General Information of Drug (ID: DM5TQ2O)

Drug Name
Galangin Drug Info
Synonyms
Galangin; 548-83-4; Norizalpinin; 3,5,7-Trihydroxyflavone; 3,5,7-Trihydroxy-2-phenyl-4H-chromen-4-one; 3,5,7-triOH-Flavone; UNII-142FWE6ECS; 3,5,7-Trihydroxy-2-phenyl-4-benzopyrone; 4H-1-Benzopyran-4-one, 3,5,7-trihydroxy-2-phenyl-; EINECS 208-960-4; NSC407229; FLAVONE, 3,5,7-TRIHYDROXY-; NSC 407229; NSC-407229; 4H-Benzopyran-4-one, 3,5,7-trihydroxy-2-phenyl-; BRN 0272179; 142FWE6ECS; 3,5,7-trihydroxy-2-phenylchromen-4-one; CHEBI:5262; CHEMBL309490; VCCRNZQBSJXYJD-UHFFFAOYSA-N; 3,5,7-trihydroxy-2-phenyl-4H-benzopyran-4-one
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5281616
ChEBI ID
CHEMBL309490
CAS Number
CAS 548-83-4
TTD Drug ID
DM5TQ2O

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Approved Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
IB-MECA DM9G5XD Psoriasis vulgaris EA90 Phase 3 [10]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [11]
NITD609 DMQHBSX Malaria 1F40-1F45 Phase 2 [12]
CF102 DMP56WJ Hepatocellular carcinoma 2C12.02 Phase 2 [13]
SCH-442416 DMQ2K1V N. A. N. A. Phase 1 [14]
AST-004 DM5WMG7 Stroke 8B20 Phase 1 [15]
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [16]
BAY 60-6583 DMTEJV1 Myocardial ischemia BA6Z Preclinical [17]
CF602 DM0ULO2 Inflammation 1A00-CA43.1 Preclinical [13]
CF502 DMQSJ20 Inflammation 1A00-CA43.1 Preclinical [13]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Caffeine DMKBJWP Allergic rhinitis CA08.0 Approved [18]
Istradefylline DM20VSK Parkinson disease 8A00.0 Approved [19]
Regadenoson DM76VHG Radionuclide imaging N.A. Approved [20]
Tozadenant DMATC14 Parkinson disease 8A00.0 Phase 3 [21]
Binodenoson DMVHF8G Hypertension BA00-BA04 Phase 3 [22]
Apadenoson DMD8QTC Coronary artery disease BA80 Phase 3 [23]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [11]
Dexefaroxan DMTY4KN Parkinson disease 8A00.0 Phase 2 [24]
AMP-579 DMJ4GPR Hyperlipidaemia 5C80 Phase 2 [25]
BIIB014 DMH7RJ1 Parkinson disease 8A00.0 Phase 2 [26]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
PINOCEMBRIN DM96VWD N. A. N. A. Phase 2 [4]
NARINGENIN DMHAZLM N. A. N. A. Phase 1 [4]
Chrysin DM7V2LG Discovery agent N.A. Investigative [4]
APIGENIN DMI3491 Discovery agent N.A. Investigative [4]
KAEMPFEROL DMHEMUB Discovery agent N.A. Investigative [4]
ISORHAMNETIN DMQ4Z6E Discovery agent N.A. Investigative [4]
ACACETIN DMQOB0X Discovery agent N.A. Investigative [4]
TRISMETHOXYRESVERATROL DM6USPC Discovery agent N.A. Investigative [27]
CHRYSOERIOL DM96ECL Discovery agent N.A. Investigative [4]
DIOSMETIN DM4KXIM Discovery agent N.A. Investigative [4]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [30]
Artemether DM48QOT Malaria 1F40-1F45 Approved [31]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [32]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [33]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [34]
Estrone DM5T6US Acne vulgaris ED80 Approved [35]
Leflunomide DMR8ONJ Arthritis FA20 Approved [36]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [38]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [39]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [40]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [41]
Cepharanthine DM9Y5JB N. A. N. A. Approved [42]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [43]
Clozapine DMFC71L Schizophrenia 6A20 Approved [44]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [45]
Trifluoperazine DMKBYWI Anxiety Approved [46]
Olanzapine DMPFN6Y Bipolar depression Approved [44]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [47]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [48]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [49]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [50]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [51]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [52]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [53]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [54]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [55]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [56]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [57]
Selenium DM25CGV N. A. N. A. Approved [58]
Methotrexate DM2TEOL Anterior urethra cancer Approved [59]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [60]
Trovafloxacin DM6AN32 Acute gonococcal cervicitis Approved [61]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [62]
Chloramphenicol DMFXEWT Bacterial infection 1A00-1C4Z Approved [63]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [64]
Artesunate DMR27C8 Infection of P. falciparum 1F40 Approved [65]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [66]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [67]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [68]
Gefitinib DM15F0X Colon adenocarcinoma Approved [69]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [70]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [71]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [72]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [73]
Methotrexate DM2TEOL Anterior urethra cancer Approved [74]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [75]
Quercetin DM3NC4M Obesity 5B81 Approved [76]
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Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [77]
Gefitinib DM15F0X Colon adenocarcinoma Approved [78]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [79]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [80]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [81]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [82]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [81]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [83]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [84]
Methotrexate DM2TEOL Anterior urethra cancer Approved [85]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [86]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [87]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [88]
Gefitinib DM15F0X Colon adenocarcinoma Approved [89]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [70]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [90]
Etretinate DM2CZFA Keratosis ED56 Approved [91]
Prednisone DM2HG4X Acute asthma CA23 Approved [92]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [82]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [93]
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Drug(s) Affected By Bcl-2-like protein 1 (BCL2L1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [94]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [95]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [80]
Selenium DM25CGV N. A. N. A. Approved [58]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [96]
Methotrexate DM2TEOL Anterior urethra cancer Approved [59]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [97]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [98]
Quercetin DM3NC4M Obesity 5B81 Approved [99]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [100]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [101]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [102]
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [103]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
Testosterone enanthate DMB6871 N. A. N. A. Approved [104]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [105]
Demecolcine DMCZQGK Solid tumour/cancer 2A00-2F9Z Approved [106]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [107]
Ethanol DMDRQZU Chronic pain MG30 Approved [108]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [64]
⏷ 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 [109]
Quercetin DM3NC4M Obesity 5B81 Approved [101]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [102]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [110]
Panobinostat DM58WKG Chronic graft versus host disease Approved [111]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [112]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [113]
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [113]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [52]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [107]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [114]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [115]
Leflunomide DMR8ONJ Arthritis FA20 Approved [116]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [52]
Demecolcine DMCZQGK Solid tumour/cancer 2A00-2F9Z Approved [106]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [64]
Arsenic DMTL2Y1 N. A. N. A. Approved [117]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [118]
Prednisolone DMQ8FR2 Acute adrenal insufficiency Approved [119]
Resveratrol DM3RWXL Giant cell arteritis 4A44.2 Phase 3 [120]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [121]
Methotrexate DM2TEOL Anterior urethra cancer Approved [59]
Trovafloxacin DM6AN32 Acute gonococcal cervicitis Approved [61]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [122]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [52]
Melphalan DMOLNHF Hematologic disease 3C0Z Approved [123]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [64]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [124]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [118]
COUMARIN DM0N8ZM Discovery agent N.A. Investigative [125]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [109]
Methotrexate DM2TEOL Anterior urethra cancer Approved [126]
Quercetin DM3NC4M Obesity 5B81 Approved [8]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [127]
Panobinostat DM58WKG Chronic graft versus host disease Approved [111]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [128]
Leflunomide DMR8ONJ Arthritis FA20 Approved [116]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [105]
Ketorolac DMI4EL5 Postoperative inflammation 1A00-CA43.1 Approved [128]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [129]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [130]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [131]
Trovafloxacin DM6AN32 Acute gonococcal cervicitis Approved [61]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
Cantharidin DMBP5N3 Molluscum contagiosum infection 1E76 Approved [132]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [105]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [107]
Gentamicin DMKINJO Bacteremia 1A73 Approved [131]
Artesunate DMR27C8 Infection of P. falciparum 1F40 Approved [65]
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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
Adenosine A2a receptor (ADORA2A) TTM2AOE AA2AR_HUMAN Inhibitor [2]
Adenosine A3 receptor (ADORA3) TTJFY5U AA3R_HUMAN Inhibitor [3]
Cytochrome P450 1B1 (CYP1B1) TTI84H7 CP1B1_HUMAN Inhibitor [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [5]
Autophagy-related protein 16-1 (ATG16L1) OTEOYC5D A16L1_HUMAN Gene/Protein Processing [6]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Gene/Protein Processing [7]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Gene/Protein Processing [7]
Endothelial PAS domain-containing protein 1 (EPAS1) OTRE3O8U EPAS1_HUMAN Gene/Protein Processing [8]
Mothers against decapentaplegic homolog 1 (SMAD1) OTQSHR25 SMAD1_HUMAN Gene/Protein Processing [6]
Mothers against decapentaplegic homolog 2 (SMAD2) OTC6VB4K SMAD2_HUMAN Gene/Protein Processing [6]
Mothers against decapentaplegic homolog 4 (SMAD4) OTWQWCKG SMAD4_HUMAN Gene/Protein Processing [6]
Mothers against decapentaplegic homolog 6 (SMAD6) OTUZZWUD SMAD6_HUMAN Gene/Protein Processing [6]
Nuclear receptor subfamily 1 group I member 3 (NR1I3) OTS3SGH7 NR1I3_HUMAN Gene/Protein Processing [9]

References

1 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: 410).
2 Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem. 1997 Aug 1;40(16):2588-95.
3 Interactions of flavonoids and other phytochemicals with adenosine receptors. J Med Chem. 1996 Feb 2;39(3):781-8.
4 Selective inhibition of methoxyflavonoids on human CYP1B1 activity. Bioorg Med Chem. 2010 Sep 1;18(17):6310-5.
5 3-Hydroxyflavone and structural analogues differentially activate pregnane X receptor: Implication for inflammatory bowel disease. Pharmacol Res. 2015 Oct;100:64-72.
6 Galangin suppresses HepG2 cell proliferation by activating the TGF- receptor/Smad pathway. Toxicology. 2014 Dec 4;326:9-17. doi: 10.1016/j.tox.2014.09.010. Epub 2014 Sep 28.
7 Galangin inhibits growth of human head and neck squamous carcinoma cells in vitro and in vivo. Chem Biol Interact. 2014 Dec 5;224:149-56. doi: 10.1016/j.cbi.2014.10.027. Epub 2014 Nov 4.
8 Flavonoids-induced accumulation of hypoxia-inducible factor (HIF)-1alpha/2alpha is mediated through chelation of iron. J Cell Biochem. 2008 Apr 15;103(6):1989-98. doi: 10.1002/jcb.21588.
9 Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR). Toxicol Lett. 2015 Mar 4;233(2):68-77.
10 A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60.
11 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
12 Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.
13 2011 Pipeline of Can-Fite BioPharm.
14 Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4.
15 Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke. Stroke. 2022 Jan;53(1):238-248.
16 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
17 Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71.
18 Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
19 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
21 Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76.
22 Coronary circulation responses to binodenoson, a selective adenosine A2A receptor agonist. Am J Cardiol. 2007 Jun 1;99(11):1507-12.
23 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: 3290).
24 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
25 Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.
26 Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54.
27 Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors. J Med Chem. 2002 Jan 3;45(1):160-4.
28 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.
29 Bioactive terpenoids and flavonoids from Ginkgo biloba extract induce the expression of hepatic drug-metabolizing enzymes through pregnane X receptor, constitutive androstane receptor, and aryl hydrocarbon receptor-mediated pathways. Pharm Res. 2009 Apr;26(4):872-82.
30 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
31 Fetal bovine serum and human constitutive androstane receptor: evidence for activation of the SV23 splice variant by artemisinin, artemether, and arteether in a serum-free cell culture system. Toxicol Appl Pharmacol. 2014 Jun 1;277(2):221-30. doi: 10.1016/j.taap.2014.03.023. Epub 2014 Apr 12.
32 Constitutive androstane/active receptor is a target of retinoic acid receptor in humans. Biochem Pharmacol. 2010 Jul 1;80(1):129-35. doi: 10.1016/j.bcp.2010.02.023. Epub 2010 Mar 6.
33 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
34 Expression and inducibility of cytochrome P450s (CYP1A1, 2B6, 2E1, 3A4) in human cord blood CD34(+) stem cell-derived differentiating neuronal cells. Toxicol Sci. 2012 Oct;129(2):392-410.
35 Agonistic effects of diverse xenobiotics on the constitutive androstane receptor as detected in a recombinant yeast-cell assay. Toxicol In Vitro. 2018 Feb;46:335-349. doi: 10.1016/j.tiv.2017.09.014. Epub 2017 Sep 18.
36 Teriflunomide is an indirect human constitutive androstane receptor (CAR) activator interacting with epidermal growth factor (EGF) signaling. Front Pharmacol. 2018 Oct 11;9:993.
37 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.
38 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
39 Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
40 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.
41 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.
42 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.
43 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.
44 Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
45 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
46 Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.
47 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
48 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
49 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
50 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
51 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
52 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.
53 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
54 The genomic response of Ishikawa cells to bisphenol A exposure is dose- and time-dependent. Toxicology. 2010 Apr 11;270(2-3):137-49. doi: 10.1016/j.tox.2010.02.008. Epub 2010 Feb 17.
55 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
56 Effects of progesterone treatment on expression of genes involved in uterine quiescence. Reprod Sci. 2011 Aug;18(8):781-97.
57 Time course study of A formation and neurite outgrowth disruption in differentiated human neuroblastoma cells exposed to H2O2: protective role of autophagy. Toxicol In Vitro. 2013 Sep;27(6):1780-8. doi: 10.1016/j.tiv.2013.05.005. Epub 2013 May 29.
58 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.
59 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
60 Arsenic trioxide induces autophagic cell death in osteosarcoma cells via the ROS-TFEB signaling pathway. Biochem Biophys Res Commun. 2018 Jan 29;496(1):167-175. doi: 10.1016/j.bbrc.2018.01.018. Epub 2018 Jan 4.
61 TNF enhances trovafloxacin-induced in vitro hepatotoxicity by inhibiting protective autophagy. Toxicol Lett. 2021 May 15;342:73-84. doi: 10.1016/j.toxlet.2021.02.009. Epub 2021 Feb 17.
62 Hydroquinone-induced endoplasmic reticulum stress affects TK6 cell autophagy and apoptosis via ATF6-mTOR. Environ Toxicol. 2023 Aug;38(8):1874-1890. doi: 10.1002/tox.23814. Epub 2023 May 6.
63 Mitochondrial DNA deletions and chloramphenicol treatment stimulate the autophagic transcript ATG12. Autophagy. 2007 Jul-Aug;3(4):377-80. doi: 10.4161/auto.4239. Epub 2007 Jul 5.
64 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
65 Artesunate alleviates liver fibrosis by regulating ferroptosis signaling pathway. Biomed Pharmacother. 2019 Jan;109:2043-2053. doi: 10.1016/j.biopha.2018.11.030. Epub 2018 Nov 26.
66 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
67 Indomethacin inhibits cell growth of medullary thyroid carcinoma by reducing cell cycle progression into S phase. Exp Biol Med (Maywood). 2008 Nov;233(11):1433-40. doi: 10.3181/0804-RM-127. Epub 2008 Sep 12.
68 Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer. Endocr Relat Cancer. 2011 Apr 28;18(3):333-45. doi: 10.1530/ERC-10-0262. Print 2011 Jun.
69 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
70 BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile. J Biochem Mol Toxicol. 2019 May;33(5):e22286. doi: 10.1002/jbt.22286. Epub 2019 Jan 23.
71 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
72 Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
73 Sulindac induces specific degradation of the HPV oncoprotein E7 and causes growth arrest and apoptosis in cervical carcinoma cells. Cancer Lett. 2007 Jan 8;245(1-2):103-11. doi: 10.1016/j.canlet.2005.12.034. Epub 2006 Feb 20.
74 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
75 HMG-CoA reductase inhibitor simvastatin inhibits cell cycle progression at the G1/S checkpoint in immortalized lymphocytes from Alzheimer's disease patients independently of cholesterol-lowering effects. J Pharmacol Exp Ther. 2008 Jan;324(1):352-9. doi: 10.1124/jpet.107.128959. Epub 2007 Oct 10.
76 Inhibition of prostate cancer cell colony formation by the flavonoid quercetin correlates with modulation of specific regulatory genes. Clin Diagn Lab Immunol. 2004 Jan;11(1):63-9. doi: 10.1128/cdli.11.1.63-69.2004.
77 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.
78 Evidence of securin-mediated resistance to gefitinib-induced apoptosis in human cancer cells. Chem Biol Interact. 2013 Apr 25;203(2):412-22. doi: 10.1016/j.cbi.2013.03.011. Epub 2013 Mar 22.
79 Cigarette smoke and asbestos activate poly-ADP-ribose polymerase in alveolar epithelial cells. J Investig Med. 2001 Jan;49(1):68-76. doi: 10.2310/6650.2001.34092.
80 Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
81 The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. J Biochem Mol Toxicol. 1999;13(6):338-47. doi: 10.1002/(sici)1099-0461(1999)13:6<338::aid-jbt8>3.0.co;2-7.
82 Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
83 Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells. Toxicol In Vitro. 2021 Jun;73:105138. doi: 10.1016/j.tiv.2021.105138. Epub 2021 Mar 6.
84 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
85 Methotrexate induces poly(ADP-ribose) polymerase-dependent, caspase 3-independent apoptosis in subsets of proliferating CD4+ T cells. Clin Exp Immunol. 2007 May;148(2):288-95. doi: 10.1111/j.1365-2249.2007.03335.x. Epub 2007 Feb 7.
86 Zidovudine induces S-phase arrest and cell cycle gene expression changes in human cells. Mutagenesis. 2005 Mar;20(2):139-46. doi: 10.1093/mutage/gei019. Epub 2005 Mar 22.
87 Cannabidiol Activates Neuronal Precursor Genes in Human Gingival Mesenchymal Stromal Cells. J Cell Biochem. 2017 Jun;118(6):1531-1546. doi: 10.1002/jcb.25815. Epub 2016 Dec 29.
88 Gene expression profiles with activation of the estrogen receptor alpha-selective estrogen receptor modulator complex in breast cancer cells expressing wild-type estrogen receptor. Cancer Res. 2002 Aug 1;62(15):4419-26.
89 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
90 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.
91 Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26. doi: 10.1111/j.1365-2133.2008.08931.x. Epub 2008 Nov 25.
92 Glucocorticoids induce G1 arrest of lymphoblastic cells through retinoblastoma protein Rb1 dephosphorylation in childhood acute lymphoblastic leukemia in vivo. Cancer Biol Ther. 2004 May;3(5):470-6. doi: 10.4161/cbt.3.5.838. Epub 2004 May 9.
93 Utilization of CDKN1A/p21 gene for class discrimination of DNA damage-induced clastogenicity. Toxicology. 2014 Jan 6;315:8-16. doi: 10.1016/j.tox.2013.10.009. Epub 2013 Nov 6.
94 Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
95 Expression of the retinoic acid-metabolizing enzyme CYP26A1 limits programmed cell death. Mol Pharmacol. 2005 May;67(5):1808-17. doi: 10.1124/mol.104.005769. Epub 2005 Feb 9.
96 Role of BAX in the apoptotic response to anticancer agents. Science. 2000 Nov 3;290(5493):989-92. doi: 10.1126/science.290.5493.989.
97 Mechanisms of thymidine kinase/ganciclovir and cytosine deaminase/ 5-fluorocytosine suicide gene therapy-induced cell death in glioma cells. Oncogene. 2005 Feb 10;24(7):1231-43. doi: 10.1038/sj.onc.1208290.
98 Simvastatin induces apoptosis in human colon cancer cells and in tumor xenografts, and attenuates colitis-associated colon cancer in mice. Int J Cancer. 2008 Aug 15;123(4):951-7. doi: 10.1002/ijc.23593.
99 Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
100 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
101 Suppression of transforming growth factor beta/smad signaling in keloid-derived fibroblasts by quercetin: implications for the treatment of excessive scars. J Trauma. 2004 Nov;57(5):1032-7. doi: 10.1097/01.ta.0000114087.46566.eb.
102 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.
103 Ouabain impairs cell migration, and invasion and alters gene expression of human osteosarcoma U-2 OS cells. Environ Toxicol. 2017 Nov;32(11):2400-2413. doi: 10.1002/tox.22453. Epub 2017 Aug 10.
104 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.
105 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
106 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
107 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.
108 Chronic ethanol exposure increases goosecoid (GSC) expression in human embryonic carcinoma cell differentiation. J Appl Toxicol. 2014 Jan;34(1):66-75.
109 MS4A3-HSP27 target pathway reveals potential for haematopoietic disorder treatment in alimentary toxic aleukia. Cell Biol Toxicol. 2023 Feb;39(1):201-216. doi: 10.1007/s10565-021-09639-4. Epub 2021 Sep 28.
110 Glucosamine promotes osteogenic differentiation of dental pulp stem cells through modulating the level of the transforming growth factor-beta type I receptor. J Cell Physiol. 2010 Oct;225(1):140-51.
111 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.
112 Endoplasmic reticulum stress contributes to arsenic trioxide-induced intrinsic apoptosis in human umbilical and bone marrow mesenchymal stem cells. Environ Toxicol. 2016 Mar;31(3):314-28.
113 The differential cancer growth associated with anaesthetics in a cancer xenograft model of mice: mechanisms and implications of postoperative cancer recurrence. Cell Biol Toxicol. 2023 Aug;39(4):1561-1575. doi: 10.1007/s10565-022-09747-9. Epub 2022 Aug 12.
114 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
115 THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
116 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
117 Prenatal arsenic exposure and shifts in the newborn proteome: interindividual differences in tumor necrosis factor (TNF)-responsive signaling. Toxicol Sci. 2014 Jun;139(2):328-37. doi: 10.1093/toxsci/kfu053. Epub 2014 Mar 27.
118 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.
119 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
120 The role of sirtuin 1 in osteoblastic differentiation in human periodontal ligament cells. J Periodontal Res. 2011 Dec;46(6):712-21. doi: 10.1111/j.1600-0765.2011.01394.x. Epub 2011 Jul 11.
121 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.
122 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
123 Bone marrow osteoblast damage by chemotherapeutic agents. PLoS One. 2012;7(2):e30758. doi: 10.1371/journal.pone.0030758. Epub 2012 Feb 17.
124 Predictive toxicology using systemic biology and liver microfluidic "on chip" approaches: application to acetaminophen injury. Toxicol Appl Pharmacol. 2012 Mar 15;259(3):270-80.
125 Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.
126 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
127 Systems analysis of transcriptome and proteome in retinoic acid/arsenic trioxide-induced cell differentiation/apoptosis of promyelocytic leukemia. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7653-8.
128 Ibuprofen-mediated reduction of hypoxia-inducible factors HIF-1alpha and HIF-2alpha in prostate cancer cells. Clin Cancer Res. 2003 Aug 1;9(8):3150-7.
129 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.
130 Low Autophagy (ATG) Gene Expression Is Associated with an Immature AML Blast Cell Phenotype and Can Be Restored during AML Differentiation Therapy. Oxid Med Cell Longev. 2018 Mar 18;2018:1482795. doi: 10.1155/2018/1482795. eCollection 2018.
131 Effect of nephrotoxicants and hepatotoxicants on gene expression profile in human peripheral blood mononuclear cells. Biochem Biophys Res Commun. 2010 Oct 15;401(2):245-50. doi: 10.1016/j.bbrc.2010.09.039. Epub 2010 Sep 16.
132 Endoplasmic reticulum stress contributes to autophagy and apoptosis in cantharidin-induced nephrotoxicity. Food Chem Toxicol. 2022 May;163:112986. doi: 10.1016/j.fct.2022.112986. Epub 2022 Apr 6.