Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DME0205)
DME Name UDP-glucuronosyltransferase 2B10 (UGT2B10), Homo sapiens
Synonyms UDP-glucuronosyltransferase family 2 member B10; UDPGT 2B10; UGT2B10; OMIM: 600070; MGI: 2140962; HomoloGene: 117389; GeneCards: UGT2B10
Gene Name UGT2B10
UniProt ID
UDB10_HUMAN
Gene ID
7365
EC Number    EC: 2.4.1.17     (Click to Show/Hide the Complete EC Tree)
Transferase
Glycosyltransferases
Hexosyltransferase
EC: 2.4.1.17
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Interactome
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       Interactions between Xenobiotics and DME (XEOTIC)                      
Jump to Detailed Interactome Data                      
       Interactions between Host Protein and DME (HOSPPI)                     
Jump to Detailed Interactome Data                      
      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Sequence
MALKWTTVLLIQLSFYFSSGSCGKVLVWAAEYSLWMNMKTILKELVQRGHEVTVLASSAS
ILFDPNDSSTLKLEVYPTSLTKTEFENIIMQLVKRLSEIQKDTFWLPFSQEQEILWAIND
IIRNFCKDVVSNKKLMKKLQESRFDIVFADAYLPCGELLAELFNIPFVYSHSFSPGYSFE
RHSGGFIFPPSYVPVVMSKLSDQMTFMERVKNMLYVLYFDFWFQIFNMKKWDQFYSEVLG
RPTTLSETMRKADIWLMRNSWNFKFPHPFLPNVDFVGGLHCKPAKPLPKEMEEFVQSSGE
NGVVVFSLGSMVSNMTEERANVIATALAKIPQKVLWRFDGNKPDALGLNTRLYKWIPQND
LLGHPKTRAFITHGGANGIYEAIYHGIPMVGIPLFFDQPDNIAHMKAKGAAVRVDFNTMS
STDLLNALKTVINDPSYKENIMKLSRIQHDQPVKPLDRAVFWIEFVMRHKGAKHLRVAAH
NLTWFQYHSLDVIGFLLACVATVLFIITKCCLFCFWKFARKGKKGKRD
Pathway Ascorbate and aldarate metabolism (hsa00053 )
Chemical carcinogenesis (hsa05204 )
Drug metabolism - cytochrome P450 (hsa00982 )
Drug metabolism - other enzymes (hsa00983 )
Metabolic pathways (hsa01100 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Pentose and glucuronate interconversions (hsa00040 )
Porphyrin and chlorophyll metabolism (hsa00860 )
Retinol metabolism (hsa00830 )
Steroid hormone biosynthesis (hsa00140 )
Function This enzyme is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:        10 Drugs
Cyproheptadine
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [1]
Dexmedetomidine hydrochloride
 Drug Info Approved Tension headache ICD11: 8A81 [2]
Azatadine
 Drug Info Approved Allergic rhinitis ICD11: CA08 [3]
Cyclizine
 Drug Info Approved Nausea ICD11: MD90 [4]
Desloratadine
 Drug Info Approved Allergic rhinitis ICD11: CA08 [5]
Ketotifen
 Drug Info Approved Conjunctivitis ICD11: 9A60 [6]
Ketotifen
 Drug Info Approved Conjunctivitis ICD11: 9A60 [7]
Loratadine
 Drug Info Approved Allergic rhinitis ICD11: CA08 [8]
Trimipramine
 Drug Info Approved Depression ICD11: 6A71 [9]
Osilodrostat
 Drug Info Approved Cushing syndrome ICD11: 5A70 [10]
      Drugs in Phase 4 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
Pizotifen
 Drug Info Phase 4 Migraine ICD11: 8A80 [7]
      Drugs in Phase 2 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
ABT-126
 Drug Info Phase 2 Alzheimer disease ICD11: 8A20 [11]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          1 Drugs
Cotinine
 Drug Info Investigative Nicotine dependence ICD11: 6C4A [12]
      Experimental Enzyme Kinetic Data of Drugs Click to Show/Hide the Full List of Drugs:          1 Drugs
Cotinine
 Drug Info Investigative Nicotine dependence Km = 0.0278 microM [12]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR008317 ABT-126 ABT-126 metabolite M11 Conjugation - Glucuronidation ABT-126 [11]
MR010077 Atipamezole Atipamezole Metabolite M1 Conjugation - N-glucuronidation Atipamezole [13]
MR004135 Cyproheptadine Cyproheptadine N-glucuronide Conjugation - N-glucuronidation Cyproheptadine [1]
MR000769 Desloratadine Desloratadine N-glucuronidation Conjugation - Glucuronidation Desloratadine [5], [8]
MR000804 Dexmedetomidine hydrochloride Dexmedetomidine N-glucuronidation Conjugation - Glucuronidation Dexmedetomidine hydrochloride [2]
MR001376 Ketotifen Ketotifen-N-glucuronide Conjugation - N-Glucuronidation Ketotifen [6], [7]
MR006904 Desloratadine Desloratadine glucuronide Conjugation - Glucuronidation Loratadine [8]
MR005179 Pizotifen Pizotifen glucuronide metabolite Conjugation - N-glucuronidation Pizotifen [7]
⏷ Show the Full List of 8 MR(s)
References
1 Human metabolism of cyproheptadine
2 Large inter-individual variability in pharmacokinetics of dexmedetomidine and its two major N-glucuronides in adult intensive care unit patients J Pharm Biomed Anal. 2019 Oct 25;175:112777. doi: 10.1016/j.jpba.2019.07.025.
3 Use of Phenotypically Poor Metabolizer Individual Donor Human Liver Microsomes To Identify Selective Substrates of UGT2B10
4 N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification
5 Further characterization of the metabolism of desloratadine and its cytochrome P450 and UDP-glucuronosyltransferase inhibition potential: identification of desloratadine as a relatively selective UGT2B10 inhibitor. Drug Metab Dispos. 2015 Sep;43(9):1294-302.
6 N+-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group Drug Metab Dispos. 1998 Sep;26(9):830-7.
7 Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97.
8 A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement Drug Metab Dispos. 2015 Apr;43(4):523-33. doi: 10.1124/dmd.114.062620.
9 Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Drug Metab Dispos. 2010 May;38(5):863-70.
10 DrugBank(Pharmacology-Metabolism):Osilodrostat
11 Metabolism and Disposition of a Novel Selective 7 Neuronal Acetylcholine Receptor Agonist ABT-126 in Humans: Characterization of the Major Roles for Flavin-Containing Monooxygenases and UDP-Glucuronosyl Transferase 1A4 and 2B10 in Catalysis
12 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. Drug Metab Dispos. 2016 Mar;44(3):378-88.
13 Assessment and Confirmation of Species Difference in Nonlinear Pharmacokinetics of Atipamezole with Physiologically Based Pharmacokinetic Modeling

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