Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DME0065)
DME Name UDP-glucuronosyltransferase 1A7 (UGT1A7), Homo sapiens
Synonyms UDP-glucuronosyltransferase family 1 member A7; UDP-glucuronosyltransferase 1-G; UDP-glucuronosyltransferase 1-7; UDPGT 1-7; UGT-1G; UGT1*7; UGT1-07; UGT1.7; UGT1A7; UGT1G
Gene Name UGT1A7
UniProt ID
UD17_HUMAN
Gene ID
54577
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 Microbiome and DME (MICBIO)                       
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       Interactions between Xenobiotics and DME (XEOTIC)                      
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       Interactions between Host Protein and DME (HOSPPI)                     
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      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Sequence
MARAGWTGLLPLYVCLLLTCGFAKAGKLLVVPMDGSHWFTMQSVVEKLILRGHEVVVVMP
EVSWQLGRSLNCTVKTYSTSYTLEDQDREFMVFADARWTAPLRSAFSLLTSSSNGIFDLF
FSNCRSLFNDRKLVEYLKESCFDAVFLDPFDACGLIVAKYFSLPSVVFARGIFCHYLEEG
AQCPAPLSYVPRLLLGFSDAMTFKERVWNHIMHLEEHLFCPYFFKNVLEIASEILQTPVT
AYDLYSHTSIWLLRTDFVLEYPKPVMPNMIFIGGINCHQGKPVPMEFEAYINASGEHGIV
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:        15 Drugs
Fospropofol disodium
 Drug Info Approved Monitored anaesthesia care ICD11: N.A. [1]
Cannabidiol
 Drug Info Approved Lennox-Gastaut syndrome ICD11: 8A62 [2]
Mycophenolate mofetil
 Drug Info Approved Crohn disease ICD11: DD70 [3]
Opicapone
 Drug Info Approved Parkinsonism ICD11: 8A00 [4]
Naproxen
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [5]
Intedanib
 Drug Info Approved Idiopathic pulmonary fibrosis ICD11: CB03 [6]
Candesartan cilexetil
 Drug Info Approved Essential hypertension ICD11: BA00 [7]
Mycophenolic acid
 Drug Info Approved Crohn disease ICD11: DD70 [8], [9]
Mycophenolic acid
 Drug Info Approved Crohn disease ICD11: DD70 [10]
Edaravone
 Drug Info Approved Cerebral stroke ICD11: 8B11 [11]
Hesperidin
 Drug Info Approved Vascular purpura ICD11: 3B60 [12]
Vorinostat
 Drug Info Approved Cutaneous T-cell lymphoma ICD11: 2B01 [13]
Gaboxadol
 Drug Info Approved Insomnia ICD11: 7A00-7A0Z [14]
Telmisartan
 Drug Info Approved Essential hypertension ICD11: BA00 [15]
Telmisartan
 Drug Info Approved Essential hypertension ICD11: BA00 [16]
      Drugs in Phase 4 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
Silymarin
 Drug Info Phase 4 Fatty liver disease ICD11: DB92 [17], [18]
      Drugs in Phase 3 Clinical Trial Click to Show/Hide the Full List of Drugs:          2 Drugs
AKB-6548
 Drug Info Phase 3 Anaemia ICD11: 3A90 [19]
Curcumin
 Drug Info Phase 3 Stomach cancer ICD11: 2B72 [20]
      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 [21]
BAICALEIN
 Drug Info Phase 2 Influenza virus infection ICD11: 1E30-1E32 [22]
LJN452
 Drug Info Phase 2 Primary biliary cholangitis ICD11: DB96 [23]
BIA 3-202
 Drug Info Phase 2 Parkinsonism ICD11: 8A00 [24]
AR-67
 Drug Info Phase 2 Brain cancer ICD11: 2A00 [25]
      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 [26]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          5 Drugs
Eugenol
 Drug Info Investigative Discovery agent ICD: N.A. [20]
Phloretin
 Drug Info Investigative Discovery agent ICD: N.A. [20]
Chrysin
 Drug Info Investigative Discovery agent ICD: N.A. [20]
Cis-4-hydroxytamoxifen
 Drug Info Investigative Discovery agent ICD: N.A. [27]
Anthraflavic acid
 Drug Info Investigative Discovery agent ICD: N.A. [20]
      Experimental Enzyme Kinetic Data of Drugs Click to Show/Hide the Full List of Drugs:          5 Drugs
Curcumin
 Drug Info Phase 3 Stomach cancer Km = 0.1 microM [20]
Eugenol
 Drug Info Investigative Discovery agent Km = 0.0084 microM [20]
Phloretin
 Drug Info Investigative Discovery agent Km = 0.0068 microM [20]
Chrysin
 Drug Info Investigative Discovery agent Km = 0.004 microM [20]
Anthraflavic acid
 Drug Info Investigative Discovery agent Km = 0.01 microM [20]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR009142 AKB-6548 Vadadustat-O-glucuronide Conjugation - O-glucuronidation AKB-6548 [19]
MR011560 AR-67 AR-67 glucuronides Unclear - Unclear AR-67 [25]
MR007264 Catechol intermediate ARQ-501 M2 Conjugation - Monoglucuronidation ARQ-501 [28]
MR008613 BAICALEIN Baicalein-7-O-glucuronide Unclear - Unclear BAICALEIN [29]
MR005294 Cis-4-hydroxytamoxifen Cis-4-hydroxytamoxifen-O-glucuronide Conjugation - Glucuronidation Cis-4-hydroxytamoxifen [27]
MR013043 Darexaban maleate Darexaban glucuronide Unclear - Unclear Darexaban maleate [30], [26]
MR000896 Edaravone Edaravone glucuronide conjugates Conjugation - Glucuronidation Edaravone [11]
MR007850 Propofol Propofol-O-glucuronide Conjugation - O-glucuronidation Fospropofol disodium [1]
MR007455 FYX-051 Unclear Conjugation - N1-Glucuronidation FYX-051 [31]
MR007455 FYX-051 Unclear Conjugation - N2-Glucuronidation FYX-051 [31]
MR011092 Gaboxadol Gaboxadol-O-glucuronide Conjugation - O-glucuronidation Gaboxadol [14]
MR008303 LJN452 LJN452 metabolite M22 Conjugation - Glucuronidation LJN452 [23]
MR004815 Mycophenolate mofetil Mycophenolic acid glucuronide Conjugation - Glucuronidation Mycophenolate mofetil [3]
MR004816 Mycophenolate mofetil Mycophenolic acyl-glucuronide (AcMPAG) Conjugation - Glucuronidation Mycophenolate mofetil [3]
MR004824 Mycophenolic acid Mycophenolic acid glucuronide Conjugation - O-glucuronidation Mycophenolic acid [8], [9]
MR004873 O-Desmethylnaproxen O-Desmethylnaproxen acyl glucuronide Conjugation - Glucuronidation Naproxen [5]
MR004872 O-Desmethylnaproxen O-Desmethylnaproxen O-glucuronide Conjugation - Glucuronidation Naproxen [5]
MR012707 Phloretin Unclear Conjugation - Glucuronidation Phloretin [20]
MR008594 Puerarin Puerarin-7-O-glucuronide Conjugation - Glucuronidation Puerarin [21]
MR005262 Silymarin 20-O-beta-D-Glu Conjugation - Glucuronidation Silymarin [17], [18]
MR005263 Silymarin Silybin 7-glucoside Conjugation - Glucuronidation Silymarin [17], [18]
MR007484 SN-38 SN-38G Conjugation - Glucuronidation SN-38 [32], [33]
MR002375 Telmisartan Telmisartan glucuronide Conjugation - Glucuronidation Telmisartan [34]
⏷ Show the Full List of 23 MR(s)
References
1 Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects
2 Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol Drug Metab Dispos. 2021 Oct;49(10):882-891. doi: 10.1124/dmd.120.000350.
3 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
4 Metabolism and disposition of opicapone in the rat and metabolic enzymes phenotyping
5 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.
6 Characterization of Enzymes Involved in Nintedanib Metabolism in Humans
7 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.
8 Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96.
9 The main role of UGT1A9 in the hepatic metabolism of mycophenolic acid and the effects of naturally occurring variants
10 Identification of the UDP-glucuronosyltransferase isoforms involved in mycophenolic acid phase II metabolism. Drug Metab Dispos. 2005 Jan;33(1):139-46.
11 LABEL:ADICAVA- edaravone injection RADICAVA ORS- edaravone kit
12 U. S. FDA Label -Hesperidin
13 Uridine 5'-diphospho-glucuronosyltransferase genetic polymorphisms and response to cancer chemotherapy. Future Oncol. 2010 Apr;6(4):563-85.
14 Metabolism and renal elimination of gaboxadol in humans: role of UDP-glucuronosyltransferases and transporters
15 Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin Drug Metab Dispos. 2012 Apr;40(4):825-35. doi: 10.1124/dmd.111.043984.
16 In vitro glucuronidation of the angiotensin II receptor antagonist telmisartan in the cat: a comparison with other species
17 Evidence for differences in regioselective and stereoselective glucuronidation of silybin diastereomers from milk thistle (Silybum marianum) by human UDP-glucuronosyltransferases
18 Metabolism, Transport and Drug-Drug Interactions of Silymarin
19 DrugBank(Pharmacology-Metabolism):AKB-6548
20 Differential and special properties of the major human UGT1-encoded gastrointestinal UDP-glucuronosyltransferases enhance potential to control chemical uptake. J Biol Chem. 2004 Jan 9;279(2):1429-41.
21 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for puerarin metabolism in human liver microsomes
22 Involvement of UDP-glucuronosyltransferases in the extensive liver and intestinal first-pass metabolism of flavonoid baicalein
23 Evaluation of the Absorption, Metabolism, and Excretion of a Single Oral 1-mg Dose of Tropifexor in Healthy Male Subjects and the Concentration Dependence of Tropifexor Metabolism
24 Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation
25 Metabolic pathways of the camptothecin analog AR-67
26 Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine
27 Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2006-14.
28 Metabolic profile, enzyme kinetics, and reaction phenotyping of -lapachone metabolism in human liver and intestine in vitro
29 Hepatic metabolism and disposition of baicalein via the coupling of conjugation enzymes and transporters-in vitro and in vivo evidences
30 Absorption, metabolism and excretion of darexaban (YM150), a new direct factor Xa inhibitor in humans
31 DrugBank(Pharmacology-Metabolism):FYX-051
32 Clinical pharmacokinetics and metabolism of irinotecan (CPT-11)
33 Individualization of Irinotecan Treatment: A Review of Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics
34 Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. Drug Metab Dispos. 2012 Apr;40(4):825-35.

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