Details of Drug Off-Target (DOT)

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

• DOT Name: UDP-glucuronosyltransferase 1A9
• Synonyms: UGT1A9; EC 2.4.1.17; UDP-glucuronosyltransferase 1-9; UDPGT 1-9; UGT1*9; UGT1-09; UGT1.9; UDP-glucuronosyltransferase 1-I; UGT-1I; UGT1I; lugP4
• Gene Name: UGT1A9
• UniProt ID: UD19_HUMAN
• EC Number: 2.4.1.17
• Pfam ID: PF00201
• Sequence:
  MACTGWTSPLPLCVCLLLTCGFAEAGKLLVVPMDGSHWFTMRSVVEKLILRGHEVVVVMP
  EVSWQLGRSLNCTVKTYSTSYTLEDLDREFKAFAHAQWKAQVRSIYSLLMGSYNDIFDLF
  FSNCRSLFKDKKLVEYLKESSFDAVFLDPFDNCGLIVAKYFSLPSVVFARGILCHYLEEG
  AQCPAPLSYVPRILLGFSDAMTFKERVRNHIMHLEEHLLCHRFFKNALEIASEILQTPVT
  EYDLYSHTSIWLLRTDFVLDYPKPVMPNMIFIGGINCHQGKPLPMEFEAYINASGEHGIV
  VFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLLGH
  PMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSEDL
  ENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDLTW
  YQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
• 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. Also catalyzes the glucuronidation of the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist caderastan, a drug which can inhibit the effect of angiotensin II. Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan. Also metabolizes mycophenolate, an immunosuppressive agent ; [Isoform 2]: Lacks UGT glucuronidation 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, colon, 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:
  PPARA activates gene expression (R-HSA-1989781)
  Aspirin ADME (R-HSA-9749641)
  Paracetamol ADME (R-HSA-9753281)
  Glucuronidation (R-HSA-156588)

Molecular Interaction Atlas (MIA) of This DOT

This DOT Affected the Biotransformations of 50 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Ethanol	DMDRQZU	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Ethanol.	[25]
Irinotecan	DMP6SC2	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Irinotecan.	[26]
Diclofenac	DMPIHLS	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Diclofenac.	[27]
Nicotine	DMWX5CO	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Nicotine.	[28]
Indomethacin	DMSC4A7	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Indomethacin.	[29]
Capsaicin	DMGMF6V	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Capsaicin.	[30]
Ibuprofen	DM8VCBE	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Ibuprofen.	[29]
Ursodeoxycholic acid	DMCUT21	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Ursodeoxycholic acid.	[31]
Estrone	DM5T6US	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Estrone.	[32]
Morphine	DMRMS0L	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Morphine.	[34]
Masoprocol	DMMVNZ0	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Masoprocol.	[30]
Flurbiprofen	DMGN4BY	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Flurbiprofen.	[29]
Naproxen	DMZ5RGV	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Naproxen.	[35]
Etodolac	DM6WJO9	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Etodolac.	[35]
Ketoprofen	DMRKXPT	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Ketoprofen.	[35]
Tolcapone	DM8MNVO	Approved	UDP-glucuronosyltransferase 1A9 decreases the glucuronidation of Tolcapone.	[36]
Cotinine	DMCEZ1B	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Cotinine.	[37]
Entacapone	DMLBVKQ	Approved	UDP-glucuronosyltransferase 1A9 decreases the glucuronidation of Entacapone.	[36]
Ofloxacin	DM0VQN3	Approved	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Ofloxacin.	[38]
LAROPIPRANT	DM5FABJ	Phase 4	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of LAROPIPRANT.	[42]
Resveratrol	DM3RWXL	Phase 3	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Resveratrol.	[43]
Curcumin	DMQPH29	Phase 3	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Curcumin.	[30]
Ranirestat	DMD5QRS	Phase 3	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Ranirestat.	[44]
Muraglitazar	DMG3NFZ	Phase 3	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Muraglitazar.	[45]
Genistein	DM0JETC	Phase 2/3	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Genistein.	[30]
Sitafloxacin	DMTV5XC	Phase 2	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Sitafloxacin.	[38]
Eugenol	DM7US1H	Patented	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Eugenol.	[30]
Steroid derivative 1	DMB0NVQ	Patented	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Steroid derivative 1.	[47]
Bropirimine	DMMT1YQ	Discontinued in Phase 3	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Bropirimine.	[48]
EMODIN	DMAEDQG	Terminated	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of EMODIN.	[30]
Coumestrol	DM40TBU	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Coumestrol.	[30]
Arachidonic acid	DMUOQZD	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Arachidonic acid.	[49]
BRN-3548355	DM4KXT0	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of BRN-3548355.	[50]
Chrysin	DM7V2LG	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Chrysin.	[30]
Daidzein	DMRFTJX	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Daidzein.	[30]
Apigenin	DMI3491	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Apigenin.	[30]
Farnesol	DMV2X1B	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Farnesol.	[51]
biochanin A	DM0HPWY	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of biochanin A.	[30]
3,7,3',4'-TETRAHYDROXYFLAVONE	DMES906	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of 3,7,3',4'-TETRAHYDROXYFLAVONE.	[30]
Aloe-emodin	DMPTY8S	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Aloe-emodin.	[52]
Plumbagin	DM9BS50	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Plumbagin.	[30]
Formononetin	DM7WFZ8	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Formononetin.	[30]
Mononitrophenol	DM4QO9G	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Mononitrophenol.	[53]
ACMC-1AKLT	DMRQ70X	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of ACMC-1AKLT.	[54]
7-hydroxycoumarin	DMTMNO7	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of 7-hydroxycoumarin.	[53]
Hydroxyestrone	DMBO7ZD	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Hydroxyestrone.	[47]
BRN-1999480	DMC9Q4D	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of BRN-1999480.	[47]
Anthraflavic acid	DMN1YFU	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Anthraflavic acid.	[30]
SCOPOLETIN	DM645FP	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of SCOPOLETIN.	[53]
Quinizarin	DMRQCK3	Investigative	UDP-glucuronosyltransferase 1A9 increases the glucuronidation of Quinizarin.	[30]

This DOT Affected the Drug Response of 5 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Bezafibrate	DMZDCS0	Approved	UDP-glucuronosyltransferase 1A9 increases the response to substance of Bezafibrate.	[33]
Probenecid	DMMFWOJ	Approved	UDP-glucuronosyltransferase 1A9 affects the response to substance of Probenecid.	[33]
Raltegravir	DMYURI6	Approved	UDP-glucuronosyltransferase 1A9 affects the response to substance of Raltegravir.	[41]
Benoxaprofen	DM5ZOX8	Withdrawn from market	UDP-glucuronosyltransferase 1A9 affects the response to substance of Benoxaprofen.	[33]
Fibrates	DMFNTMY	Investigative	UDP-glucuronosyltransferase 1A9 affects the response to substance of Fibrates.	[33]

This DOT Affected the Regulation of Drug Effects of 3 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Oxazepam	DMXNZM4	Approved	UDP-glucuronosyltransferase 1A9 increases the metabolism of Oxazepam.	[39]
Bexagliflozin	DMK56G0	Approved	UDP-glucuronosyltransferase 1A9 increases the metabolism of Bexagliflozin.	[40]
Puerarin	DMJIMXH	Phase 2	UDP-glucuronosyltransferase 1A9 increases the metabolism of Puerarin.	[46]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the expression of UDP-glucuronosyltransferase 1A9.	[1]
Acetaminophen	DMUIE76	Approved	Acetaminophen decreases the expression of UDP-glucuronosyltransferase 1A9.	[2]
Estradiol	DMUNTE3	Approved	Estradiol decreases the activity of UDP-glucuronosyltransferase 1A9.	[3]
Quercetin	DM3NC4M	Approved	Quercetin decreases the activity of UDP-glucuronosyltransferase 1A9.	[4]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of UDP-glucuronosyltransferase 1A9.	[5]
Methotrexate	DM2TEOL	Approved	Methotrexate decreases the expression of UDP-glucuronosyltransferase 1A9.	[6]
Obeticholic acid	DM3Q1SM	Approved	Obeticholic acid decreases the expression of UDP-glucuronosyltransferase 1A9.	[7]
Rifampicin	DM5DSFZ	Approved	Rifampicin increases the expression of UDP-glucuronosyltransferase 1A9.	[8]
Chenodiol	DMQ8JIK	Approved	Chenodiol decreases the expression of UDP-glucuronosyltransferase 1A9.	[9]
Propofol	DMB4OLE	Approved	Propofol decreases the activity of UDP-glucuronosyltransferase 1A9.	[3]
Omeprazole	DM471KJ	Approved	Omeprazole increases the expression of UDP-glucuronosyltransferase 1A9.	[10]
Niflumic acid	DMJ3I1Q	Approved	Niflumic acid decreases the activity of UDP-glucuronosyltransferase 1A9.	[11]
Tucatinib	DMBESUA	Approved	Tucatinib decreases the activity of UDP-glucuronosyltransferase 1A9.	[12]
Opicapone	DM1BKA6	Approved	Opicapone decreases the activity of UDP-glucuronosyltransferase 1A9.	[13]
3,4-Dihydroxycinnamic Acid	DMVZL26	Phase 4	3,4-Dihydroxycinnamic Acid decreases the activity of UDP-glucuronosyltransferase 1A9.	[14]
LM-94	DMW3QGJ	Phase 1/2	LM-94 increases the activity of UDP-glucuronosyltransferase 1A9.	[15]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of UDP-glucuronosyltransferase 1A9.	[16]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of UDP-glucuronosyltransferase 1A9.	[17]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of UDP-glucuronosyltransferase 1A9.	[18]
Kaempferol	DMHEMUB	Investigative	Kaempferol decreases the activity of UDP-glucuronosyltransferase 1A9.	[4]
(E)-4-(3,5-dimethoxystyryl)phenol	DMYXI2V	Investigative	(E)-4-(3,5-dimethoxystyryl)phenol decreases the activity of UDP-glucuronosyltransferase 1A9.	[19]
2-tert-butylbenzene-1,4-diol	DMNXI1E	Investigative	2-tert-butylbenzene-1,4-diol increases the expression of UDP-glucuronosyltransferase 1A9.	[20]
Myricetin	DMTV4L0	Investigative	Myricetin decreases the activity of UDP-glucuronosyltransferase 1A9.	[4]
Chlorogenic acid	DM2Y3P4	Investigative	Chlorogenic acid decreases the activity of UDP-glucuronosyltransferase 1A9.	[14]
Morin	DM2OGZ5	Investigative	Morin decreases the activity of UDP-glucuronosyltransferase 1A9.	[4]
Piceatannol	DMYOP45	Investigative	Piceatannol decreases the activity of UDP-glucuronosyltransferase 1A9.	[21]
Galangin	DM5TQ2O	Investigative	Galangin decreases the activity of UDP-glucuronosyltransferase 1A9.	[4]
MANGIFERIN	DMWAF5Z	Investigative	MANGIFERIN increases the expression of UDP-glucuronosyltransferase 1A9.	[22]
Phloretin	DMYA50U	Investigative	Phloretin decreases the activity of UDP-glucuronosyltransferase 1A9.	[14]
AMENTOFLAVONE	DMLRNV2	Investigative	AMENTOFLAVONE decreases the activity of UDP-glucuronosyltransferase 1A9.	[23]
pregnenolone-16alpha-carbonitrile	DM0LW7G	Investigative	pregnenolone-16alpha-carbonitrile increases the expression of UDP-glucuronosyltransferase 1A9.	[24]
Phlorizin	DMNARGO	Investigative	Phlorizin decreases the activity of UDP-glucuronosyltransferase 1A9.	[14]

References

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