Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DME0075)
DME Name UDP-glucuronosyltransferase 1A10 (UGT1A10), Homo sapiens
Synonyms UDP-glucuronosyltransferase family 1 member A10; UDP-glucuronosyltransferase 1-J; UDP-glucuronosyltransferase 1-10; UDPGT 1-10; UGT-1J; UGT1*10; UGT1-10; UGT1.10; UGT1A10; UGT1J
Gene Name UGT1A10
UniProt ID
UD110_HUMAN
Gene ID
54575
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
(loading-time for this interactome depdends on the speed of web connection)
       Interactions between Microbiome and DME (MICBIO)                       
Jump to Detailed Interactome Data                      
       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
MARAGWTSPVPLCVCLLLTCGFAEAGKLLVVPMDGSHWFTMQSVVEKLILRGHEVVVVMP
EVSWQLERSLNCTVKTYSTSYTLEDQNREFMVFAHAQWKAQAQSIFSLLMSSSSGFLDLF
FSHCRSLFNDRKLVEYLKESSFDAVFLDPFDTCGLIVAKYFSLPSVVFTRGIFCHHLEEG
AQCPAPLSYVPNDLLGFSDAMTFKERVWNHIVHLEDHLFCQYLFRNALEIASEILQTPVT
AYDLYSHTSIWLLRTDFVLDYPKPVMPNMIFIGGINCHQGKPLPMEFEAYINASGEHGIV
VFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLLGH
PMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSEDL
ENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDLTW
YQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
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:        19 Drugs
Tamoxifen citrate
 Drug Info Approved Breast cancer ICD11: 2C60 [1]
Fospropofol disodium
 Drug Info Approved Monitored anaesthesia care ICD11: N.A. [2]
Mycophenolate mofetil
 Drug Info Approved Crohn disease ICD11: DD70 [3]
Valproic acid
 Drug Info Approved Epilepsy ICD11: 8A60 [4]
Opicapone
 Drug Info Approved Parkinsonism ICD11: 8A00 [5]
Lasofoxifene
 Drug Info Approved Osteoporosis ICD11: FB83 [6]
Naproxen
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [7]
Etodolac
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [8]
Intedanib
 Drug Info Approved Idiopathic pulmonary fibrosis ICD11: CB03 [9]
Raloxifene
 Drug Info Approved Osteoporosis ICD11: FB83 [10]
Acetaminophen
 Drug Info Approved Anaesthesia ICD11: 8E22 [11]
Candesartan cilexetil
 Drug Info Approved Essential hypertension ICD11: BA00 [12]
Losartan potassium
 Drug Info Approved Essential hypertension ICD11: BA00 [8]
Mycophenolic acid
 Drug Info Approved Crohn disease ICD11: DD70 [13], [14]
Mycophenolic acid
 Drug Info Approved Crohn disease ICD11: DD70 [15]
Troglitazone
 Drug Info Approved Diabetes mellitus ICD11: 5A10 [16]
Edaravone
 Drug Info Approved Cerebral stroke ICD11: 8B11 [17]
Telmisartan
 Drug Info Approved Essential hypertension ICD11: BA00 [18]
LAROPIPRANT
 Drug Info Phase 4 Atherosclerosis ICD11: BA80 [19]
      Drugs in Phase 4 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
Bazedoxifene
 Drug Info Phase 4 Schizophrenia ICD11: 6A20 [20]
      Drugs in Phase 3 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
Heroin
 Drug Info Phase 3 Opiate dependence ICD11: 6C43 [21]
      Drugs in Phase 2 Clinical Trial Click to Show/Hide the Full List of Drugs:          5 Drugs
Puerarin
 Drug Info Phase 2 Alcohol dependence ICD11: 6C40 [22]
BCP-13498
 Drug Info Phase 2 Anaesthesia ICD11: 8E22 [23]
BIA 3-202
 Drug Info Phase 2 Parkinsonism ICD11: 8A00 [24]
(Z)-endoxifen
 Drug Info Phase 2 Breast cancer ICD11: 2C60-2C6Y [25]
Endoxifen
 Drug Info Phase 2 Breast cancer ICD11: 2C60-2C6Y [25]
      Drugs in Phase 1 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
OTSSP167
 Drug Info Phase 1 Myelodysplastic syndrome ICD11: 2A37 [26]
      Discontinued/withdrawn Drugs Click to Show/Hide the Full List of Drugs:          1 Drugs
Darexaban maleate
 Drug Info Discontinued in Phase 3 Acute coronary syndrome ICD11: BA41-BA43 [27]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          4 Drugs
Hydroxyestrone
 Drug Info Investigative Discovery agent ICD: N.A. [28]
Cis-4-hydroxytamoxifen
 Drug Info Investigative Discovery agent ICD: N.A. [1]
Hydroxybenzo(a)pyrene
 Drug Info Investigative Discovery agent ICD: N.A. [29]
Hydroxybenzo[a]pyrene
 Drug Info Investigative Discovery agent ICD: N.A. [29]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR000048 Acetaminophen Acetaminophen glucuronide Conjugation - Glucuronidation Acetaminophen [11], [30], [31]
MR000349 Bazedoxifene Bazedoxifene-5-glucuronide Conjugation - Glucuronidation Bazedoxifene [32]
MR000350 Bazedoxifene Bazedoxifene-4'-glucuronide Conjugation - Glucuronidation Bazedoxifene [32]
MR005294 Cis-4-hydroxytamoxifen Cis-4-hydroxytamoxifen-O-glucuronide Conjugation - Glucuronidation Cis-4-hydroxytamoxifen [1]
MR013043 Darexaban maleate Darexaban glucuronide Unclear - Unclear Darexaban maleate [33], [27]
MR006689 11-Hydroxy-delta-9-THC 11-Hydroxy-delta-9-THC-glucuronide Conjugation - Glucuronidation Dronabinol [8]
MR000896 Edaravone Edaravone glucuronide conjugates Conjugation - Glucuronidation Edaravone [17]
MR011558 Endoxifen Endoxifen O-Glucuronide Unclear - Unclear Endoxifen [25]
MR002737 Etodolac Etodolac acyl glucuronide Conjugation - Glucuronidation Etodolac [34]
MR007850 Propofol Propofol-O-glucuronide Conjugation - O-glucuronidation Fospropofol disodium [2]
MR013333 Morphine Morphine-3-glucuronide Conjugation - Glucuronidation Heroin [21]
MR007041 Hydroxybenzo(a)pyrene Hydroxybenzo(a)pyrene Glucuronidated metabolites Conjugation - Glucuronidation Hydroxybenzo(a)pyrene [29]
MR007042 Hydroxybenzo[a]pyrene Hydroxybenzo[a]pyrene Glucuronidated metabolites Conjugation - Glucuronidation Hydroxybenzo[a]pyrene [29]
MR007047 Hydroxyestrone 2-hydroxyestrone 2-glucuronide Conjugation - O-glucuronidation Hydroxyestrone [28]
MR006915 Losartan potassium Losartan N2-glucuronide Conjugation - N-glucuronidation Losartan potassium [35]
MR004815 Mycophenolate mofetil Mycophenolic acid glucuronide Conjugation - Glucuronidation Mycophenolate mofetil [36]
MR004816 Mycophenolate mofetil Mycophenolic acyl-glucuronide (AcMPAG) Conjugation - Glucuronidation Mycophenolate mofetil [36]
MR004824 Mycophenolic acid Mycophenolic acid glucuronide Conjugation - O-glucuronidation Mycophenolic acid [13], [14]
MR004873 O-Desmethylnaproxen O-Desmethylnaproxen acyl glucuronide Conjugation - Glucuronidation Naproxen [8]
MR004872 O-Desmethylnaproxen O-Desmethylnaproxen O-glucuronide Conjugation - Glucuronidation Naproxen [8]
MR008449 OTSSP167 OTS167-G Unclear - Unclear OTSSP167 [26]
MR002012 Acetaminophen Acetaminophen glucuronide Conjugation - Glucuronidation Phenacetin [37]
MR008594 Puerarin Puerarin-7-O-glucuronide Conjugation - Glucuronidation Puerarin [22]
MR010029 Raloxifene Raloxifen-4-glucoronide(M2) Conjugation - Glucuronidation Raloxifene [38], [39], [40]
MR010030 Raloxifene Raloxifene-6-bate-glucuronide(M1) Conjugation - Glucuronidation Raloxifene [38], [39]
MR010031 Raloxifene Raloxifene-6, 4-diglucuronide(M3) Conjugation - Glucuronidation Raloxifene [38], [39]
MR003527 4-hydroxytamoxifen Tamoxifen glucuronides Conjugation - Glucuronidation Tamoxifen citrate [41]
MR003520 Endoxifen Tamoxifen glucuronides Conjugation - Glucuronidation Tamoxifen citrate [41]
MR003520 Endoxifen Tamoxifen glucuronides Conjugation - Glucuronidation Tamoxifen citrate [41]
MR003520 Endoxifen Tamoxifen glucuronides Conjugation - Glucuronidation Tamoxifen citrate [41]
MR002465 Troglitazone Troglitazone glucuronide metabolite Conjugation - Glucuronidation Troglitazone [42], [16]
MR002497 Valproic acid Valproic acid beta-O-glucuronide metabolite Oxidation - Dehydrogenation Valproic acid [8]
MR005667 Vorinostat Vorinostat-O-Glucuronide metabolite Unclear - Unclear Vorinostat [43], [44]
⏷ Show the Full List of 33 MR(s)
References
1 Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2006-14.
2 Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects
3 [Pharmacology of mycophenolate mofetil: recent data and clinical consequences]. Nephrologie. 2001;22(7):331-7.
4 UDP glucuronosyltransferase (UGT) 1A6 pharmacogenetics: II. Functional impact of the three most common nonsynonymous UGT1A6 polymorphisms (S7A, T181A, and R184S). J Pharmacol Exp Ther. 2005 Jun;313(3):1340-6.
5 Metabolism and disposition of opicapone in the rat and metabolic enzymes phenotyping
6 DrugBank(Pharmacology-Metabolism):Lasofoxifene
7 S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
8 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
9 Characterization of Enzymes Involved in Nintedanib Metabolism in Humans
10 Characterization of raloxifene glucuronidation: potential role of UGT1A8 genotype on raloxifene metabolism in vivo. Cancer Prev Res (Phila). 2013 Jul;6(7):719-30.
11 Simultaneous quantification of abemaciclib and its active metabolites in human and mouse plasma by UHPLC-MS/MS J Pharm Biomed Anal. 2021 Sep 5;203:114225. doi: 10.1016/j.jpba.2021.114225.
12 The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan Biochem Pharmacol. 2008 Sep 15;76(6):763-72. doi: 10.1016/j.bcp.2008.07.006.
13 Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96.
14 The main role of UGT1A9 in the hepatic metabolism of mycophenolic acid and the effects of naturally occurring variants
15 Identification of the UDP-glucuronosyltransferase isoforms involved in mycophenolic acid phase II metabolism. Drug Metab Dispos. 2005 Jan;33(1):139-46.
16 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
17 LABEL:ADICAVA- edaravone injection RADICAVA ORS- edaravone kit
18 In vitro glucuronidation of the angiotensin II receptor antagonist telmisartan in the cat: a comparison with other species
19 Metabolism of MK-0524, a prostaglandin D2 receptor 1 antagonist, in microsomes and hepatocytes from preclinical species and humans
20 In vitro metabolism, permeability, and efflux of bazedoxifene in humans. Drug Metab Dispos. 2010 Sep;38(9):1471-9.
21 PharmGKB:Heroin
22 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for puerarin metabolism in human liver microsomes
23 UDP-glucuronosyltransferases and clinical drug-drug interactions. Pharmacol Ther. 2005 Apr;106(1):97-132.
24 Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation
25 Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen
26 Glucuronidation of OTS167 in Humans Is Catalyzed by UDP-Glucuronosyltransferases UGT1A1, UGT1A3, UGT1A8, and UGT1A10
27 Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine
28 Structural and functional studies of UDP-glucuronosyltransferases. Drug Metab Rev. 1999 Nov;31(4):817-99.
29 Importance of UDP-glucuronosyltransferase 1A10 (UGT1A10) in the detoxification of polycyclic aromatic hydrocarbons: decreased glucuronidative activity of the UGT1A10139Lys isoform. Drug Metab Dispos. 2006 Jun;34(6):943-9.
30 Application of a Volumetric Absorptive Microsampling (VAMS)-Based Method for the Determination of Paracetamol and Four of its Metabolites as a Tool for Pharmacokinetic Studies in Obese and Non-Obese Patients. Clin Pharmacokinet. 2022 Dec;61(12):1719-1733. doi: 10.1007/s40262-022-01187-2.
31 Evaluation of urinary acetaminophen metabolites and its association with the genetic polymorphisms of the metabolising enzymes, and serum acetaminophen concentrations in preterm neonates with patent ductus arteriosus. Xenobiotica. 2021 Nov;51(11):1335-1342. doi: 10.1080/00498254.2021.1982070.
32 UGT1A1*28 polymorphism influences glucuronidation of bazedoxifene. Pharmazie. 2015 Feb;70(2):94-6.
33 Absorption, metabolism and excretion of darexaban (YM150), a new direct factor Xa inhibitor in humans
34 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development Curr Med Chem. 2009;16(27):3480-675. doi: 10.2174/092986709789057635.
35 Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814.
36 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
37 DrugBank(Pharmacology-Metabolism)Phenacetin
38 Raloxifene glucuronidation in liver and intestinal microsomes of humans and monkeys: contribution of UGT1A1, UGT1A8 and UGT1A9
39 Determination of raloxifene and its glucuronides in human urine by liquid chromatography-tandem mass spectrometry assay
40 Pharmacokinetics of raloxifene and its clinical application
41 PharmGKB:Tamoxifen citrate
42 Clinical pharmacokinetics of troglitazone Clin Pharmacokinet. 1999 Aug;37(2):91-104. doi: 10.2165/00003088-199937020-00001.
43 Stability studies of vorinostat and its two metabolites in human plasma, serum and urine
44 Uridine 5'-diphospho-glucuronosyltransferase genetic polymorphisms and response to cancer chemotherapy. Future Oncol. 2010 Apr;6(4):563-85.

If you find any error in data or bug in web service, please kindly report it to Dr. Yin and Dr. Li.