Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTUEOER3)

• DOT Name: UDP-glucuronosyltransferase 1A3
• Synonyms: UGT1A3; EC 2.4.1.17; UDP-glucuronosyltransferase 1-3; UDPGT 1-3; UGT1*3; UGT1-03; UGT1.3; UDP-glucuronosyltransferase 1-C; UGT-1C; UGT1C; UDP-glucuronosyltransferase 1A isoform 3
• Gene Name: UGT1A3
• UniProt ID: UD13_HUMAN
• EC Number: 2.4.1.17
• Pfam ID: PF00201
• Sequence:
  MATGLQVPLPWLATGLLLLLSVQPWAESGKVLVVPIDGSHWLSMREVLRELHARGHQAVV
  LTPEVNMHIKEENFFTLTTYAISWTQDEFDRHVLGHTQLYFETEHFLKKFFRSMAMLNNM
  SLVYHRSCVELLHNEALIRHLNATSFDVVLTDPVNLCAAVLAKYLSIPTVFFLRNIPCDL
  DFKGTQCPNPSSYIPRLLTTNSDHMTFMQRVKNMLYPLALSYICHAFSAPYASLASELFQ
  REVSVVDILSHASVWLFRGDFVMDYPRPIMPNMVFIGGINCANRKPLSQEFEAYINASGE
  HGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQND
  LLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMT
  SEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAH
  DLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
• Function: [Isoform 1]: UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol and estrone. Contributes to bile acid (BA) detoxification by catalyzing the glucuronidation of BA substrates, which are natural detergents for dietary lipids absorption. Involved in the glucuronidation of calcidiol, which is the major circulating form of vitamin D3, essential for the regulation of calcium and phosphate homeostasis. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonists losartan, candesartan and zolarsartan, which can inhibit the effect of angiotensin II ; [Isoform 2]: Lacks UDP-glucuronosyltransferase (UGT) activity but acts as a negative regulator of isoform 1.
• Tissue Specificity: .Expressed in liver, kidney, colon, esophagus and small intestine.; [Isoform 2]: Expressed in liver, kidney and colon. Not expressed in esophagus and small intestine.
• KEGG Pathway:
  Pentose and glucuro.te interconversions (hsa00040)
  Ascorbate and aldarate metabolism (hsa00053)
  Steroid hormone biosynthesis (hsa00140)
  Retinol metabolism (hsa00830)
  Porphyrin metabolism (hsa00860)
  Metabolism of xenobiotics by cytochrome P450 (hsa00980)
  Drug metabolism - cytochrome P450 (hsa00982)
  Drug metabolism - other enzymes (hsa00983)
  Metabolic pathways (hsa01100)
  Biosynthesis of cofactors (hsa01240)
  Bile secretion (hsa04976)
  Chemical carcinogenesis - D. adducts (hsa05204)
  Chemical carcinogenesis - receptor activation (hsa05207)
• Reactome Pathway:
  NR1H2 & NR1H3 regulate gene expression to control bile acid homeostasis (R-HSA-9623433)
  Aspirin ADME (R-HSA-9749641)
  Atorvastatin ADME (R-HSA-9754706)
  Prednisone ADME (R-HSA-9757110)
  Glucuronidation (R-HSA-156588)
• BioCyc Pathway: MetaCyc:HS09519-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

This DOT Affected the Biotransformations of 54 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Acetaminophen	DMUIE76	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Acetaminophen.	[20]
Vorinostat	DMWMPD4	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Vorinostat.	[22]
Diethylstilbestrol	DMN3UXQ	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Diethylstilbestrol.	[23]
Aspirin	DM672AH	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Aspirin.	[20]
Etoposide	DMNH3PG	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Etoposide.	[24]
Nicotine	DMWX5CO	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Nicotine.	[25]
Indomethacin	DMSC4A7	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Indomethacin.	[20]
Obeticholic acid	DM3Q1SM	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Obeticholic acid.	[11]
Sulindac	DM2QHZU	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Sulindac.	[26]
Ibuprofen	DM8VCBE	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ibuprofen.	[20]
Ursodeoxycholic acid	DMCUT21	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ursodeoxycholic acid.	[11]
Estrone	DM5T6US	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Estrone.	[20]
Morphine	DMRMS0L	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Morphine.	[27]
Estriol	DMOEM2I	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Estriol.	[20]
Flurbiprofen	DMGN4BY	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Flurbiprofen.	[20]
Mefenamic acid	DMK7HFI	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Mefenamic acid.	[20]
Naproxen	DMZ5RGV	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Naproxen.	[28]
Etodolac	DM6WJO9	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Etodolac.	[28]
Ketoprofen	DMRKXPT	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ketoprofen.	[28]
Salicyclic acid	DM2F8XZ	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Salicyclic acid.	[20]
Lamotrigine	DM8SXYG	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Lamotrigine.	[29]
Furosemide	DMMQ8ZG	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Furosemide.	[20]
Entacapone	DMLBVKQ	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Entacapone.	[30]
Ofloxacin	DM0VQN3	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ofloxacin.	[32]
Ezetimibe	DM7A8TW	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ezetimibe.	[33]
Fenoprofen	DML5VQ0	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Fenoprofen.	[20]
Diflunisal	DM7EN8I	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Diflunisal.	[20]
Felbinac	DMKZEIB	Approved	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Felbinac.	[20]
LAROPIPRANT	DM5FABJ	Phase 4	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of LAROPIPRANT.	[34]
Resveratrol	DM3RWXL	Phase 3	UDP-glucuronosyltransferase 1A3 affects the glucuronidation of Resveratrol.	[35]
EXISULIND	DMBY56U	Phase 3	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of EXISULIND.	[26]
Ranirestat	DMD5QRS	Phase 3	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ranirestat.	[36]
Muraglitazar	DMG3NFZ	Phase 3	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Muraglitazar.	[37]
Sitafloxacin	DMTV5XC	Phase 2	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Sitafloxacin.	[32]
Flavonoid derivative 1	DMCQP0B	Patented	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Flavonoid derivative 1.	[39]
T83193	DMHO29Y	Patented	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of T83193.	[20]
Steroid derivative 1	DMB0NVQ	Patented	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Steroid derivative 1.	[20]
Ferulic Acid	DMJC7NF	Patented	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Ferulic Acid.	[20]
INDOPROFEN	DM5QSKN	Withdrawn from market	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of INDOPROFEN.	[20]
Bropirimine	DMMT1YQ	Discontinued in Phase 3	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Bropirimine.	[40]
Arachidonic acid	DMUOQZD	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Arachidonic acid.	[41]
Farnesol	DMV2X1B	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Farnesol.	[42]
methyl salicylate	DMKCG8H	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of methyl salicylate.	[20]
BETULIN	DMGQRON	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of BETULIN.	[43]
Mononitrophenol	DM4QO9G	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Mononitrophenol.	[30]
2-hydroxy-17beta-estradiol	DMM9Z0B	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of 2-hydroxy-17beta-estradiol.	[20]
Fibrates	DMFNTMY	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Fibrates.	[20]
Cinnamic acid	DM340FH	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Cinnamic acid.	[20]
Hydroxyestrone	DMBO7ZD	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Hydroxyestrone.	[20]
BRN-1999480	DMC9Q4D	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of BRN-1999480.	[20]
SCOPOLETIN	DM645FP	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of SCOPOLETIN.	[30]
Lauric Acid	DM9C8KQ	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Lauric Acid.	[44]
Decanoic Acid	DM8FMYL	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Decanoic Acid.	[44]
Diphenylacetic Acid	DMP6IHR	Investigative	UDP-glucuronosyltransferase 1A3 increases the glucuronidation of Diphenylacetic Acid.	[20]

This DOT Affected the Drug Response of 3 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Cisplatin	DMRHGI9	Approved	UDP-glucuronosyltransferase 1A3 affects the response to substance of Cisplatin.	[21]
Probenecid	DMMFWOJ	Approved	UDP-glucuronosyltransferase 1A3 affects the response to substance of Probenecid.	[31]
Benoxaprofen	DM5ZOX8	Withdrawn from market	UDP-glucuronosyltransferase 1A3 affects the response to substance of Benoxaprofen.	[31]

This DOT Affected the Regulation of Drug Effects of 1 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Puerarin	DMJIMXH	Phase 2	UDP-glucuronosyltransferase 1A3 increases the metabolism of Puerarin.	[38]

1 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the methylation of UDP-glucuronosyltransferase 1A3.	[1]

33 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of UDP-glucuronosyltransferase 1A3.	[2]
Quercetin	DM3NC4M	Approved	Quercetin decreases the activity of UDP-glucuronosyltransferase 1A3.	[3]
Phenobarbital	DMXZOCG	Approved	Phenobarbital increases the expression of UDP-glucuronosyltransferase 1A3.	[4]
Rosiglitazone	DMILWZR	Approved	Rosiglitazone increases the expression of UDP-glucuronosyltransferase 1A3.	[5]
Diclofenac	DMPIHLS	Approved	Diclofenac decreases the activity of UDP-glucuronosyltransferase 1A3.	[6]
Fenofibrate	DMFKXDY	Approved	Fenofibrate increases the expression of UDP-glucuronosyltransferase 1A3.	[7]
Rifampicin	DM5DSFZ	Approved	Rifampicin increases the expression of UDP-glucuronosyltransferase 1A3.	[8]
Chenodiol	DMQ8JIK	Approved	Chenodiol increases the expression of UDP-glucuronosyltransferase 1A3.	[9]
Omeprazole	DM471KJ	Approved	Omeprazole increases the expression of UDP-glucuronosyltransferase 1A3.	[10]
Lapatinib	DM3BH1Y	Approved	Lapatinib decreases the activity of UDP-glucuronosyltransferase 1A3.	[11]
Osimertinib	DMRJLAT	Approved	Osimertinib decreases the activity of UDP-glucuronosyltransferase 1A3.	[12]
Flunitrazepam	DMGR5Z3	Approved	Flunitrazepam decreases the activity of UDP-glucuronosyltransferase 1A3.	[6]
Tucatinib	DMBESUA	Approved	Tucatinib decreases the activity of UDP-glucuronosyltransferase 1A3.	[13]
3,4-Dihydroxycinnamic Acid	DMVZL26	Phase 4	3,4-Dihydroxycinnamic Acid decreases the activity of UDP-glucuronosyltransferase 1A3.	[14]
Genistein	DM0JETC	Phase 2/3	Genistein decreases the expression of UDP-glucuronosyltransferase 1A3.	[2]
LM-94	DMW3QGJ	Phase 1/2	LM-94 increases the activity of UDP-glucuronosyltransferase 1A3.	[15]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of UDP-glucuronosyltransferase 1A3.	[16]
P1A	DMWCAQD	Discontinued in Phase 2	P1A increases the expression of UDP-glucuronosyltransferase 1A3.	[7]
PIRINIXIC ACID	DM82Y75	Preclinical	PIRINIXIC ACID increases the expression of UDP-glucuronosyltransferase 1A3.	[7]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of UDP-glucuronosyltransferase 1A3.	[2]
Bilirubin	DMI0V4O	Investigative	Bilirubin decreases the activity of UDP-glucuronosyltransferase 1A3.	[6]
Kaempferol	DMHEMUB	Investigative	Kaempferol decreases the activity of UDP-glucuronosyltransferase 1A3.	[3]
(E)-4-(3,5-dimethoxystyryl)phenol	DMYXI2V	Investigative	(E)-4-(3,5-dimethoxystyryl)phenol decreases the activity of UDP-glucuronosyltransferase 1A3.	[17]
	DM9CEI5		increases the expression of UDP-glucuronosyltransferase 1A3.	[9]
Myricetin	DMTV4L0	Investigative	Myricetin decreases the activity of UDP-glucuronosyltransferase 1A3.	[3]
Chlorogenic acid	DM2Y3P4	Investigative	Chlorogenic acid decreases the activity of UDP-glucuronosyltransferase 1A3.	[14]
Morin	DM2OGZ5	Investigative	Morin decreases the activity of UDP-glucuronosyltransferase 1A3.	[3]
Galangin	DM5TQ2O	Investigative	Galangin decreases the activity of UDP-glucuronosyltransferase 1A3.	[3]
P-Coumaric Acid	DMGJSVD	Investigative	P-Coumaric Acid decreases the activity of UDP-glucuronosyltransferase 1A3.	[14]
Phloretin	DMYA50U	Investigative	Phloretin decreases the activity of UDP-glucuronosyltransferase 1A3.	[14]
AMENTOFLAVONE	DMLRNV2	Investigative	AMENTOFLAVONE decreases the activity of UDP-glucuronosyltransferase 1A3.	[18]
pregnenolone-16alpha-carbonitrile	DM0LW7G	Investigative	pregnenolone-16alpha-carbonitrile increases the expression of UDP-glucuronosyltransferase 1A3.	[19]
Phlorizin	DMNARGO	Investigative	Phlorizin decreases the activity of UDP-glucuronosyltransferase 1A3.	[14]

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