Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM2L3PE)

Drug Name
Hyperforin Drug Info
Synonyms
hyperforin; 11079-53-1; hyperforine; hiperforina; UNII-RM741E34FP; CHEBI:5834; RM741E34FP; CHEMBL1237210; (1R,5S,6R,7S)-4-hydroxy-6-methyl-1,3,7-tris(3-methylbut-2-en-1-yl)-6-(4-methylpent-3-en-1-yl)-5-(2-methylpropanoyl)bicyclo[3.3.1]non-3-ene-2,9-dione; (1R,5S,6R,7S)-4-hydroxy-5-isobutyryl-6-methyl-1,3,7-tris(3-methylbut-2-en-1-yl)-6-(4-methylpent-3-en-1-yl)bicyclo[3.3.1]non-3-ene-2,9-dione; HSDB 7646; (+)-Hyperforin; Spectrum5_002025; SCHEMBL98723; CHEMBL501711; GTPL2764; SCHEMBL15557965; Hyperforin, &gt
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
441298
ChEBI ID
CHEMBL5834
CAS Number
CAS 11079-53-1
TTD Drug ID
DM2L3PE
VARIDT Drug ID
DR00582

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Arachidonate 5-lipoxygenase (5-LOX)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zileuton DMVRIC2 Allergic asthma CA23.0 Approved [9]
Diethylcarbamazine DM1TJ8F Elephantiasis Approved [10]
Silymarin DMXBYQR N. A. N. A. Phase 4 [11]
3,4-Dihydroxycinnamic Acid DMVZL26 Thrombocytopenia 3B64 Phase 4 [12]
Avastin+/-Tarceva DMA86FL Non-small-cell lung cancer 2C25.Y Phase 3 [13]
ABT-761 DM3FIC2 Asthma CA23 Phase 3 [14]
Tenidap DMHQRYE Rheumatoid arthritis FA20 Phase 3 [15]
FPL-62064 DMGF8MZ Inflammation 1A00-CA43.1 Phase 3 [16]
Flobufen DMPSG4D Rheumatoid arthritis FA20 Phase 3 [17]
Darbufelone DMYVKM5 Asthma CA23 Phase 2/3 [18]
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Drug(s) Targeting Prostaglandin G/H synthase 1 (COX-1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Salicyclic acid DM2F8XZ Acne vulgaris ED80 Approved [19]
Naproxen DMZ5RGV Bursitis Approved [20]
Mesalazine DMOL5IU Diverticulitis Approved [21]
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Hypertriglyceridemia 5C80.1 Approved [22]
Bromfenac DMKB79O Pain MG30-MG3Z Approved [23]
Aminosalicylic Acid DMENSL5 Crohn disease DD70 Approved [24]
Flufenamic Acid DMC8VNH Dysmenorrhea GA34.3 Approved [25]
Piroxicam DMTK234 Osteoarthritis FA00-FA05 Approved [24]
Suprofen DMKXJZ7 Miosis LA11.62 Approved [26]
Gamma-Homolinolenic acid DMSXKYG Malnutrition 5B50-5B71 Approved [27]
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Drug(s) Targeting Pregnane X receptor (NR1I2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
WAY-214950 DM8ODI7 Discovery agent N.A. Investigative [28]
3-keto-lithocholic acid DM5LUED Discovery agent N.A. Investigative [29]
pregnenolone-16alpha-carbonitrile DM0LW7G Discovery agent N.A. Investigative [30]
trihydroxycholestane DMSP56N Discovery agent N.A. Investigative [31]
schisandrin A DMWQ480 Discovery agent N.A. Investigative [32]
Drug(s) Affected By 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (CYP24A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [33]
Calcidiol DMN4CV5 Hypophosphatemia Approved [34]
Calcipotriol DM03CP7 Psoriasis EA90 Approved [35]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [36]
Quercetin DM3NC4M Obesity 5B81 Approved [37]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [38]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [4]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [39]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [40]
Testosterone DM7HUNW Hot flushes GA30 Approved [41]
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Drug(s) Affected By ATP-dependent translocase ABCB1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [42]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [43]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [44]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [45]
Cepharanthine DM9Y5JB N. A. N. A. Approved [46]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [47]
Clozapine DMFC71L Schizophrenia 6A20 Approved [48]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [49]
Trifluoperazine DMKBYWI Anxiety Approved [50]
Olanzapine DMPFN6Y Bipolar depression Approved [48]
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Drug(s) Affected By 5-aminolevulinate synthase, non-specific, mitochondrial (ALAS1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Selenium DM25CGV N. A. N. A. Approved [51]
Quercetin DM3NC4M Obesity 5B81 Approved [37]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [52]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [53]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [5]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [54]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [55]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [56]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [57]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [58]
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Drug(s) Affected By Solute carrier family 22 member 1 (SLC22A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenoxybenzamine DM8KSQH Malignant essential hypertension BA00 Approved [59]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [60]
Trospium chloride DM32XZT Discovery agent N.A. Approved [61]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [62]
Lamivudine DMI347A Chronic HBV infection 1E51.0Z Approved [63]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [64]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [58]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [65]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [66]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [64]
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Drug(s) Affected By CASP8 and FADD-like apoptosis regulator (CFLAR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [67]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [68]
Methotrexate DM2TEOL Anterior urethra cancer Approved [69]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [70]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [71]
Quercetin DM3NC4M Obesity 5B81 Approved [72]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [73]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [74]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [75]
Ethacrynic acid DM60QMR Edema MG29 Approved [76]
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Drug(s) Affected By Interleukin-8 (CXCL8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [77]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [78]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [79]
Pantothenic acid DM091H2 Vitamin deficiency 5B55-5B71 Approved [80]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [81]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [82]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [83]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [84]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [85]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [83]
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Drug(s) Affected By Tumor necrosis factor receptor superfamily member 6 (FAS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [67]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [86]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [87]
Methotrexate DM2TEOL Anterior urethra cancer Approved [88]
Epinephrine DM3KJBC Acute asthma CA23 Approved [89]
Quercetin DM3NC4M Obesity 5B81 Approved [90]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [91]
Fructose DM43AN2 Vomiting MD90 Approved [92]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [67]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [93]
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Drug(s) Affected By Mitogen-activated protein kinase 3 (MAPK3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [94]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [95]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [96]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [97]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [98]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [99]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [100]
Gefitinib DM15F0X Colon adenocarcinoma Approved [101]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [102]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [103]
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Drug(s) Affected By Mitogen-activated protein kinase 1 (MAPK1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [104]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [95]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [105]
Paclitaxel DMLB81S Breast carcinoma Approved [106]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [107]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [94]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [108]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [109]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [97]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [98]
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Drug(s) Affected By Tumor necrosis factor ligand superfamily member 6 (FASLG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [110]
Gefitinib DM15F0X Colon adenocarcinoma Approved [111]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [112]
Epinephrine DM3KJBC Acute asthma CA23 Approved [89]
Quercetin DM3NC4M Obesity 5B81 Approved [113]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [114]
Fructose DM43AN2 Vomiting MD90 Approved [92]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [115]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [116]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [75]
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Drug(s) Affected By Cytochrome c (CYCS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [109]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [117]
Gefitinib DM15F0X Colon adenocarcinoma Approved [118]
Leuprorelin acetate DM15HAT Prostate cancer 2C82.0 Approved [119]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [120]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [121]
Methotrexate DM2TEOL Anterior urethra cancer Approved [122]
Quercetin DM3NC4M Obesity 5B81 Approved [37]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [123]
Pefloxacin DM49IGF Gonococcal urethritis 1A70.0Y Approved [124]
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Drug(s) Affected By Bcl-2 homologous antagonist/killer (BAK1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [125]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [126]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [127]
Methotrexate DM2TEOL Anterior urethra cancer Approved [128]
Quercetin DM3NC4M Obesity 5B81 Approved [129]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [130]
Levamisole DM5EN79 Parasitic infection 1D0Y-1G2Z Approved [131]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [132]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [133]
Promethazine DM6I5GR Hyperemesis gravidarum Approved [134]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Arachidonate 5-lipoxygenase (5-LOX) TT2J34L LOX5_HUMAN Inhibitor [2]
Pregnane X receptor (NR1I2) TT7LCTF NR1I2_HUMAN Binder [3]
Prostaglandin G/H synthase 1 (COX-1) TT8NGED PGH1_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (CYP24A1) OTG2T749 CP24A_HUMAN Gene/Protein Processing [4]
5-aminolevulinate synthase, non-specific, mitochondrial (ALAS1) OTQY6ZSF HEM1_HUMAN Gene/Protein Processing [5]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [5]
Bcl-2 homologous antagonist/killer (BAK1) OTDP6ILW BAK_HUMAN Gene/Protein Processing [6]
CASP8 and FADD-like apoptosis regulator (CFLAR) OTX14BAS CFLAR_HUMAN Gene/Protein Processing [6]
Cytochrome c (CYCS) OTBFALJD CYC_HUMAN Gene/Protein Processing [7]
E3 ubiquitin-protein ligase XIAP OT24GP9B XIAP_HUMAN Gene/Protein Processing [6]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Gene/Protein Processing [8]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [6]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [6]

References

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2 Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase. Biochem Pharmacol. 2002 Dec 15;64(12):1767-75.
3 Pregnane X receptor (PXR) regulates P-glycoprotein at the blood-brain barrier: functional similarities between pig and human PXR. J Pharmacol Exp Ther. 2009 Apr;329(1):141-9.
4 Possible involvement of pregnane X receptor-enhanced CYP24 expression in drug-induced osteomalacia. J Clin Invest. 2005 Jan;115(1):177-86.
5 No activation of human pregnane X receptor by hyperforin-related phloroglucinols. J Pharmacol Exp Ther. 2014 Mar;348(3):393-400.
6 Hyperforin induces apoptosis through extrinsic/intrinsic pathways and inhibits EGFR/ERK/NF-B-mediated anti-apoptotic potential in glioblastoma. Environ Toxicol. 2020 Oct;35(10):1058-1069. doi: 10.1002/tox.22942. Epub 2020 Jun 2.
7 Neuroprotective role of hyperforin on aluminum maltolate-induced oxidative damage and apoptosis in PC12 cells and SH-SY5Y cells. Chem Biol Interact. 2019 Feb 1;299:15-26. doi: 10.1016/j.cbi.2018.11.016. Epub 2018 Nov 24.
8 Hyperforin, the active component of St. John's wort, induces IL-8 expression in human intestinal epithelial cells via a MAPK-dependent, NF-kappaB-independent pathway. J Clin Immunol. 2004 Nov;24(6):623-36. doi: 10.1007/s10875-004-6248-z.
9 5-lipoxygenase inhibitor zileuton attenuates ischemic brain damage: involvement of matrix metalloproteinase 9. Neurol Res. 2009 Oct;31(8):848-52.
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18 Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells. Bioorg Med Chem. 2013 May 1;21(9):2551-9.
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33 DNA microarray analysis of vitamin D-induced gene expression in a human colon carcinoma cell line. Physiol Genomics. 2004 Apr 13;17(2):122-9. doi: 10.1152/physiolgenomics.00002.2003.
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39 19-Nor-1,25(OH)2D2 (a novel, noncalcemic vitamin D analogue), combined with arsenic trioxide, has potent antitumor activity against myeloid leukemia. Cancer Res. 2005 Mar 15;65(6):2488-97.
40 Similarities and differences between two modes of antagonism of the thyroid hormone receptor. ACS Chem Biol. 2011 Oct 21;6(10):1096-106.
41 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
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44 Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
45 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
46 Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
47 Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
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51 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.
52 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
53 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
54 The Isoniazid Metabolites Hydrazine and Pyridoxal Isonicotinoyl Hydrazone Modulate Heme Biosynthesis. Toxicol Sci. 2019 Mar 1;168(1):209-224. doi: 10.1093/toxsci/kfy294.
55 Changes in gene expression profiles of multiple myeloma cells induced by arsenic trioxide (ATO): possible mechanisms to explain ATO resistance in vivo. Br J Haematol. 2005 Mar;128(5):636-44.
56 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
57 Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
58 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.
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