Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTQ2XMO3)

DOT Name Aldo-keto reductase family 1 member C2 (AKR1C2)
Synonyms
EC 1.-.-.-; EC 1.1.1.112; EC 1.1.1.209; EC 1.1.1.53; EC 1.1.1.62; EC 1.3.1.20; 3-alpha-HSD3; Chlordecone reductase homolog HAKRD; Dihydrodiol dehydrogenase 2; DD-2; DD2; Dihydrodiol dehydrogenase/bile acid-binding protein; DD/BABP; Type III 3-alpha-hydroxysteroid dehydrogenase; EC 1.1.1.357
Gene Name AKR1C2
Related Disease
46,XY disorder of sex development due to testicular 17,20-desmolase deficiency ( )
UniProt ID
AK1C2_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
PDB ID
1IHI; 1J96; 1XJB; 2HDJ; 2IPJ; 4JQ1; 4JQ2; 4JQ3; 4JQ4; 4JQA; 4JTQ; 4JTR; 4L1W; 4L1X; 4XO6; 4XO7
EC Number
1.-.-.-; 1.1.1.112; 1.1.1.209; 1.1.1.357; 1.1.1.53; 1.1.1.62; 1.3.1.20
Pfam ID
PF00248
Sequence
MDSKYQCVKLNDGHFMPVLGFGTYAPAEVPKSKALEAVKLAIEAGFHHIDSAHVYNNEEQ
VGLAIRSKIADGSVKREDIFYTSKLWSNSHRPELVRPALERSLKNLQLDYVDLYLIHFPV
SVKPGEEVIPKDENGKILFDTVDLCATWEAMEKCKDAGLAKSIGVSNFNHRLLEMILNKP
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. Works in concert with the 5-alpha/5-beta-steroid reductases to convert steroid hormones into the 3-alpha/5-alpha and 3-alpha/5-beta-tetrahydrosteroids. Catalyzes the inactivation of the most potent androgen 5-alpha-dihydrotestosterone (5-alpha-DHT) to 5-alpha-androstane-3-alpha,17-beta-diol (3-alpha-diol). Also specifically able to produce 17beta-hydroxy-5alpha-androstan-3-one/5alphaDHT. May also reduce conjugated steroids such as 5alpha-dihydrotestosterone sulfate. Displays affinity for bile acids.
Tissue Specificity Expressed in fetal testes. Expressed in fetal and adult adrenal glands.
KEGG Pathway
Steroid hormone biosynthesis (hsa00140 )
Metabolic pathways (hsa01100 )
Chemical carcinogenesis - D. adducts (hsa05204 )
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 )
Synthesis of bile acids and bile salts via 7alpha-hydroxycholesterol (R-HSA-193368 )
BioCyc Pathway
MetaCyc:HS07754-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

1 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
46,XY disorder of sex development due to testicular 17,20-desmolase deficiency DISEZQMU Supportive Autosomal recessive [1]
------------------------------------------------------------------------------------
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Biotransformations of 6 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Progesterone DMUY35B Approved Aldo-keto reductase family 1 member C2 (AKR1C2) increases the reduction of Progesterone. [46]
Oxcarbazepine DM5PU6O Approved Aldo-keto reductase family 1 member C2 (AKR1C2) increases the reduction of Oxcarbazepine. [49]
ELTANOLONE DM38CIV Discontinued in Phase 3 Aldo-keto reductase family 1 member C2 (AKR1C2) increases the reduction of ELTANOLONE. [26]
Nitrobenzanthrone DMN6L70 Investigative Aldo-keto reductase family 1 member C2 (AKR1C2) increases the reduction of Nitrobenzanthrone. [51]
Acenaphthenol DMT3QYZ Investigative Aldo-keto reductase family 1 member C2 (AKR1C2) increases the oxidation of Acenaphthenol. [53]
tetrahydrodeoxycorticosterone DMF8M0W Investigative Aldo-keto reductase family 1 member C2 (AKR1C2) affects the oxidation of tetrahydrodeoxycorticosterone. [23]
------------------------------------------------------------------------------------
⏷ Show the Full List of 6 Drug(s)
This DOT Affected the Drug Response of 2 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Fluorouracil DMUM7HZ Approved Aldo-keto reductase family 1 member C2 (AKR1C2) affects the response to substance of Fluorouracil. [47]
Paclitaxel DMLB81S Approved Aldo-keto reductase family 1 member C2 (AKR1C2) increases the response to substance of Paclitaxel. [48]
------------------------------------------------------------------------------------
This DOT Affected the Regulation of Drug Effects of 3 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Dihydrotestosterone DM3S8XC Phase 4 Aldo-keto reductase family 1 member C2 (AKR1C2) increases the metabolism of Dihydrotestosterone. [50]
PGF2alpha DM4XAU7 Clinical trial Aldo-keto reductase family 1 member C2 (AKR1C2) increases the metabolism of PGF2alpha. [25]
Phenanthrene-9,10-dione DMG8KS9 Investigative Aldo-keto reductase family 1 member C2 (AKR1C2) increases the metabolism of Phenanthrene-9,10-dione. [52]
------------------------------------------------------------------------------------
2 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 Aldo-keto reductase family 1 member C2 (AKR1C2). [2]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the methylation of Aldo-keto reductase family 1 member C2 (AKR1C2). [38]
------------------------------------------------------------------------------------
88 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [3]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [4]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [5]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [6]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [7]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [8]
Arsenic DMTL2Y1 Approved Arsenic increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [9]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [10]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [11]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [12]
Vorinostat DMWMPD4 Approved Vorinostat increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [13]
Testosterone DM7HUNW Approved Testosterone decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [14]
Zoledronate DMIXC7G Approved Zoledronate decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [15]
Phenobarbital DMXZOCG Approved Phenobarbital increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [16]
Menadione DMSJDTY Approved Menadione increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [12]
Bortezomib DMNO38U Approved Bortezomib affects the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [17]
Azathioprine DMMZSXQ Approved Azathioprine increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [18]
Aspirin DM672AH Approved Aspirin decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Testosterone enanthate DMB6871 Approved Testosterone enanthate affects the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [20]
Sodium lauryl sulfate DMLJ634 Approved Sodium lauryl sulfate increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
Malathion DMXZ84M Approved Malathion increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [22]
Indomethacin DMSC4A7 Approved Indomethacin decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Cidofovir DMA13GD Approved Cidofovir affects the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [15]
Fenofibrate DMFKXDY Approved Fenofibrate increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [15]
Ifosfamide DMCT3I8 Approved Ifosfamide increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [15]
Clodronate DM9Y6X7 Approved Clodronate increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [15]
Sulindac DM2QHZU Approved Sulindac decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Ibuprofen DM8VCBE Approved Ibuprofen decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Liothyronine DM6IR3P Approved Liothyronine increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [24]
Vitamin C DMXJ7O8 Approved Vitamin C increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [6]
Ursodeoxycholic acid DMCUT21 Approved Ursodeoxycholic acid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Adefovir dipivoxil DMMAWY1 Approved Adefovir dipivoxil decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [15]
Chenodiol DMQ8JIK Approved Chenodiol decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [25]
Ampicillin DMHWE7P Approved Ampicillin decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [10]
Chlorambucil DMRKE63 Approved Chlorambucil decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [6]
Flurbiprofen DMGN4BY Approved Flurbiprofen decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Mefenamic acid DMK7HFI Approved Mefenamic acid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Naproxen DMZ5RGV Approved Naproxen decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Diazepam DM08E9O Approved Diazepam decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [26]
Salicyclic acid DM2F8XZ Approved Salicyclic acid increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
Benzbromarone DMC3YUA Approved Benzbromarone decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Dutasteride DMQ4TJK Approved Dutasteride increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [27]
Glibenclamide DM8JXPZ Approved Glibenclamide decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [28]
Flunitrazepam DMGR5Z3 Approved Flunitrazepam decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [26]
Flufenamic Acid DMC8VNH Approved Flufenamic Acid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Dydrogesterone DMAKIDV Approved Dydrogesterone decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [29]
Meclofenamic acid DM05FXR Approved Meclofenamic acid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Oestradiol valerate and dienogest DMZK0FQ Approved Oestradiol valerate and dienogest decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [29]
Glipizide DMZA5PQ Approved Glipizide decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [28]
Gliquidone DMB0EUX Approved Gliquidone decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [28]
Nitrazepam DMEGIQ6 Approved Nitrazepam decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [26]
Estazolam DMZGXUM Approved Estazolam decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [26]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [30]
SNDX-275 DMH7W9X Phase 3 SNDX-275 decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [31]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [32]
Tocopherol DMBIJZ6 Phase 2 Tocopherol increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [33]
DNCB DMDTVYC Phase 2 DNCB increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [6]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [34]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [35]
Eugenol DM7US1H Patented Eugenol increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [6]
T83193 DMHO29Y Patented T83193 increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
Benzylcinnamate DMD7Z3H Patented Benzylcinnamate increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
4-Hydroxybenzoicacid DM3WQNY Patented 4-Hydroxybenzoicacid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [36]
HEXESTROL DM9AGWQ Withdrawn from market HEXESTROL decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Zomepirac DM7APNJ Withdrawn from market Zomepirac decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
Phenolphthalein DM5SICT Withdrawn from market Phenolphthalein decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Celastrol DMWQIJX Preclinical Celastrol increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [37]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [39]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
Sulforaphane DMQY3L0 Investigative Sulforaphane increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [40]
chloropicrin DMSGBQA Investigative chloropicrin increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [41]
3R14S-OCHRATOXIN A DM2KEW6 Investigative 3R14S-OCHRATOXIN A decreases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [42]
OXYQUINOLINE DMZVS9Y Investigative OXYQUINOLINE increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [10]
cinnamaldehyde DMZDUXG Investigative cinnamaldehyde increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [43]
Lead acetate DML0GZ2 Investigative Lead acetate increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [44]
Linalool DMGZQ5P Investigative Linalool increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
DM9CEI5 decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Benzoquinone DMNBA0G Investigative Benzoquinone increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
NSC-1771 DMNXDGQ Investigative NSC-1771 increases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [45]
Caffeic acid phenethyl ester DMRJKIV Investigative Caffeic acid phenethyl ester decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [36]
citral DM53ZGY Investigative citral increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
Aminophenol DMEMCQ9 Investigative Aminophenol increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
18beta-Glycyrrhetic acid DMFMRN8 Investigative 18beta-Glycyrrhetic acid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [23]
Medazepam DMNKSX3 Investigative Medazepam decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [26]
1-Phenyl-propane-1,2-dione DM04SWY Investigative 1-Phenyl-propane-1,2-dione increases the expression of Aldo-keto reductase family 1 member C2 (AKR1C2). [21]
diphenylamine-2-carboxylic acid DMBV19T Investigative diphenylamine-2-carboxylic acid decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [19]
OCTYL_GALLATE DMXLGUS Investigative OCTYL_GALLATE decreases the activity of Aldo-keto reductase family 1 member C2 (AKR1C2). [36]
------------------------------------------------------------------------------------
⏷ Show the Full List of 88 Drug(s)

References

1 Why boys will be boys: two pathways of fetal testicular androgen biosynthesis are needed for male sexual differentiation. Am J Hum Genet. 2011 Aug 12;89(2):201-18. doi: 10.1016/j.ajhg.2011.06.009. Epub 2011 Jul 28.
2 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
3 Cyclosporine A--induced oxidative stress in human renal mesangial cells: a role for ERK 1/2 MAPK signaling. Toxicol Sci. 2012 Mar;126(1):101-13.
4 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
5 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
6 Oxidative stress mechanisms do not discriminate between genotoxic and nongenotoxic liver carcinogens. Chem Res Toxicol. 2015 Aug 17;28(8):1636-46.
7 Long-term estrogen exposure promotes carcinogen bioactivation, induces persistent changes in gene expression, and enhances the tumorigenicity of MCF-7 human breast cancer cells. Toxicol Appl Pharmacol. 2009 Nov 1;240(3):355-66.
8 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
9 Inorganic arsenic exposure promotes malignant progression by HDAC6-mediated down-regulation of HTRA1. J Appl Toxicol. 2023 Aug;43(8):1214-1224. doi: 10.1002/jat.4457. Epub 2023 Mar 11.
10 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
11 Aberrantly expressed genes in HaCaT keratinocytes chronically exposed to arsenic trioxide. Biomark Insights. 2011 Feb 8;6:7-16.
12 Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
13 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
14 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
15 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
16 Proteomic analysis of hepatic effects of phenobarbital in mice with humanized liver. Arch Toxicol. 2022 Oct;96(10):2739-2754. doi: 10.1007/s00204-022-03338-7. Epub 2022 Jul 26.
17 Proteasome inhibitors MG-132 and bortezomib induce AKR1C1, AKR1C3, AKR1B1, and AKR1B10 in human colon cancer cell lines SW-480 and HT-29. Chem Biol Interact. 2011 May 30;191(1-3):239-49.
18 A transcriptomics-based in vitro assay for predicting chemical genotoxicity in vivo. Carcinogenesis. 2012 Jul;33(7):1421-9.
19 Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3): role in breast cancer and inhibition by non-steroidal anti-inflammatory drug analogs. Chem Biol Interact. 2009 Mar 16;178(1-3):221-7.
20 Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
21 A new in vitro method for identifying chemical sensitizers combining peptide binding with ARE/EpRE-mediated gene expression in human skin cells. Cutan Ocul Toxicol. 2010 Sep;29(3):171-92.
22 Differential gene expression in normal human mammary epithelial cells treated with malathion monitored by DNA microarrays. Environ Health Perspect. 2005 Aug;113(8):1046-51.
23 Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone. Chem Biol Interact. 2003 Feb 1;143-144:503-13.
24 Thyroid hormone responsive genes in cultured human fibroblasts. J Clin Endocrinol Metab. 2005 Feb;90(2):936-43.
25 Relationship of human liver dihydrodiol dehydrogenases to hepatic bile-acid-binding protein and an oxidoreductase of human colon cells. Biochem J. 1996 Jan 15;313 ( Pt 2)(Pt 2):373-6.
26 Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5.
27 Dutasteride affects progesterone metabolizing enzyme activity/expression in human breast cell lines resulting in suppression of cell proliferation and detachment. J Steroid Biochem Mol Biol. 2006 Aug;100(4-5):129-40.
28 Initro inhibition of AKR1Cs by sulphonylureas and the structural basis. Chem Biol Interact. 2015 Oct 5;240:310-5.
29 Progestin effects on expression of AKR1C1-AKR1C3, SRD5A1 and PGR in the Z-12 endometriotic epithelial cell line. Chem Biol Interact. 2013 Feb 25;202(1-3):218-25.
30 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
31 Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
32 Integrated transcriptomic and metabolomic analyses to characterize the anti-cancer effects of (-)-epigallocatechin-3-gallate in human colon cancer cells. Toxicol Appl Pharmacol. 2020 Aug 15;401:115100. doi: 10.1016/j.taap.2020.115100. Epub 2020 Jun 6.
33 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
34 Altered gene expression patterns in MCF-7 cells induced by the urban dust particulate complex mixture standard reference material 1649a. Cancer Res. 2005 Feb 15;65(4):1251-8.
35 CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.
36 Initro CAPE inhibitory activity towards human AKR1C3 and the molecular basis. Chem Biol Interact. 2016 Jun 25;253:60-5.
37 Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators. Cancer Cell. 2006 Oct;10(4):321-30.
38 DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.
39 From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
40 Transcriptomic responses of cancerous and noncancerous human colon cells to sulforaphane and selenium. Chem Res Toxicol. 2014 Mar 17;27(3):377-86.
41 Molecular targets of chloropicrin in human airway epithelial cells. Toxicol In Vitro. 2017 Aug;42:247-254.
42 Ochratoxin a lowers mRNA levels of genes encoding for key proteins of liver cell metabolism. Cancer Genomics Proteomics. 2008 Nov-Dec;5(6):319-32.
43 Genes specifically modulated in sensitized skins allow the detection of sensitizers in a reconstructed human skin modelDevelopment of the SENS-IS assay. Toxicol In Vitro. 2015 Jun;29(4):787-802.
44 Analysis of lead toxicity in human cells. BMC Genomics. 2012 Jul 27;13:344.
45 The intra- and inter-laboratory reproducibility and predictivity of the KeratinoSens assay to predict skin sensitizers in vitro: results of a ring-study in five laboratories. Toxicol In Vitro. 2011 Apr;25(3):733-44.
46 Human types 1 and 3 3 alpha-hydroxysteroid dehydrogenases: differential lability and tissue distribution. J Clin Endocrinol Metab. 2001 Feb;86(2):841-6. doi: 10.1210/jcem.86.2.7216.
47 Gene expression profiling of 30 cancer cell lines predicts resistance towards 11 anticancer drugs at clinically achieved concentrations. Int J Cancer. 2006 Apr 1;118(7):1699-712. doi: 10.1002/ijc.21570.
48 cDNA microarray analysis of isogenic paclitaxel- and doxorubicin-resistant breast tumor cell lines reveals distinct drug-specific genetic signatures of resistance. Breast Cancer Res Treat. 2006 Mar;96(1):17-39. doi: 10.1007/s10549-005-9026-6. Epub 2005 Dec 2.
49 The role of carbonyl reducing enzymes in oxcarbazepine in vitro metabolism in man. Chem Biol Interact. 2014 Sep 5;220:241-7.
50 Human cytosolic 3alpha-hydroxysteroid dehydrogenases of the aldo-keto reductase superfamily display significant 3beta-hydroxysteroid dehydrogenase activity: implications for steroid hormone metabolism and action. J Biol Chem. 2004 Mar 12;279(11):10784-95. doi: 10.1074/jbc.M313308200. Epub 2003 Dec 12.
51 Role of Human Aldo-Keto Reductases in the Metabolic Activation of the Carcinogenic Air Pollutant 3-Nitrobenzanthrone. Chem Res Toxicol. 2018 Nov 19;31(11):1277-1288. doi: 10.1021/acs.chemrestox.8b00250. Epub 2018 Nov 8.
52 An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies. Biochem Pharmacol. 2008 Jan 15;75(2):484-93.
53 New enzymatic assay for the AKR1C enzymes. Chem Biol Interact. 2013 Feb 25;202(1-3):204-9.