General Information of Drug Off-Target (DOT) (ID: OTH1C8OJ)

DOT Name UDP-glucuronosyltransferase 1A1
Synonyms UGT1A1; EC 2.4.1.17; Bilirubin-specific UDPGT isozyme 1; hUG-BR1; UDP-glucuronosyltransferase 1-1; UDPGT 1-1; UGT1*1; UGT1-01; UGT1.1; UDP-glucuronosyltransferase 1A isoform 1
Gene Name UGT1A1
Related Disease
Crigler-najjar syndrome type 1 ( )
Crigler-Najjar syndrome type 2 ( )
Gilbert syndrome ( )
UniProt ID
UD11_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
2.4.1.17
Pfam ID
PF00201
Sequence
MAVESQGGRPLVLGLLLCVLGPVVSHAGKILLIPVDGSHWLSMLGAIQQLQQRGHEIVVL
APDASLYIRDGAFYTLKTYPVPFQREDVKESFVSLGHNVFENDSFLQRVIKTYKKIKKDS
AMLLSGCSHLLHNKELMASLAESSFDVMLTDPFLPCSPIVAQYLSLPTVFFLHALPCSLE
FEATQCPNPFSYVPRPLSSHSDHMTFLQRVKNMLIAFSQNFLCDVVYSPYATLASEFLQR
EVTVQDLLSSASVWLFRSDFVKDYPRPIMPNMVFVGGINCLHQNPLSQEFEAYINASGEH
GIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDL
LGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTS
EDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHD
LTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
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, estrone and estriol. Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates. Also catalyzes the glucuronidation 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 losartan, 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 ; [Isoform 2]: Lacks UGT glucuronidation activity but acts as a negative regulator of isoform 1.
Tissue Specificity .Expressed in liver, colon and small intestine. Not expressed in kidney, esophagus and skin.; [Isoform 2]: Expressed in liver, colon, small intestine and kidney. Not expressed in esophagus and skin.
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
Heme degradation (R-HSA-189483 )
Defective UGT1A1 causes hyperbilirubinemia (R-HSA-5579002 )
Aspirin ADME (R-HSA-9749641 )
Paracetamol ADME (R-HSA-9753281 )
Glucuronidation (R-HSA-156588 )

Molecular Interaction Atlas (MIA) of This DOT

3 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Crigler-najjar syndrome type 1 DISBEAZY Definitive Autosomal recessive [1]
Crigler-Najjar syndrome type 2 DISB9PPH Definitive Autosomal recessive [2]
Gilbert syndrome DISMUZF4 Strong Autosomal recessive [3]
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Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 6 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Cisplatin DMRHGI9 Approved UDP-glucuronosyltransferase 1A1 affects the response to substance of Cisplatin. [59]
Vorinostat DMWMPD4 Approved UDP-glucuronosyltransferase 1A1 affects the response to substance of Vorinostat. [61]
Atazanavir DMSYRBX Approved UDP-glucuronosyltransferase 1A1 increases the Bone marrow toxicity ADR of Atazanavir. [68]
Cimetidine DMH61ZB Approved UDP-glucuronosyltransferase 1A1 increases the Haemolytic anaemia ADR of Cimetidine. [69]
Pazopanib DMF57DM Approved UDP-glucuronosyltransferase 1A1 increases the Hemorrhage ADR of Pazopanib. [74]
Prochlorperazine DM53SRA Approved UDP-glucuronosyltransferase 1A1 increases the Metabolic disorder ADR of Prochlorperazine. [69]
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⏷ Show the Full List of 6 Drug(s)
This DOT Affected the Biotransformations of 43 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Estradiol DMUNTE3 Approved UDP-glucuronosyltransferase 1A1 decreases the glucuronidation of Estradiol. [60]
Diethylstilbestrol DMN3UXQ Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Diethylstilbestrol. [62]
Etoposide DMNH3PG Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Etoposide. [63]
Irinotecan DMP6SC2 Approved UDP-glucuronosyltransferase 1A1 decreases the glucuronidation of Irinotecan. [60]
Ethinyl estradiol DMODJ40 Approved UDP-glucuronosyltransferase 1A1 decreases the glucuronidation of Ethinyl estradiol. [60]
Capsaicin DMGMF6V Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Capsaicin. [64]
Ibuprofen DM8VCBE Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Ibuprofen. [65]
Estrone DM5T6US Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Estrone. [66]
Morphine DMRMS0L Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Morphine. [67]
Estriol DMOEM2I Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Estriol. [66]
Masoprocol DMMVNZ0 Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Masoprocol. [64]
Flurbiprofen DMGN4BY Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Flurbiprofen. [65]
Carvedilol DMHTEAO Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Carvedilol. [70]
Entacapone DMLBVKQ Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Entacapone. [71]
Ofloxacin DM0VQN3 Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Ofloxacin. [72]
Ezetimibe DM7A8TW Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Ezetimibe. [73]
Buprenorphine DMPRI8G Approved UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Buprenorphine. [75]
LAROPIPRANT DM5FABJ Phase 4 UDP-glucuronosyltransferase 1A1 increases the glucuronidation of LAROPIPRANT. [76]
Ranirestat DMD5QRS Phase 3 UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Ranirestat. [77]
Muraglitazar DMG3NFZ Phase 3 UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Muraglitazar. [60]
Belinostat DM6OC53 Phase 2 UDP-glucuronosyltransferase 1A1 decreases the glucuronidation of Belinostat. [78]
Sitafloxacin DMTV5XC Phase 2 UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Sitafloxacin. [72]
Eugenol DM7US1H Patented UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Eugenol. [64]
Steroid derivative 1 DMB0NVQ Patented UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Steroid derivative 1. [66]
Bropirimine DMMT1YQ Discontinued in Phase 3 UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Bropirimine. [80]
EMODIN DMAEDQG Terminated UDP-glucuronosyltransferase 1A1 increases the glucuronidation of EMODIN. [64]
Coumestrol DM40TBU Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Coumestrol. [64]
Bilirubin DMI0V4O Investigative UDP-glucuronosyltransferase 1A1 decreases the glucuronidation of Bilirubin. [60]
Arachidonic acid DMUOQZD Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Arachidonic acid. [81]
Farnesol DMV2X1B Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Farnesol. [82]
3,7,3',4'-TETRAHYDROXYFLAVONE DMES906 Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of 3,7,3',4'-TETRAHYDROXYFLAVONE. [64]
Galangin DM5TQ2O Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Galangin. [64]
Plumbagin DM9BS50 Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Plumbagin. [64]
Formononetin DM7WFZ8 Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Formononetin. [64]
Mononitrophenol DM4QO9G Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Mononitrophenol. [71]
2-hydroxy-17beta-estradiol DMM9Z0B Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of 2-hydroxy-17beta-estradiol. [83]
ACMC-1AKLT DMRQ70X Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of ACMC-1AKLT. [84]
20-HETE DM5BAJ9 Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of 20-HETE. [81]
Hydroxyestrone DMBO7ZD Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Hydroxyestrone. [66]
BRN-1999480 DMC9Q4D Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of BRN-1999480. [66]
Anthraflavic acid DMN1YFU Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Anthraflavic acid. [75]
SCOPOLETIN DM645FP Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of SCOPOLETIN. [71]
Quinizarin DMRQCK3 Investigative UDP-glucuronosyltransferase 1A1 increases the glucuronidation of Quinizarin. [64]
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⏷ Show the Full List of 43 Drug(s)
This DOT Affected the Regulation of Drug Effects of 2 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Puerarin DMJIMXH Phase 2 UDP-glucuronosyltransferase 1A1 increases the metabolism of Puerarin. [79]
SN-38G DM2UVNB Investigative UDP-glucuronosyltransferase 1A1 increases the abundance of SN-38G. [85]
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86 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of UDP-glucuronosyltransferase 1A1. [4]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of UDP-glucuronosyltransferase 1A1. [5]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of UDP-glucuronosyltransferase 1A1. [6]
Arsenic DMTL2Y1 Approved Arsenic increases the expression of UDP-glucuronosyltransferase 1A1. [7]
Quercetin DM3NC4M Approved Quercetin increases the expression of UDP-glucuronosyltransferase 1A1. [8]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of UDP-glucuronosyltransferase 1A1. [9]
Testosterone DM7HUNW Approved Testosterone increases the expression of UDP-glucuronosyltransferase 1A1. [9]
Triclosan DMZUR4N Approved Triclosan increases the expression of UDP-glucuronosyltransferase 1A1. [10]
Carbamazepine DMZOLBI Approved Carbamazepine increases the expression of UDP-glucuronosyltransferase 1A1. [11]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of UDP-glucuronosyltransferase 1A1. [12]
Decitabine DMQL8XJ Approved Decitabine increases the expression of UDP-glucuronosyltransferase 1A1. [13]
Phenobarbital DMXZOCG Approved Phenobarbital increases the expression of UDP-glucuronosyltransferase 1A1. [14]
Fulvestrant DM0YZC6 Approved Fulvestrant increases the expression of UDP-glucuronosyltransferase 1A1. [15]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of UDP-glucuronosyltransferase 1A1. [16]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of UDP-glucuronosyltransferase 1A1. [17]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of UDP-glucuronosyltransferase 1A1. [17]
Diclofenac DMPIHLS Approved Diclofenac increases the expression of UDP-glucuronosyltransferase 1A1. [18]
Clozapine DMFC71L Approved Clozapine increases the expression of UDP-glucuronosyltransferase 1A1. [18]
Indomethacin DMSC4A7 Approved Indomethacin decreases the activity of UDP-glucuronosyltransferase 1A1. [19]
Obeticholic acid DM3Q1SM Approved Obeticholic acid increases the expression of UDP-glucuronosyltransferase 1A1. [20]
Fenofibrate DMFKXDY Approved Fenofibrate increases the expression of UDP-glucuronosyltransferase 1A1. [17]
Rifampicin DM5DSFZ Approved Rifampicin increases the expression of UDP-glucuronosyltransferase 1A1. [21]
Sulindac DM2QHZU Approved Sulindac increases the expression of UDP-glucuronosyltransferase 1A1. [22]
Pioglitazone DMKJ485 Approved Pioglitazone increases the expression of UDP-glucuronosyltransferase 1A1. [23]
Phenytoin DMNOKBV Approved Phenytoin increases the expression of UDP-glucuronosyltransferase 1A1. [24]
Ritonavir DMU764S Approved Ritonavir affects the expression of UDP-glucuronosyltransferase 1A1. [25]
Chenodiol DMQ8JIK Approved Chenodiol increases the expression of UDP-glucuronosyltransferase 1A1. [26]
Omeprazole DM471KJ Approved Omeprazole increases the expression of UDP-glucuronosyltransferase 1A1. [27]
Clotrimazole DMMFCIH Approved Clotrimazole affects the expression of UDP-glucuronosyltransferase 1A1. [25]
Nilotinib DM7HXWT Approved Nilotinib decreases the activity of UDP-glucuronosyltransferase 1A1. [28]
Naproxen DMZ5RGV Approved Naproxen decreases the activity of UDP-glucuronosyltransferase 1A1. [19]
Ketoprofen DMRKXPT Approved Ketoprofen decreases the activity of UDP-glucuronosyltransferase 1A1. [19]
Furosemide DMMQ8ZG Approved Furosemide increases the expression of UDP-glucuronosyltransferase 1A1. [18]
Gemfibrozil DMD8Q3J Approved Gemfibrozil increases the expression of UDP-glucuronosyltransferase 1A1. [29]
Osimertinib DMRJLAT Approved Osimertinib decreases the activity of UDP-glucuronosyltransferase 1A1. [30]
Niflumic acid DMJ3I1Q Approved Niflumic acid decreases the activity of UDP-glucuronosyltransferase 1A1. [19]
Flunitrazepam DMGR5Z3 Approved Flunitrazepam decreases the activity of UDP-glucuronosyltransferase 1A1. [31]
Diflunisal DM7EN8I Approved Diflunisal decreases the activity of UDP-glucuronosyltransferase 1A1. [19]
Tucatinib DMBESUA Approved Tucatinib decreases the activity of UDP-glucuronosyltransferase 1A1. [32]
Opicapone DM1BKA6 Approved Opicapone decreases the activity of UDP-glucuronosyltransferase 1A1. [33]
Isoflavone DM7U58J Phase 4 Isoflavone increases the expression of UDP-glucuronosyltransferase 1A1. [34]
3,4-Dihydroxycinnamic Acid DMVZL26 Phase 4 3,4-Dihydroxycinnamic Acid decreases the activity of UDP-glucuronosyltransferase 1A1. [35]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of UDP-glucuronosyltransferase 1A1. [36]
Curcumin DMQPH29 Phase 3 Curcumin increases the expression of UDP-glucuronosyltransferase 1A1. [37]
EXISULIND DMBY56U Phase 3 EXISULIND increases the expression of UDP-glucuronosyltransferase 1A1. [22]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of UDP-glucuronosyltransferase 1A1. [38]
Afimoxifene DMFORDT Phase 2 Afimoxifene decreases the expression of UDP-glucuronosyltransferase 1A1. [15]
LM-94 DMW3QGJ Phase 1/2 LM-94 increases the activity of UDP-glucuronosyltransferase 1A1. [28]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of UDP-glucuronosyltransferase 1A1. [39]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of UDP-glucuronosyltransferase 1A1. [40]
Leflunomide DMR8ONJ Phase 1 Trial Leflunomide increases the expression of UDP-glucuronosyltransferase 1A1. [41]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 increases the expression of UDP-glucuronosyltransferase 1A1. [18]
Flavonoid derivative 1 DMCQP0B Patented Flavonoid derivative 1 increases the expression of UDP-glucuronosyltransferase 1A1. [42]
Ticrynafen DMLFSTR Withdrawn from market Ticrynafen increases the expression of UDP-glucuronosyltransferase 1A1. [18]
PIRINIXIC ACID DM82Y75 Preclinical PIRINIXIC ACID increases the expression of UDP-glucuronosyltransferase 1A1. [43]
Taxifolin DMQJSF9 Preclinical Taxifolin increases the expression of UDP-glucuronosyltransferase 1A1. [42]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of UDP-glucuronosyltransferase 1A1. [44]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of UDP-glucuronosyltransferase 1A1. [45]
Sulforaphane DMQY3L0 Investigative Sulforaphane decreases the expression of UDP-glucuronosyltransferase 1A1. [46]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE DMNQL17 Investigative 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE increases the expression of UDP-glucuronosyltransferase 1A1. [47]
Butanoic acid DMTAJP7 Investigative Butanoic acid increases the expression of UDP-glucuronosyltransferase 1A1. [45]
Chlorpyrifos DMKPUI6 Investigative Chlorpyrifos increases the expression of UDP-glucuronosyltransferase 1A1. [48]
Cycloheximide DMGDA3C Investigative Cycloheximide decreases the expression of UDP-glucuronosyltransferase 1A1. [15]
Dibutyl phthalate DMEDGKO Investigative Dibutyl phthalate increases the expression of UDP-glucuronosyltransferase 1A1. [48]
Rutin DMEHRAJ Investigative Rutin increases the expression of UDP-glucuronosyltransferase 1A1. [21]
Chrysin DM7V2LG Investigative Chrysin increases the expression of UDP-glucuronosyltransferase 1A1. [49]
Kaempferol DMHEMUB Investigative Kaempferol decreases the activity of UDP-glucuronosyltransferase 1A1. [50]
CATECHIN DMY38SB Investigative CATECHIN decreases the activity of UDP-glucuronosyltransferase 1A1. [35]
Daidzein DMRFTJX Investigative Daidzein increases the activity of UDP-glucuronosyltransferase 1A1. [51]
(E)-4-(3,5-dimethoxystyryl)phenol DMYXI2V Investigative (E)-4-(3,5-dimethoxystyryl)phenol decreases the activity of UDP-glucuronosyltransferase 1A1. [52]
Apigenin DMI3491 Investigative Apigenin increases the expression of UDP-glucuronosyltransferase 1A1. [53]
biochanin A DM0HPWY Investigative biochanin A increases the expression of UDP-glucuronosyltransferase 1A1. [34]
Myricetin DMTV4L0 Investigative Myricetin decreases the activity of UDP-glucuronosyltransferase 1A1. [50]
Chlorogenic acid DM2Y3P4 Investigative Chlorogenic acid decreases the activity of UDP-glucuronosyltransferase 1A1. [35]
Morin DM2OGZ5 Investigative Morin decreases the activity of UDP-glucuronosyltransferase 1A1. [50]
MANGIFERIN DMWAF5Z Investigative MANGIFERIN increases the expression of UDP-glucuronosyltransferase 1A1. [54]
P-Coumaric Acid DMGJSVD Investigative P-Coumaric Acid decreases the activity of UDP-glucuronosyltransferase 1A1. [35]
Hyperforin DM2L3PE Investigative Hyperforin increases the expression of UDP-glucuronosyltransferase 1A1. [55]
Fibrates DMFNTMY Investigative Fibrates increases the expression of UDP-glucuronosyltransferase 1A1. [29]
Phloretin DMYA50U Investigative Phloretin decreases the activity of UDP-glucuronosyltransferase 1A1. [35]
Acacetin DMQOB0X Investigative Acacetin increases the expression of UDP-glucuronosyltransferase 1A1. [34]
AMENTOFLAVONE DMLRNV2 Investigative AMENTOFLAVONE decreases the activity of UDP-glucuronosyltransferase 1A1. [56]
pregnenolone-16alpha-carbonitrile DM0LW7G Investigative pregnenolone-16alpha-carbonitrile increases the expression of UDP-glucuronosyltransferase 1A1. [57]
Phlorizin DMNARGO Investigative Phlorizin decreases the activity of UDP-glucuronosyltransferase 1A1. [35]
GINKGOLIDE A DMKZJ7T Investigative GINKGOLIDE A increases the expression of UDP-glucuronosyltransferase 1A1. [58]
ROBINETIN DMASOWP Investigative ROBINETIN increases the expression of UDP-glucuronosyltransferase 1A1. [42]
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⏷ Show the Full List of 86 Drug(s)

References

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