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Literature summary extracted from

  • Pattanawongsa, A.; Nair, P.C.; Rowland, A.; Miners, J.O.
    Human UDP-glucuronosyltransferase (UGT) 2B10: validation of cotinine as a selective probe substrate, inhibition by UGT enzyme-selective inhibitors and antidepressant and antipsychotic drugs, and structural determinants of enzyme inhibition (2016), Drug Metab. Dispos., 44, 378-388.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 gene UGT2B10, recombinant expressin in HEK-293T cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 (-)-nicotine
-
 Homo sapiens
2.4.1.17 amitriptyline
-
 Homo sapiens
2.4.1.17 aripiprazole
-
 Homo sapiens
2.4.1.17 chlorpromazine
-
 Homo sapiens
2.4.1.17 citalopram
-
 Homo sapiens
2.4.1.17 clomipramine
-
 Homo sapiens
2.4.1.17 clozapine
-
 Homo sapiens
2.4.1.17 desipramine
-
 Homo sapiens
2.4.1.17 desloratadine
-
 Homo sapiens
2.4.1.17 desmethylnortriptyline
-
 Homo sapiens
2.4.1.17 desvenlafaxine
-
 Homo sapiens
2.4.1.17 didesmethylimipramine
-
 Homo sapiens
2.4.1.17 doxepin
-
 Homo sapiens
2.4.1.17 duloxetine
-
 Homo sapiens
2.4.1.17 fluconazole
-
 Homo sapiens
2.4.1.17 fluoxetine
-
 Homo sapiens
2.4.1.17 fluphenazine
-
 Homo sapiens
2.4.1.17 fluvoxamine
-
 Homo sapiens
2.4.1.17 haloperidol
-
 Homo sapiens
2.4.1.17 hecogenin
-
 Homo sapiens
2.4.1.17 imipramine
-
 Homo sapiens
2.4.1.17 itraconazole
-
 Homo sapiens
2.4.1.17 ketoconazole
-
 Homo sapiens
2.4.1.17 loratadine
-
 Homo sapiens
2.4.1.17 loxapine
-
 Homo sapiens
2.4.1.17 mianserin
-
 Homo sapiens
2.4.1.17 mirtazapine
-
 Homo sapiens
2.4.1.17 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
2.4.1.17 niflumic acid
-
 Homo sapiens
2.4.1.17 norclomipramine
-
 Homo sapiens
2.4.1.17 nortriptyline
-
 Homo sapiens
2.4.1.17 olanzapine
-
 Homo sapiens
2.4.1.17 paroxetine
-
 Homo sapiens
2.4.1.17 perphenazine
-
 Homo sapiens
2.4.1.17 Phenelzine
-
 Homo sapiens
2.4.1.17 Phenylbutazone
-
 Homo sapiens
2.4.1.17 protriptyline
-
 Homo sapiens
2.4.1.17 quetiapine
-
 Homo sapiens
2.4.1.17 selegiline
-
 Homo sapiens
2.4.1.17 sertraline
-
 Homo sapiens
2.4.1.17 thioridazine
-
 Homo sapiens
2.4.1.17 tranylcypromine
-
 Homo sapiens
2.4.1.17 trimipramine
-
 Homo sapiens
2.4.1.17 venlafaxine
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 additional information
-
 additional information Michaelis-Menten kinetics Homo sapiens
2.4.1.17 0.0278
-
 cotinine pH 7.4, 37°C, recombinant isozyme UGT2B10 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+ required Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P36537 UGT2B10
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 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 ?
-
 ?
2.4.1.17 UDP-glucuronate + cotinine cotinine is a highly selective substrate of human liver microsomal UGT2B10 Homo sapiens UDP + cotinine N-beta-D-glucuronoside
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase 2B10
-
 Homo sapiens
2.4.1.17 UGT2B10
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.17 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.17 7.4
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 additional information
-
 additional information inhibition kinetics Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.00218
-
 pH 7.4, 37°C Homo sapiens loratadine
2.4.1.17 0.00224
-
 pH 7.4, 37°C Homo sapiens mianserin
2.4.1.17 0.00364
-
 pH 7.4, 37°C Homo sapiens doxepin
2.4.1.17 0.00386
-
 pH 7.4, 37°C Homo sapiens desloratadine
2.4.1.17 0.00645
-
 pH 7.4, 37°C Homo sapiens amitriptyline
2.4.1.17 0.0119
-
 pH 7.4, 37°C Homo sapiens ketoconazole
2.4.1.17 0.026
-
 pH 7.4, 37°C Homo sapiens clomipramine
2.4.1.17 0.031
-
 pH 7.4, 37°C Homo sapiens mirtazapine
2.4.1.17 0.0326
-
 pH 7.4, 37°C Homo sapiens trimipramine
2.4.1.17 0.0341
-
 pH 7.4, 37°C Homo sapiens desipramine
2.4.1.17 0.0343
-
 pH 7.4, 37°C Homo sapiens protriptyline
2.4.1.17 0.036
-
 pH 7.4, 37°C Homo sapiens loxapine
2.4.1.17 0.0362
-
 pH 7.4, 37°C Homo sapiens didesmethylimipramine
2.4.1.17 0.0428
-
 pH 7.4, 37°C Homo sapiens imipramine
2.4.1.17 0.0437
-
 pH 7.4, 37°C Homo sapiens desmethylnortriptyline
2.4.1.17 0.0439
-
 pH 7.4, 37°C Homo sapiens quetiapine
2.4.1.17 0.0453
-
 pH 7.4, 37°C Homo sapiens nortriptyline
2.4.1.17 0.0508
-
 pH 7.4, 37°C Homo sapiens norclomipramine
2.4.1.17 0.0535
-
 pH 7.4, 37°C Homo sapiens fluphenazine
2.4.1.17 0.0558
-
 pH 7.4, 37°C Homo sapiens aripiprazole
2.4.1.17 0.0613
-
 pH 7.4, 37°C Homo sapiens clozapine
2.4.1.17 0.0635
-
 pH 7.4, 37°C Homo sapiens paroxetine
2.4.1.17 0.0662
-
 pH 7.4, 37°C Homo sapiens perphenazine
2.4.1.17 0.0672
-
 pH 7.4, 37°C Homo sapiens selegiline
2.4.1.17 0.0713
-
 pH 7.4, 37°C Homo sapiens thioridazine
2.4.1.17 0.0724
-
 pH 7.4, 37°C Homo sapiens fluoxetine
2.4.1.17 0.079
-
 pH 7.4, 37°C Homo sapiens chlorpromazine
2.4.1.17 0.0812
-
 pH 7.4, 37°C Homo sapiens duloxetine
2.4.1.17 0.0927
-
 pH 7.4, 37°C Homo sapiens sertraline
2.4.1.17 0.0942
-
 pH 7.4, 37°C Homo sapiens Phenelzine
2.4.1.17 0.168
-
 pH 7.4, 37°C Homo sapiens niflumic acid
2.4.1.17 0.214
-
 pH 7.4, 37°C Homo sapiens (-)-nicotine
2.4.1.17 0.218
-
 pH 7.4, 37°C Homo sapiens citalopram
2.4.1.17 0.22
-
 pH 7.4, 37°C Homo sapiens Phenylbutazone
2.4.1.17 0.224
-
 pH 7.4, 37°C Homo sapiens fluvoxamine
2.4.1.17 0.276
-
 pH 7.4, 37°C Homo sapiens olanzapine
2.4.1.17 0.44
-
 pH 7.4, 37°C Homo sapiens desvenlafaxine
2.4.1.17 1.136
-
 pH 7.4, 37°C Homo sapiens fluconazole

General Information

EC Number General Information Comment Organism
2.4.1.17 physiological function important role of enzyme UGT2B10 in the N-glucuronidation of drugs and other xenobiotics Homo sapiens