Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTQKR4CM)

DOT Name Aldo-keto reductase family 1 member C1 (AKR1C1)
Synonyms
EC 1.1.1.-; EC 1.1.1.112; EC 1.1.1.209; EC 1.1.1.210; EC 1.1.1.357; EC 1.1.1.51; EC 1.1.1.53; EC 1.1.1.62; EC 1.3.1.20; 20-alpha-hydroxysteroid dehydrogenase; 20-alpha-HSD; EC 1.1.1.149; Chlordecone reductase homolog HAKRC; Dihydrodiol dehydrogenase 1; DD1; High-affinity hepatic bile acid-binding protein; HBAB
Gene Name AKR1C1
UniProt ID
AK1C1_HUMAN
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
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PDB ID
1MRQ; 3C3U; 3GUG; 3NTY; 4YVP; 6A7A; 6IJX
EC Number
1.1.1.-; 1.1.1.112; 1.1.1.149; 1.1.1.209; 1.1.1.210; 1.1.1.357; 1.1.1.51; 1.1.1.53; 1.1.1.62; 1.3.1.20
Pfam ID
PF00248
Sequence
MDSKYQCVKLNDGHFMPVLGFGTYAPAEVPKSKALEATKLAIEAGFRHIDSAHLYNNEEQ
VGLAIRSKIADGSVKREDIFYTSKLWCNSHRPELVRPALERSLKNLQLDYVDLYLIHFPV
SVKPGEEVIPKDENGKILFDTVDLCATWEAVEKCKDAGLAKSIGVSNFNRRQLEMILNKP
GLKYKPVCNQVECHPYFNQRKLLDFCKSKDIVLVAYSALGSHREEPWVDPNSPVLLEDPV
LCALAKKHKRTPALIALRYQLQRGVVVLAKSYNEQRIRQNVQVFEFQLTSEEMKAIDGLN
RNVRYLTLDIFAGPPNYPFSDEY
Function
Cytosolic aldo-keto reductase that catalyzes the NADH and NADPH-dependent reduction of ketosteroids to hydroxysteroids. Most probably acts as a reductase in vivo since the oxidase activity measured in vitro is inhibited by physiological concentrations of NADPH. Displays a broad positional specificity acting on positions 3, 17 and 20 of steroids and regulates the metabolism of hormones like estrogens and androgens. May also reduce conjugated steroids such as 5alpha-dihydrotestosterone sulfate. Displays affinity for bile acids.
Tissue Specificity Expressed in all tissues tested including liver, prostate, testis, adrenal gland, brain, uterus, mammary gland and keratinocytes. Highest levels found in liver, mammary gland and brain.
KEGG Pathway
Steroid hormone biosynthesis (hsa00140 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Metabolic pathways (hsa01100 )
Chemical carcinogenesis - reactive oxygen species (hsa05208 )
Reactome Pathway
Synthesis of bile acids and bile salts via 24-hydroxycholesterol (R-HSA-193775 )
Synthesis of bile acids and bile salts via 27-hydroxycholesterol (R-HSA-193807 )
Retinoid metabolism and transport (R-HSA-975634 )
Prednisone ADME (R-HSA-9757110 )
Synthesis of bile acids and bile salts via 7alpha-hydroxycholesterol (R-HSA-193368 )
BioCyc Pathway
MetaCyc:HS10741-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 3 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Temozolomide DMKECZD Approved Aldo-keto reductase family 1 member C1 (AKR1C1) affects the response to substance of Temozolomide. [58]
Arsenic trioxide DM61TA4 Approved Aldo-keto reductase family 1 member C1 (AKR1C1) decreases the response to substance of Arsenic trioxide. [59]
DTI-015 DMXZRW0 Approved Aldo-keto reductase family 1 member C1 (AKR1C1) affects the response to substance of DTI-015. [58]
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This DOT Affected the Regulation of Drug Effects of 4 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Tofacitinib DMBS370 Approved Aldo-keto reductase family 1 member C1 (AKR1C1) increases the metabolism of Tofacitinib. [60]
Phenanthrene-9,10-dione DMG8KS9 Investigative Aldo-keto reductase family 1 member C1 (AKR1C1) increases the metabolism of Phenanthrene-9,10-dione. [63]
Acenaphthenol DMT3QYZ Investigative Aldo-keto reductase family 1 member C1 (AKR1C1) increases the metabolism of Acenaphthenol. [64]
Prostaglandin G2 DME74SP Investigative Aldo-keto reductase family 1 member C1 (AKR1C1) increases the metabolism of Prostaglandin G2. [65]
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This DOT Affected the Biotransformations of 4 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Oxcarbazepine DM5PU6O Approved Aldo-keto reductase family 1 member C1 (AKR1C1) increases the reduction of Oxcarbazepine. [61]
ELTANOLONE DM38CIV Discontinued in Phase 3 Aldo-keto reductase family 1 member C1 (AKR1C1) increases the reduction of ELTANOLONE. [32]
Nitrobenzanthrone DMN6L70 Investigative Aldo-keto reductase family 1 member C1 (AKR1C1) increases the reduction of Nitrobenzanthrone. [62]
tetrahydrodeoxycorticosterone DMF8M0W Investigative Aldo-keto reductase family 1 member C1 (AKR1C1) affects the oxidation of tetrahydrodeoxycorticosterone. [24]
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95 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 Aldo-keto reductase family 1 member C1 (AKR1C1). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [2]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [3]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [4]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [5]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [6]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [7]
Arsenic DMTL2Y1 Approved Arsenic increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [8]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [9]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [10]
Vorinostat DMWMPD4 Approved Vorinostat increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [11]
Testosterone DM7HUNW Approved Testosterone increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [12]
Triclosan DMZUR4N Approved Triclosan decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [13]
Progesterone DMUY35B Approved Progesterone decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [14]
Menadione DMSJDTY Approved Menadione affects the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [15]
Fluorouracil DMUM7HZ Approved Fluorouracil affects the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [16]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [17]
Bortezomib DMNO38U Approved Bortezomib increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [18]
Azathioprine DMMZSXQ Approved Azathioprine increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [19]
Aspirin DM672AH Approved Aspirin decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Testosterone enanthate DMB6871 Approved Testosterone enanthate affects the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [21]
Sodium lauryl sulfate DMLJ634 Approved Sodium lauryl sulfate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
Malathion DMXZ84M Approved Malathion increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [23]
Indomethacin DMSC4A7 Approved Indomethacin decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
Simvastatin DM30SGU Approved Simvastatin increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [25]
Sulindac DM2QHZU Approved Sulindac decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Ibuprofen DM8VCBE Approved Ibuprofen decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Liothyronine DM6IR3P Approved Liothyronine increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [26]
Ursodeoxycholic acid DMCUT21 Approved Ursodeoxycholic acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
Sodium phenylbutyrate DMXLBCQ Approved Sodium phenylbutyrate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [27]
Bexarotene DMOBIKY Approved Bexarotene increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [28]
Chenodiol DMQ8JIK Approved Chenodiol decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [29]
Cholecalciferol DMGU74E Approved Cholecalciferol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [30]
Benzoic acid DMKB9FI Approved Benzoic acid increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
Gamolenic acid DMQN30Z Approved Gamolenic acid increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [31]
Flurbiprofen DMGN4BY Approved Flurbiprofen decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Mefenamic acid DMK7HFI Approved Mefenamic acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Naproxen DMZ5RGV Approved Naproxen decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Ethacrynic acid DM60QMR Approved Ethacrynic acid increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [9]
Diazepam DM08E9O Approved Diazepam decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [32]
Salicyclic acid DM2F8XZ Approved Salicyclic acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Dutasteride DMQ4TJK Approved Dutasteride increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [33]
Glibenclamide DM8JXPZ Approved Glibenclamide decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [34]
Glimepiride DM5FSJA Approved Glimepiride decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [34]
Flunitrazepam DMGR5Z3 Approved Flunitrazepam decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [32]
Norethindrone DMTY169 Approved Norethindrone decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [35]
Flufenamic Acid DMC8VNH Approved Flufenamic Acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
Dydrogesterone DMAKIDV Approved Dydrogesterone decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [14]
Meclofenamic acid DM05FXR Approved Meclofenamic acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Oestradiol valerate and dienogest DMZK0FQ Approved Oestradiol valerate and dienogest decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [14]
Glipizide DMZA5PQ Approved Glipizide decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [34]
Gliquidone DMB0EUX Approved Gliquidone decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [34]
Nitrazepam DMEGIQ6 Approved Nitrazepam decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [32]
Estazolam DMZGXUM Approved Estazolam decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [32]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [36]
SNDX-275 DMH7W9X Phase 3 SNDX-275 decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [37]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [38]
Fenretinide DMRD5SP Phase 3 Fenretinide increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [39]
Seocalcitol DMKL9QO Phase 3 Seocalcitol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [10]
Amiodarone DMUTEX3 Phase 2/3 Trial Amiodarone increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [40]
DNCB DMDTVYC Phase 2 DNCB increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
GSK2110183 DMZHB37 Phase 2 GSK2110183 increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [41]
Disulfiram DMCL2OK Phase 2 Trial Disulfiram increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [42]
Leflunomide DMR8ONJ Phase 1 Trial Leflunomide decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [43]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [44]
Eugenol DM7US1H Patented Eugenol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
4-Hydroxybenzoicacid DM3WQNY Patented 4-Hydroxybenzoicacid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [45]
HEXESTROL DM9AGWQ Withdrawn from market HEXESTROL decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
Zomepirac DM7APNJ Withdrawn from market Zomepirac decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
Phenolphthalein DM5SICT Withdrawn from market Phenolphthalein decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
MG-132 DMKA2YS Preclinical MG-132 increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [18]
Celastrol DMWQIJX Preclinical Celastrol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [46]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [48]
Milchsaure DM462BT Investigative Milchsaure increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
Sulforaphane DMQY3L0 Investigative Sulforaphane increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [49]
3R14S-OCHRATOXIN A DM2KEW6 Investigative 3R14S-OCHRATOXIN A decreases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [50]
geraniol DMS3CBD Investigative geraniol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [51]
OXYQUINOLINE DMZVS9Y Investigative OXYQUINOLINE increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [52]
Resorcinol DMM37C0 Investigative Resorcinol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [51]
cinnamaldehyde DMZDUXG Investigative cinnamaldehyde increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [53]
crotylaldehyde DMTWRQI Investigative crotylaldehyde increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [54]
Dibutyl phthalate DMEDGKO Investigative Dibutyl phthalate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [55]
Aminohippuric acid DMUN54G Investigative Aminohippuric acid affects the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [56]
Lead acetate DML0GZ2 Investigative Lead acetate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [57]
2-tert-butylbenzene-1,4-diol DMNXI1E Investigative 2-tert-butylbenzene-1,4-diol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [51]
DM9CEI5 decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
Farnesol DMV2X1B Investigative Farnesol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [51]
methyl salicylate DMKCG8H Investigative methyl salicylate increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
2-Propanol, Isopropanol DML5O0H Investigative 2-Propanol, Isopropanol increases the expression of Aldo-keto reductase family 1 member C1 (AKR1C1). [22]
Caffeic acid phenethyl ester DMRJKIV Investigative Caffeic acid phenethyl ester decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [45]
18beta-Glycyrrhetic acid DMFMRN8 Investigative 18beta-Glycyrrhetic acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [24]
Medazepam DMNKSX3 Investigative Medazepam decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [32]
diphenylamine-2-carboxylic acid DMBV19T Investigative diphenylamine-2-carboxylic acid decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [20]
OCTYL_GALLATE DMXLGUS Investigative OCTYL_GALLATE decreases the activity of Aldo-keto reductase family 1 member C1 (AKR1C1). [45]
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⏷ Show the Full List of 95 Drug(s)
1 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of Aldo-keto reductase family 1 member C1 (AKR1C1). [47]
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References

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