
amitriptyline | - |
Homo sapiens | |
aripiprazole | - |
Homo sapiens | |
chlorpromazine | - |
Homo sapiens | |
citalopram | - |
Homo sapiens | |
clomipramine | - |
Homo sapiens | |
clozapine | - |
Homo sapiens | |
desipramine | - |
Homo sapiens | |
desloratadine | - |
Homo sapiens | |
desmethylnortriptyline | - |
Homo sapiens | |
desvenlafaxine | - |
Homo sapiens | |
didesmethylimipramine | - |
Homo sapiens | |
doxepin | - |
Homo sapiens | |
duloxetine | - |
Homo sapiens | |
fluconazole | - |
Homo sapiens | |
fluoxetine | - |
Homo sapiens | |
fluphenazine | - |
Homo sapiens | |
fluvoxamine | - |
Homo sapiens | |
haloperidol | - |
Homo sapiens | |
hecogenin | - |
Homo sapiens | |
imipramine | - |
Homo sapiens | |
itraconazole | - |
Homo sapiens | |
ketoconazole | - |
Homo sapiens | |
loratadine | - |
Homo sapiens | |
loxapine | - |
Homo sapiens | |
mianserin | - |
Homo sapiens | |
mirtazapine | - |
Homo sapiens | |
additional information | the majority of antidepressant and antipsychotic drugs screened for effects on UGT2B10 inhibit the enzyme activity with IC50 values below 0.1 mM. The most potent inhibition is observed with the tricyclic antidepressants amitriptyline and doxepin and the tetracyclic antidepressant mianserin, and the structurally related compounds desloratadine and loratadine. Molecular modeling using a ligand-based approach indicates that hydrophobic and charge interactions are involved in inhibitor binding, whereas spatial features influence the potency of UGT2B10 inhibition. UGT enzyme-selective inhibitor screening, overview | Homo sapiens | |
niflumic acid | - |
Homo sapiens | |
norclomipramine | - |
Homo sapiens | |
nortriptyline | - |
Homo sapiens | |
olanzapine | - |
Homo sapiens | |
paroxetine | - |
Homo sapiens | |
perphenazine | - |
Homo sapiens | |
Phenelzine | - |
Homo sapiens | |
Phenylbutazone | - |
Homo sapiens | |
protriptyline | - |
Homo sapiens | |
quetiapine | - |
Homo sapiens | |
selegiline | - |
Homo sapiens | |
sertraline | - |
Homo sapiens | |
thioridazine | - |
Homo sapiens | |
tranylcypromine | - |
Homo sapiens | |
trimipramine | - |
Homo sapiens | |
venlafaxine | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
0.0278 | - |
cotinine | pH 7.4, 37°C, recombinant isozyme UGT2B10 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P36537 | UGT2B10 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | most, if not all, UGT2B10 substrates are additionally glucuronidated by UGT1A4 and biphasic kinetics are frequently observed when human liver microsomes are used as the enzyme source. UGT2B10 is the high-affinity enzyme involved in most reactions. Thirteen recombinant human UGTs are screened for cotinine N-glucuronide formation, i.e. UGT 1A1, 1A3, 1A4, 1A6, 1A7, 1A8, 1A9, 1A10, 2B4, 2B7, 2B10, 2B15, and 2B17, cotinine is a highly selective substrate of human liver microsomal UGT2B10 | Homo sapiens | ? | - |
? | |
UDP-glucuronate + cotinine | cotinine is a highly selective substrate of human liver microsomal UGT2B10 | Homo sapiens | UDP + cotinine N-beta-D-glucuronoside | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UDP-glucuronosyltransferase 2B10 | - |
Homo sapiens |
UGT2B10 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00218 | - |
pH 7.4, 37°C | Homo sapiens | loratadine | |
0.00224 | - |
pH 7.4, 37°C | Homo sapiens | mianserin | |
0.00364 | - |
pH 7.4, 37°C | Homo sapiens | doxepin | |
0.00386 | - |
pH 7.4, 37°C | Homo sapiens | desloratadine | |
0.00645 | - |
pH 7.4, 37°C | Homo sapiens | amitriptyline | |
0.0119 | - |
pH 7.4, 37°C | Homo sapiens | ketoconazole | |
0.026 | - |
pH 7.4, 37°C | Homo sapiens | clomipramine | |
0.031 | - |
pH 7.4, 37°C | Homo sapiens | mirtazapine | |
0.0326 | - |
pH 7.4, 37°C | Homo sapiens | trimipramine | |
0.0341 | - |
pH 7.4, 37°C | Homo sapiens | desipramine | |
0.0343 | - |
pH 7.4, 37°C | Homo sapiens | protriptyline | |
0.036 | - |
pH 7.4, 37°C | Homo sapiens | loxapine | |
0.0362 | - |
pH 7.4, 37°C | Homo sapiens | didesmethylimipramine | |
0.0428 | - |
pH 7.4, 37°C | Homo sapiens | imipramine | |
0.0437 | - |
pH 7.4, 37°C | Homo sapiens | desmethylnortriptyline | |
0.0439 | - |
pH 7.4, 37°C | Homo sapiens | quetiapine | |
0.0453 | - |
pH 7.4, 37°C | Homo sapiens | nortriptyline | |
0.0508 | - |
pH 7.4, 37°C | Homo sapiens | norclomipramine | |
0.0535 | - |
pH 7.4, 37°C | Homo sapiens | fluphenazine | |
0.0558 | - |
pH 7.4, 37°C | Homo sapiens | aripiprazole | |
0.0613 | - |
pH 7.4, 37°C | Homo sapiens | clozapine | |
0.0635 | - |
pH 7.4, 37°C | Homo sapiens | paroxetine | |
0.0662 | - |
pH 7.4, 37°C | Homo sapiens | perphenazine | |
0.0672 | - |
pH 7.4, 37°C | Homo sapiens | selegiline | |
0.0713 | - |
pH 7.4, 37°C | Homo sapiens | thioridazine | |
0.0724 | - |
pH 7.4, 37°C | Homo sapiens | fluoxetine | |
0.079 | - |
pH 7.4, 37°C | Homo sapiens | chlorpromazine | |
0.0812 | - |
pH 7.4, 37°C | Homo sapiens | duloxetine | |
0.0927 | - |
pH 7.4, 37°C | Homo sapiens | sertraline | |
0.0942 | - |
pH 7.4, 37°C | Homo sapiens | Phenelzine | |
0.168 | - |
pH 7.4, 37°C | Homo sapiens | niflumic acid | |
0.214 | - |
pH 7.4, 37°C | Homo sapiens | (-)-nicotine | |
0.218 | - |
pH 7.4, 37°C | Homo sapiens | citalopram | |
0.22 | - |
pH 7.4, 37°C | Homo sapiens | Phenylbutazone | |
0.224 | - |
pH 7.4, 37°C | Homo sapiens | fluvoxamine | |
0.276 | - |
pH 7.4, 37°C | Homo sapiens | olanzapine | |
0.44 | - |
pH 7.4, 37°C | Homo sapiens | desvenlafaxine | |
1.136 | - |
pH 7.4, 37°C | Homo sapiens | fluconazole |
General Information | Comment | Organism |
---|---|---|
physiological function | important role of enzyme UGT2B10 in the N-glucuronidation of drugs and other xenobiotics | Homo sapiens |