Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DEF2WXN)

• DME Name: UDP-glucuronosyltransferase 1A3 (UGT1A3)
• Synonyms: UDP-glucuronosyltransferase family 1 member A3; UDP-glucuronosyltransferase 1-C; UDP-glucuronosyltransferase 1-3; UDPGT 1-3; UGT-1C; UGT1*3; UGT1-03; UGT1.3; UGT1A3; UGT1C
• Gene Name: UGT1A3
• UniProt ID: UD13_HUMAN
• INTEDE ID: DME0041
• Gene ID: 54659
• EC Number:
  EC: 2.4.1.17
  Transferase
  Glycosyltransferases
  Hexosyltransferase
  EC: 2.4.1.17
• Lineage:
  Species: Homo sapiens
  Kingdom: Metazoa
  Phylum: Chordata
  Class: Mammalia
  Order: Primates
  Family: Hominidae
  Genus: Homo
  Species: Homo sapiens
• Sequence:
  MATGLQVPLPWLATGLLLLLSVQPWAESGKVLVVPIDGSHWLSMREVLRELHARGHQAVV
  LTPEVNMHIKEENFFTLTTYAISWTQDEFDRHVLGHTQLYFETEHFLKKFFRSMAMLNNM
  SLVYHRSCVELLHNEALIRHLNATSFDVVLTDPVNLCAAVLAKYLSIPTVFFLRNIPCDL
  DFKGTQCPNPSSYIPRLLTTNSDHMTFMQRVKNMLYPLALSYICHAFSAPYASLASELFQ
  REVSVVDILSHASVWLFRGDFVMDYPRPIMPNMVFIGGINCANRKPLSQEFEAYINASGE
  HGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQND
  LLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMT
  SEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAH
  DLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
• Function: This enzyme is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
• KEGG 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)
• Reactome Pathway:
  NR1H2 & NR1H3 regulate gene expression to control bile acid homeostasis (R-HSA-9623433)
  Glucuronidation (R-HSA-156588)

Molecular Interaction Atlas (MIA) of This DME

34 Approved Drug(s) Metabolized by This DME

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ambrisentan	DMD1QXW	Pulmonary arterial hypertension	BB01.0	Approved	[1]
Anastrozole	DMNP60F	Breast cancer	2C60-2C65	Approved	[2]
Atorvastatin	DMF28YC	Cardiovascular disease	BA00-BE2Z	Approved	[3]
Baloxavir marboxil	DM1UV7F	Influenza virus infection	1E30-1E32	Approved	[4]
Candesartan	DMRK8OT	Hypertension	BA00-BA04	Approved	[5]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[6]
Cyproheptadine	DM92AH3	Rhinitis	FA20	Approved	[7]
Darolutamide	DMV7YFT	Prostate cancer	2C82.0	Approved	[8]
Deferasirox	DM6ETS0	Hypophosphatasia	5C64.3	Approved	[9]
Dexibuprofen	DMFYBD0	Ankylosing spondylitis	FA92.0	Approved	[5]
Diclofenac	DMPIHLS	Osteoarthritis	FA00-FA05	Approved	[10]
Empagliflozin	DMRF9YK	Type-1 diabetes	5A10	Approved	[11]
Etodolac	DM6WJO9	Pain	MG30-MG3Z	Approved	[5]
Ezetimibe	DM7A8TW	Hypercholesterolaemia	5C80.0	Approved	[12]
Flurbiprofen	DMGN4BY	Rheumatoid arthritis	FA20	Approved	[5]
Gemfibrozil	DMD8Q3J	Hyperlipidaemia	5C80	Approved	[13]
Hydromorphone	DMHP21E	Pain	MG30-MG3Z	Approved	[14]
Ibuprofen	DM8VCBE	Pain	MG30-MG3Z	Approved	[5]
Irbesartan	DMTP1DC	Hypertension	BA00-BA04	Approved	[5]
Ketotifen	DM74XKS	Conjunctivitis	9A60	Approved	[]
Lamotrigine	DM8SXYG	Bipolar disorder	6A60	Approved	[15]
Lorlatinib	DMICDLV	Non-small-cell lung cancer	2C25.Y	Approved	[16]
Losartan	DM72JXH	Hypertension	BA00-BA04	Approved	[5]
Lovastatin	DM9OZWQ	Hypercholesterolaemia	5C80.0	Approved	[17]
Mitiglinide	DMP8HEL	Diabetic complication	5A2Y	Approved	[5]
Morphine	DMRMS0L	Chronic pain	MG30	Approved	[7]
Naproxen	DMZ5RGV	Osteoarthritis	FA00-FA05	Approved	[18]
Pitavastatin calcium	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[19]
Retigabine	DMGNYIH	Behcet disease	4A62	Approved	[20]
Simvastatin	DM30SGU	Hypercholesterolaemia	5C80.0	Approved	[17]
Telmisartan	DMS3GX2	Hypertension	BA00-BA04	Approved	[21]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[22]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[23]
Vorinostat	DMWMPD4	Cutaneous T-cell lymphoma	2B01	Approved	[24]

5 Clinical Trial Drug(s) Metabolized by This DME

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LCQ908	DMFLJHQ	Familial chylomicronemia syndrome	5C80	Phase 3	[25]
Muraglitazar	DMG3NFZ	N. A.	N. A.	Phase 3	[26]
Rivoglitazone	DMBY31K	Ocular inflammation	9C61.24	Phase 3	[27]
TAK-875	DMIM5AP	Type-2 diabetes	5A11	Phase 3	[28]
Bevirimat	DML2D8Q	Human immunodeficiency virus infection	1C62	Phase 2	[29]

2 Discontinued Drug(s) Metabolized by This DME

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gavestinel	DM8IL1U	Nerve injury	ND56.4	Discontinued in Phase 2	[5]
Licofelone	DM7HLFD	Osteoarthritis	FA00-FA05	Discontinued in Phase 1	[30]

References

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• [23] Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
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