General Information of Drug (ID: DM8KSQH)

Drug Name
Phenoxybenzamine Drug Info
Synonyms
Bensylyt; Bensylyte; Benzylyt; Dibenylene; Dibenylin; Dibenyline; Dibenziran; Dibenzylene; Dibenzylin; Dibenzyran; Fenossibenzamina; Fenoxibenzamina; Phenoxybenzaminum; Bensylyt NEN; Fenossibenzamina [DCIT]; POB HCl; Phenoxybenzamine Hcl; A 688; Dibenzyline (TN); Fenoxibenzamina [INN-Spanish]; Phenoxybenzamine (INN);Phenoxybenzamine [INN:BAN]; Phenoxybenzaminum [INN-Latin]; N-Phenoxyisopropyl-N-benzyl-beta-chloroethylamine; Benzyl(2-chloroethyl)-(1-methyl-2-phenoxyethyl)amine; N-(2-Chloroethyl)-N-(1-methyl-2-phenoxyethyl)benzenemethanamine; N-(2-Chloroethyl)-N-(1-methyl-2-phenoxyethyl)benzylamine; N-benzyl-N-(2-chloroethyl)-1-phenoxypropan-2-amine; N-(2-chloroethyl)-N-(phenylmethyl)-1-(phenyloxy)propan-2-amine; 2-(N-Benzyl-2-chloroethylamino)-1-phenoxypropane; 688A
Indication
Disease Entry ICD 11 Status REF
Malignant essential hypertension BA00 Approved [1]
Pheochromocytoma 5A75 Approved [2]
Therapeutic Class
Antihypertensive Agents
Cross-matching ID
PubChem CID
4768
ChEBI ID
CHEBI:8077
CAS Number
CAS 59-96-1
TTD Drug ID
DM8KSQH
VARIDT Drug ID
DR00696
ACDINA Drug ID
D00526

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [11]
Haloperidol DM96SE0 Delirium Approved [12]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [13]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [14]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [15]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [16]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [17]
Pimozide DMW83TP Schizophrenia 6A20 Approved [18]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [19]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [21]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [22]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [23]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [24]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [26]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [27]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [28]
Propranolol DM79NTF Angina pectoris BA40 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [30]
Trospium chloride DM32XZT Discovery agent N.A. Approved [31]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [32]
Lamivudine DMI347A Chronic HBV infection 1E51.0Z Approved [33]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [34]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [35]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [37]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [34]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [38]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [30]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [39]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [39]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [40]
Lamivudine DMI347A Chronic HBV infection 1E51.0Z Approved [33]
Famotidine DMRL3AB Gastric ulcer DA60 Approved [40]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [34]
Trospium chloride DM32XZT Discovery agent N.A. Approved [31]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [41]
Indomethacin DMSC4A7 Bursitis Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Epinephrine DM3KJBC Acute asthma CA23 Approved [42]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [42]
Norepinephrine DMOUC09 Alopecia ED70 Approved [42]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [43]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [38]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [41]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [45]
Mifepristone DMGZQEF Cushing disease 5A70 Approved [46]
Sodium lauryl sulfate DMLJ634 Constipation DD91.1 Approved [47]
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Drug(s) Affected By Proepiregulin (EREG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [48]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [7]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [49]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [7]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [7]
Methotrexate DM2TEOL Anterior urethra cancer Approved [50]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [51]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [52]
Penbutolol DM4ES8F Hypertension BA00-BA04 Approved [7]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [53]
Vidarabine DM0N85H Hepatosplenic T-cell lymphoma Approved [53]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [54]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [55]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [56]
Etidronic acid DM1XHYJ Bone Paget disease Approved [53]
Tiaprofenic acid DM23D7J Osteoarthritis FA00-FA05 Approved [53]
Bromperidol DM24XYQ Schizophrenia 6A20 Approved [53]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [57]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [58]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [59]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [60]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [7]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [7]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [7]
Methotrexate DM2TEOL Anterior urethra cancer Approved [61]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [7]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [62]
Methylprednisolone DM4BDON Acute adrenal insufficiency Approved [61]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [63]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [64]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [65]
Methotrexate DM2TEOL Anterior urethra cancer Approved [66]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [67]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [5]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [35]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y Approved [68]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [69]
Verapamil DMA7PEW Angina pectoris BA40 Approved [70]
Methysergide DM1EF73 Migraine 8A80 Approved [9]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [71]
Methotrexate DM2TEOL Anterior urethra cancer Approved [72]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [9]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [73]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [74]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [75]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [76]
SPI-1005 DM6XFHS Reperfusion injury ND56.Z Approved [6]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [6]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [77]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [78]
Ceftazidime DM41GRA Bacteremia 1A73 Approved [6]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [6]
Ethacrynic acid DM60QMR Edema MG29 Approved [6]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [6]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-24 (IL24)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [79]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [7]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [80]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [7]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [7]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [81]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [51]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [82]
Penbutolol DM4ES8F Hypertension BA00-BA04 Approved [7]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [82]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Metallothionein-1M (MT1M)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [63]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [5]
Quercetin DM3NC4M Obesity 5B81 Approved [44]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [83]
Leflunomide DMR8ONJ Arthritis FA20 Approved [84]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [38]
Disulfiram DMCL2OK Alcohol dependence 6C40.2 Approved [5]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [85]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [86]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [87]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Antagonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cyclic AMP-dependent transcription factor ATF-3 (ATF3) OTC1UOHP ATF3_HUMAN Gene/Protein Processing [5]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Gene/Protein Processing [6]
Hepatocyte growth factor receptor (MET) OT7K55MU MET_HUMAN Gene/Protein Processing [7]
Interleukin-24 (IL24) OT4VUWH1 IL24_HUMAN Gene/Protein Processing [7]
Metallothionein-1M (MT1M) OTVT8PLU MT1M_HUMAN Gene/Protein Processing [5]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Gene/Protein Processing [8]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Gene/Protein Processing [9]
Proepiregulin (EREG) OTRM4NQY EREG_HUMAN Gene/Protein Processing [7]
Solute carrier family 22 member 1 (SLC22A1) OT7817I4 S22A1_HUMAN Gene/Protein Processing [10]
Solute carrier family 22 member 2 (SLC22A2) OTGFK1AL S22A2_HUMAN Gene/Protein Processing [10]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Phenoxybenzamine FDA Label
3 Catecholamine-secreting neuroblastoma in a 4-month-old infant: perioperative management. J Clin Anesth. 2009 Feb;21(1):54-6.
4 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
5 Identification of novel activators of the metal responsive transcription factor (MTF-1) using a gene expression biomarker in a microarray compendium. Metallomics. 2020 Sep 23;12(9):1400-1415. doi: 10.1039/d0mt00071j.
6 A Gene Expression Biomarker Predicts Heat Shock Factor 1 Activation in a Gene Expression Compendium. Chem Res Toxicol. 2021 Jul 19;34(7):1721-1737. doi: 10.1021/acs.chemrestox.0c00510. Epub 2021 Jun 25.
7 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
8 Identification of novel agonists by high-throughput screening and molecular modelling of human constitutive androstane receptor isoform 3. Arch Toxicol. 2019 Aug;93(8):2247-2264. doi: 10.1007/s00204-019-02495-6. Epub 2019 Jul 16.
9 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
10 Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36.
11 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
12 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
13 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
14 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
15 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
16 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3639).
17 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
18 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
19 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
20 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
21 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
22 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
23 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
24 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
25 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
26 Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma
27 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
28 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
29 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
30 Involvement of aryl hydrocarbon receptor in the cytotoxicity of corannulene and its derivatives. Toxicol Lett. 2020 Mar 15;321:114-121. doi: 10.1016/j.toxlet.2019.12.012. Epub 2019 Dec 9.
31 Expression of drug transporters and drug metabolizing enzymes in the bladder urothelium in man and affinity of the bladder spasmolytic trospium chloride to transporters likely involved in its pharmacokinetics. Mol Pharm. 2015 Jan 5;12(1):171-8.
32 Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). J Pharmacol Exp Ther. 2005 Dec;315(3):1288-97.
33 Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3. J Pharmacol Exp Ther. 2009 Apr;329(1):252-61. doi: 10.1124/jpet.108.146225. Epub 2009 Jan 13.
34 Interactions of human organic anion transporters and human organic cation transporters with nonsteroidal anti-inflammatory drugs. J Pharmacol Exp Ther. 2002 Nov;303(2):534-9.
35 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
36 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
37 The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for ("squelching") SRC-1 coactivator. Br J Pharmacol. 2016 May;173(10):1703-15. doi: 10.1111/bph.13472. Epub 2016 Apr 8.
38 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
39 Ameliorative effects of SLC22A2 gene polymorphism 808 G/T and cimetidine on cisplatin-induced nephrotoxicity in Chinese cancer patients. Food Chem Toxicol. 2012 Jul;50(7):2289-93. doi: 10.1016/j.fct.2012.03.077. Epub 2012 Apr 16.
40 A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther. 2005 Oct;315(1):337-45.
41 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
42 Selective transport of monoamine neurotransmitters by human plasma membrane monoamine transporter and organic cation transporter 3. J Pharmacol Exp Ther. 2010 Dec;335(3):743-53. doi: 10.1124/jpet.110.170142. Epub 2010 Sep 21.
43 Time series analysis of oxidative stress response patterns in HepG2: a toxicogenomics approach. Toxicology. 2013 Apr 5;306:24-34.
44 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.
45 LSD1 activates a lethal prostate cancer gene network independently of its demethylase function. Proc Natl Acad Sci U S A. 2018 May 1;115(18):E4179-E4188.
46 Mifepristone induced progesterone withdrawal reveals novel regulatory pathways in human endometrium. Mol Hum Reprod. 2007 Sep;13(9):641-54.
47 CXCL14 downregulation in human keratinocytes is a potential biomarker for a novel in vitro skin sensitization test. Toxicol Appl Pharmacol. 2020 Jan 1;386:114828. doi: 10.1016/j.taap.2019.114828. Epub 2019 Nov 14.
48 Cannabidiol-induced transcriptomic changes and cellular senescence in human Sertoli cells. Toxicol Sci. 2023 Feb 17;191(2):227-238. doi: 10.1093/toxsci/kfac131.
49 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
50 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
51 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
52 Retinoid-induced epidermal hyperplasia is mediated by epidermal growth factor receptor activation via specific induction of its ligands heparin-binding EGF and amphiregulin in human skin in vivo. J Invest Dermatol. 2006 Apr;126(4):732-9. doi: 10.1038/sj.jid.5700202.
53 Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. Toxicol Lett. 2015 Jan 5;232(1):193-202. doi: 10.1016/j.toxlet.2014.10.009. Epub 2014 Oct 16.
54 Induction of PXR-mediated metabolism by beta-carotene. Biochim Biophys Acta. 2005 May 30;1740(2):162-9. doi: 10.1016/j.bbadis.2004.11.013. Epub 2004 Dec 8.
55 Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR). Toxicol Appl Pharmacol. 2005 Dec 1;209(2):123-33. doi: 10.1016/j.taap.2005.03.015.
56 Identification and validation of novel human pregnane X receptor activators among prescribed drugs via ligand-based virtual screening. Drug Metab Dispos. 2011 Feb;39(2):337-44. doi: 10.1124/dmd.110.035808. Epub 2010 Nov 10.
57 Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9.
58 Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of pregnane X (PXR) receptor. Toxicol Lett. 2017 Jan 4;265:86-96.
59 ROS-dependent DNA damage contributes to crizotinib-induced hepatotoxicity via the apoptotic pathway. Toxicol Appl Pharmacol. 2019 Nov 15;383:114768. doi: 10.1016/j.taap.2019.114768. Epub 2019 Oct 19.
60 Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. Mol Cancer Ther. 2012 Jul;11(7):1557-64. doi: 10.1158/1535-7163.MCT-11-0934. Epub 2012 Jun 22.
61 Antirheumatic drug response signatures in human chondrocytes: potential molecular targets to stimulate cartilage regeneration. Arthritis Res Ther. 2009;11(1):R15.
62 All-trans retinoic acid inhibits the cell proliferation but enhances the cell invasion through up-regulation of c-met in pancreatic cancer cells. Cancer Lett. 2005 Jun 28;224(2):303-10. doi: 10.1016/j.canlet.2004.10.016. Epub 2004 Dec 8.
63 Inhibiting Heat Shock Proteins Can Potentiate the Cytotoxic Effect of Cannabidiol in Human Glioma Cells. Anticancer Res. 2015 Nov;35(11):5827-37.
64 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.
65 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
66 Development and validation of the TGx-HDACi transcriptomic biomarker to detect histone deacetylase inhibitors in human TK6 cells. Arch Toxicol. 2021 May;95(5):1631-1645. doi: 10.1007/s00204-021-03014-2. Epub 2021 Mar 26.
67 Simvastatin inactivates beta1-integrin and extracellular signal-related kinase signaling and inhibits cell proliferation in head and neck squamous cell carcinoma cells. Cancer Sci. 2007 Jun;98(6):890-9.
68 Motexafin gadolinium and zinc induce oxidative stress responses and apoptosis in B-cell lymphoma lines. Cancer Res. 2005 Dec 15;65(24):11676-88.
69 [Reversal effect of MDR1 and MDR3 gene silencing on resistance of A2780/taxol cells to paclitaxel]. Zhonghua Fu Chan Ke Za Zhi. 2007 Jun;42(6):412-6.
70 8-Methoxypsoralen disrupts MDR3-mediated phospholipids efflux and bile acid homeostasis and its relevance to hepatotoxicity. Toxicology. 2017 Jul 1;386:40-48. doi: 10.1016/j.tox.2017.05.011. Epub 2017 May 24.
71 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
72 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
73 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
74 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
75 Evaluation of gene induction of drug-metabolizing enzymes and transporters in primary culture of human hepatocytes using high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi. 2002 May;122(5):339-61.
76 NRF2 transcriptionally activates the heat shock factor 1 promoter under oxidative stress and affects survival and migration potential of MCF7 cells. J Biol Chem. 2018 Dec 14;293(50):19303-19316. doi: 10.1074/jbc.RA118.003376. Epub 2018 Oct 11.
77 Non-steroidal anti-inflammatory drugs inhibit the expression of cytokines and induce HSP70 in human monocytes. Cytokine. 1999 May;11(5):347-58. doi: 10.1006/cyto.1998.0437.
78 Simvastatin induces heat shock factor 1 in vascular endothelial cells. Atherosclerosis. 2006 Oct;188(2):265-73. doi: 10.1016/j.atherosclerosis.2005.10.045. Epub 2005 Dec 20.
79 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
80 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
81 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
82 Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitro. J Invest Dermatol. 2005 Jul;125(1):143-53.
83 Global effects of inorganic arsenic on gene expression profile in human macrophages. Mol Immunol. 2009 Feb;46(4):649-56.
84 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
85 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.
86 Identification of mechanisms of action of bisphenol a-induced human preadipocyte differentiation by transcriptional profiling. Obesity (Silver Spring). 2014 Nov;22(11):2333-43.
87 Capturing time-dependent activation of genes and stress-response pathways using transcriptomics in iPSC-derived renal proximal tubule cells. Cell Biol Toxicol. 2023 Aug;39(4):1773-1793. doi: 10.1007/s10565-022-09783-5. Epub 2022 Dec 31.