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

General Information of Drug (ID: DM702WR)

Drug Name
LTC4 Drug Info
Synonyms leukotriene C4
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5280493
ChEBI ID
CHEBI:16978
CAS Number
CAS 72025-60-6
TTD Drug ID
DM702WR
INTEDE Drug ID
DR2048

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Patented Agent(s)
Download the Complete Related Drug List
Drug(s) Targeting Uracil nucleotide/cysteinyl leukotriene receptor (GPR17)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LTE4 DMCPB0Q Discovery agent N.A. Investigative [16]
UDP-glucose DMLT4JA Discovery agent N.A. Investigative [4]
LTD4 DMIUZX3 Discovery agent N.A. Investigative [4]
ASN04421891 DMC82XN Discovery agent N.A. Investigative [17]
ASN04450772 DMKR69T Discovery agent N.A. Investigative [17]
ASN06917370 DMA20JP Discovery agent N.A. Investigative [17]
ASN02563583 DMEO3Y4 Discovery agent N.A. Investigative [17]
ASN04885796 DMQ0VZ8 Discovery agent N.A. Investigative [17]
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Drug(s) Targeting Leukotriene CysLT1 receptor (CYSLTR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Montelukast DMD157S Allergic asthma CA23.0 Approved [18]
Zafirlukast DMHNQOG Asthma CA23 Approved [19]
Pranlukast DMYHDCA Allergic rhinitis CA08.0 Approved [20]
Cinalukast DMFIC0M Asthma CA23 Approved [21]
KP-496 DMCO8UZ Asthma CA23 Phase 2 [22]
BAY-X-7195 DM2XE80 Asthma CA23 Phase 2 [23]
Masilukast DMDTI0L Asthma CA23 Phase 2 [24]
LM-1507.NA DMW6VA0 Asthma CA23 Phase 2 [25]
Iralukast DMQ3RWN Asthma CA23 Phase 2 [26]
YM-57158 DMS31YW Allergic rhinitis CA08.0 Phase 1 [27]
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Drug(s) Targeting Leukotriene CysLT2 receptor (CYSLTR2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY-X-7195 DM2XE80 Asthma CA23 Phase 2 [23]
AS-35 DMC2WI7 Asthma CA23 Discontinued in Phase 2 [28]
DS-4574 DM8GZWC Asthma CA23 Discontinued in Phase 2 [29]
Sulukast DMBSLZV Asthma CA23 Discontinued in Phase 2 [30]
ICI-198615 DM0195G Asthma CA23 Terminated [31]
MDL-43291 DMBIDQX Asthma CA23 Terminated [32]
LY-290154 DMPZ7AO Asthma CA23 Terminated [33]
FPL-55712 DMF1CDK Asthma CA23 Terminated [34]
LTE4 DMCPB0Q Discovery agent N.A. Investigative [35]
LTD4 DMIUZX3 Discovery agent N.A. Investigative [3]
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Drug(s) Metabolized By Gamma-glutamyltranspeptidase 5 (GGT5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [5]
Glutathione ester DMAV2I7 N. A. N. A. Investigative [5]
Drug(s) Metabolized By Gamma-glutamyltranspeptidase 1 (GGT1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glutathione ester DMAV2I7 N. A. N. A. Investigative [5]
Drug(s) Affected By Cysteinyl leukotriene receptor 1 (CYSLTR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zafirlukast DMHNQOG Asthma CA23 Approved [9]
Pranlukast DMYHDCA Allergic rhinitis CA08.0 Approved [9]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [36]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [37]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [38]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [39]
PMID28870136-Compound-48 DMPIM9L N. A. N. A. Patented [36]
LTE4 DMCPB0Q Discovery agent N.A. Investigative [40]
BAYu9773 DMXQ14V Discovery agent N.A. Investigative [9]
CGP-57698 DMYZ72J Discovery agent N.A. Investigative [9]
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Drug(s) Affected By Endothelin-1 (EDN1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [41]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [42]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [43]
Methotrexate DM2TEOL Anterior urethra cancer Approved [44]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [45]
Quercetin DM3NC4M Obesity 5B81 Approved [46]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [47]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [48]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [49]
Lisinopril DMUOK4C Chronic heart failure BD1Z Approved [50]
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Drug(s) Affected By P-selectin (SELP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [51]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [37]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [52]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [53]
Amlodipine DMBDAZV Angina pectoris BA40 Approved [54]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [55]
Asasantin DMCZIHT Cerebrovascular ischaemia 8B1Z Approved [56]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [57]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [58]
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [59]
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Drug(s) Affected By Leukotriene C4 synthase (LTC4S)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aspirin DM672AH Acute coronary syndrome BA41 Approved [60]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [61]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [55]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [62]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [63]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [64]
Pranlukast DMYHDCA Allergic rhinitis CA08.0 Approved [65]
Etazolate DMOCID7 Neurodegenerative disorder 8A20-8A23 Phase 2 [66]
PMID28870136-Compound-48 DMPIM9L N. A. N. A. Patented [66]
Forskolin DM6ITNG Solid tumour/cancer 2A00-2F9Z Investigative [66]
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Drug(s) Affected By Interleukin-5 (IL5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [67]
Tolnaftate DM28MU7 Dermatophytosis 1F28.2 Approved [68]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [69]
Prednisone DM2HG4X Acute asthma CA23 Approved [70]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [71]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [72]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [73]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [74]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [75]
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [76]
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Drug(s) Affected By RalA-binding protein 1 (RALBP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [77]
Selenium DM25CGV N. A. N. A. Approved [78]
Quercetin DM3NC4M Obesity 5B81 Approved [79]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [80]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [55]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [81]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [15]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [82]
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [83]
Urethane DM7NSI0 N. A. N. A. Phase 4 [84]
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Drug(s) Affected By ABC-type organic anion transporter ABCA8 (ABCA8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [85]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [86]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [87]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [88]
Indomethacin DMSC4A7 Bursitis Approved [89]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [90]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [86]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [91]
Vorinostat DMWMPD4 Adult acute monocytic leukemia Approved [92]
Triclosan DMZUR4N Malaria 1F40-1F45 Approved [93]
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Drug(s) Affected By Multidrug resistance-associated protein 1 (ABCC1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [94]
Folic Acid DMEMBJC Colorectal carcinoma Approved [95]
Methotrexate DM2TEOL Anterior urethra cancer Approved [96]
Quercetin DM3NC4M Obesity 5B81 Approved [97]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [98]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [99]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [100]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [101]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [102]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [102]
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Drug(s) Affected By ATP-binding cassette sub-family C member 2 (ABCC2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lopinavir DMITQS0 Human immunodeficiency virus infection 1C62 Approved [103]
Sulfinpyrazone DMEV954 Gout FA25 Approved [104]
Probenecid DMMFWOJ Acute gonococcal cervicitis Approved [105]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [106]
Methotrexate DM2TEOL Anterior urethra cancer Approved [96]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [107]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [108]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [100]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [109]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [90]
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Drug(s) Affected By ATP-binding cassette sub-family C member 6 (ABCC6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Benzbromarone DMC3YUA Gout FA25 Approved [110]
Verapamil DMA7PEW Angina pectoris BA40 Approved [110]
Quercetin DM3NC4M Obesity 5B81 Approved [111]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [88]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [112]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [113]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [85]
Adenosine triphosphate DM79F6G Malnutrition 5B50-5B71 Approved [8]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [86]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [55]
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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
Leukotriene CysLT1 receptor (CYSLTR1) TTGKOY9 CLTR1_HUMAN Agonist [2]
Leukotriene CysLT2 receptor (CYSLTR2) TT0PZR5 CLTR2_HUMAN Agonist [3]
Uracil nucleotide/cysteinyl leukotriene receptor (GPR17) TTMPART GPR17_HUMAN Agonist [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Gamma-glutamyltranspeptidase 5 (GGT5) DEH6CAO GGT5_HUMAN Substrate [5]
Gamma-glutamyltranspeptidase 1 (GGT1) DEPT1ME GGT1_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ABC-type organic anion transporter ABCA8 (ABCA8) OTCWLX6N ABCA8_HUMAN Regulation of Drug Effects [6]
ATP-binding cassette sub-family C member 2 (ABCC2) OTJSIGV5 MRP2_HUMAN Regulation of Drug Effects [7]
ATP-binding cassette sub-family C member 6 (ABCC6) OTZT0LKT MRP6_HUMAN Regulation of Drug Effects [8]
Cysteinyl leukotriene receptor 1 (CYSLTR1) OT904HBN CLTR1_HUMAN Protein Interaction/Cellular Processes [9]
Endothelin-1 (EDN1) OTZCACEG EDN1_HUMAN Gene/Protein Processing [10]
Interleukin-5 (IL5) OTAFPSCO IL5_HUMAN Regulation of Drug Effects [11]
Leukotriene C4 synthase (LTC4S) OT3XNFJZ LTC4S_HUMAN Biotransformations [12]
Multidrug resistance-associated protein 1 (ABCC1) OTGUN89S MRP1_HUMAN Regulation of Drug Effects [13]
P-selectin (SELP) OTWR90PK LYAM3_HUMAN Gene/Protein Processing [14]
RalA-binding protein 1 (RALBP1) OTBIGB1D RBP1_HUMAN Regulation of Drug Effects [15]

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: 3354).
2 Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature. 1999 Jun 24;399(6738):789-93.
3 Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol Pharmacol. 2000 Dec;58(6):1601-8.
4 The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor. EMBO J. 2006 Oct 4;25(19):4615-27.
5 Gamma-glutamyl compounds: substrate specificity of gamma-glutamyl transpeptidase enzymes. Anal Biochem. 2011 Jul 15;414(2):208-14.
6 Functional analysis of ABCA8, a new drug transporter. Biochem Biophys Res Commun. 2002 Oct 18;298(1):41-5.
7 Mutation of Trp1254 in the multispecific organic anion transporter, multidrug resistance protein 2 (MRP2) (ABCC2), alters substrate specificity and results in loss of methotrexate transport activity. J Biol Chem. 2001 Oct 12;276(41):38108-14. doi: 10.1074/jbc.M105160200. Epub 2001 Aug 10.
8 Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). J Biol Chem. 2002 May 10;277(19):16860-7.
9 A kinetic binding study to evaluate the pharmacological profile of a specific leukotriene C(4) binding site not coupled to contraction in human lun... Mol Pharmacol. 2000 Jun;57(6):1182-9.
10 [Zafirlukast inhibition of leukotriene C4 induced endothelin-1 expression in human airway structural cell]. Zhonghua Jie He He Hu Xi Za Zhi. 2000 Oct;23(10):617-20.
11 Attenuation of IL-5-mediated signal transduction, eosinophil survival, and inflammatory mediator release by a soluble human IL-5 receptor. J Immunol. 1997 Oct 15;159(8):4024-34.
12 Aberrant expression of active leukotriene C(4) synthase in CD16(+) neutrophils from patients with chronic myeloid leukemia. Blood. 2000 Feb 15;95(4):1456-64.
13 Role of proline 1150 in functional interactions between the membrane spanning domains and nucleotide binding domains of the MRP1 (ABCC1) transporter. Biochem Pharmacol. 2008 Apr 15;75(8):1659-69. doi: 10.1016/j.bcp.2008.01.009. Epub 2008 Feb 5.
14 Cysteinyl leukotrienes induce P-selectin expression in human endothelial cells via a non-CysLT1 receptor-mediated mechanism. J Pharmacol Exp Ther. 1997 May;281(2):655-62.
15 RLIP76 (RALBP1)-mediated transport of leukotriene C4 (LTC4) in cancer cells: implications in drug resistance. Int J Cancer. 2004 Dec 20;112(6):934-42. doi: 10.1002/ijc.20516.
16 The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repair. PLoS One. 2008;3(10):e3579.
17 In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases. J Comput Aided Mol Des. 2011 Aug;25(8):743-52.
18 Protective potential of montelukast against hepatic ischemia/reperfusion injury in rats. J Surg Res. 2010 Mar;159(1):588-94.
19 Inhibitory effects of zafirlukast on respiratory bursts of human neutrophils. Drugs Exp Clin Res. 2002;28(4):133-45.
20 Beneficial effects of leukotriene receptor antagonists in the prevention of cedar pollinosis in a community setting. J Investig Allergol Clin Immunol. 2009;19(3):195-203.
21 Prolonged protection against exercise-induced bronchoconstriction by the leukotriene D4-receptor antagonist cinalukast. J Allergy Clin Immunol. 1997 Feb;99(2):210-5.
22 Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol Int. 2006 Dec;55(4):403-10.
23 The effect of a novel leukotriene C4/D4 antagonist, BAY-x-7195, on experimental allergic reactions. Prostaglandins. 1995 Nov-Dec;50(5-6):269-85.
24 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
25 Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma. Biochem Pharmacol. 2002 Apr 15;63(8):1537-46.
26 Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro. Br J Pharmacol. 1998 Feb;123(3):590-8.
27 In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
28 Inhibition of radiolabeled leukotriene-binding by AS-35 in guinea pig lung membrane fraction. Jpn J Pharmacol. 1992 Apr;58(4):357-64.
29 Inhibitory effect of DS-4574, a mast cell stabilizer with peptidoleukotriene receptor antagonism, on gastric acid secretion in rats. Eur J Pharmacol. 1994 Apr 1;255(1-3):229-34.
30 The pharmacological evaluation of LY 170680, a novel leukotriene D4 and E4 antagonist in the guinea-pig. Br J Pharmacol. 1989 Sep;98(1):259-67.
31 Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Biochem Pharmacol. 1992 Oct 6;44(7):1411-5.
32 Conformationally restricted leukotriene receptor antagonists: [(octahydro-2-oxo-7-tetradecylidene-2H-1-benzopyran-8-yl)thio]ace tic acids. Pharmacology. 1990;40(5):271-6.
33 DOI: 10.1021/op060036x
34 Effect of the leukotriene receptor antagonists FPL 55712, LY 163443, and MK-571 on the elimination of cysteinyl leukotrienes in the rat. Br J Pharmacol. 1991 Apr;102(4):865-70.
35 Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT agonist, N-methyl-leukotriene C in calcium reporter and beta arrestin assays. Mol Pharmacol. 2011 Feb;79(2):270-8.
36 Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802.
37 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.
38 Differential contribution of the CysLTR1 gene in patients with aspirin hypersensitivity. J Clin Immunol. 2007 Nov;27(6):613-9. doi: 10.1007/s10875-007-9115-x. Epub 2007 Jul 20.
39 Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells. J Biol Chem. 2012 Dec 14;287(51):43137-55.
40 Characterization of the leukotriene D4 receptor in dimethylsulphoxide-differentiated U937 cells: comparison with the leukotriene D4 receptor in human lung and guinea-pig lung. Eur J Pharmacol. 1993 Feb 15;244(3):239-50. doi: 10.1016/0922-4106(93)90149-4.
41 ?-adrenoceptors and muscarinic receptors mediate opposing effects on endothelin-1 expression in human lung fibroblasts. Eur J Pharmacol. 2012 Sep 15;691(1-3):218-24. doi: 10.1016/j.ejphar.2012.07.002. Epub 2012 Jul 13.
42 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.
43 Induction of endothelin-1 expression by oxidative stress in vascular smooth muscle cells. Cardiovasc Pathol. 2001 Nov-Dec;10(6):311-5. doi: 10.1016/s1054-8807(01)00095-3.
44 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
45 [Effect of simvastatin on endothelin-1 expression in endothelial cell cultured hypoxically]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2008 Jan;39(1):72-5.
46 Effects of dietary polyphenols on gene expression in human vascular endothelial cells. Proc Nutr Soc. 2008 Feb;67(1):42-7.
47 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.
48 Nucleoside reverse transcriptase inhibitors induce a mitophagy-associated endothelial cytotoxicity that is reversed by coenzyme Q10 cotreatment. Toxicol Sci. 2013 Aug;134(2):323-34. doi: 10.1093/toxsci/kft105. Epub 2013 May 2.
49 Cardiac toxicity of high-dose cyclophosphamide in patients with multiple myeloma undergoing autologous hematopoietic stem cell transplantation. Int J Hematol. 2007 Jun;85(5):408-14. doi: 10.1532/IJH97.E0620.
50 Different effects of angiotensin converting enzyme inhibitors on endothelin-1 and nitric oxide balance in human vascular endothelial cells: evidence of an oxidant-sensitive pathway. Mediators Inflamm. 2008;2008:305087. doi: 10.1155/2008/305087. Epub 2008 Dec 1.
51 Platelet/endothelial biomarkers in depressed patients treated with the selective serotonin reuptake inhibitor sertraline after acute coronary events: the Sertraline AntiDepressant Heart Attack Randomized Trial (SADHART) Platelet Substudy. Circulation. 2003 Aug 26;108(8):939-44. doi: 10.1161/01.CIR.0000085163.21752.0A. Epub 2003 Aug 11.
52 Hemostatic abnormalities associated with acute promyelocytic leukemia and corrective effects of all-trans-retinoic acid or arsenic trioxide treatment. Chin Med J (Engl). 2000 Mar;113(3):236-40.
53 Lack of uniform platelet activation in patients after ischemic stroke and choice of antiplatelet therapy. Thromb Res. 2004;113(3-4):197-204. doi: 10.1016/j.thromres.2004.03.002.
54 Platelet morphology and plasma indices of platelet activation in essential hypertension: effects of amlodipine-based antihypertensive therapy. Ann Med. 2004;36(7):552-7. doi: 10.1080/07853890410017386.
55 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.
56 Magnitude and time course of platelet inhibition with Aggrenox and Aspirin in patients after ischemic stroke: the AGgrenox versus Aspirin Therapy Evaluation (AGATE) trial. Eur J Pharmacol. 2004 Sep 24;499(3):315-24. doi: 10.1016/j.ejphar.2004.07.114.
57 Effects of histamine 2 receptor antagonists on endothelial-neutrophil adhesion and surface expression of endothelial adhesion molecules induced by high glucose levels. J Diabetes Complications. 2007 Jan-Feb;21(1):50-5. doi: 10.1016/j.jdiacomp.2006.02.002.
58 Reduced plaque formation induced by rosiglitazone in an STZ-diabetes mouse model of atherosclerosis is associated with downregulation of adhesion molecules. Atherosclerosis. 2008 Jul;199(1):55-64. doi: 10.1016/j.atherosclerosis.2007.10.038. Epub 2008 Feb 21.
59 Cocaine activates platelets and increases the formation of circulating platelet containing microaggregates in humans. Heart. 2000 Jun;83(6):688-95. doi: 10.1136/heart.83.6.688.
60 Genetic and ethnic risk factors associated with drug hypersensitivity. Curr Opin Allergy Clin Immunol. 2010 Aug;10(4):280-90. doi: 10.1097/ACI.0b013e32833b1eb3.
61 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.
62 Promoter polymorphism influences the effect of dexamethasone on transcriptional activation of the LTC4 synthase gene. Eur J Hum Genet. 2003 Aug;11(8):619-22. doi: 10.1038/sj.ejhg.5201015.
63 17-Estradiol Activates HSF1 via MAPK Signaling in ER-Positive Breast Cancer Cells. Cancers (Basel). 2019 Oct 11;11(10):1533. doi: 10.3390/cancers11101533.
64 The A-444C polymorphism in the leukotriene C4 synthase gene is associated with aspirin-induced urticaria. J Investig Allergol Clin Immunol. 2009;19(5):375-82.
65 Leukotriene C4 synthase gene A(-444)C polymorphism and clinical response to a CYS-LT(1) antagonist, pranlukast, in Japanese patients with moderate asthma. Pharmacogenetics. 2002 Oct;12(7):565-70. doi: 10.1097/00008571-200210000-00009.
66 Global expression profiling of theophylline response genes in macrophages: evidence of airway anti-inflammatory regulation. Respir Res. 2005 Aug 8;6(1):89. doi: 10.1186/1465-9921-6-89.
67 Regulatory role of nitric oxide on monocyte-derived dendritic cell functions. J Interferon Cytokine Res. 2003 Aug;23(8):423-31. doi: 10.1089/107999003322277838.
68 Anti-mycotics suppress interleukin-4 and interleukin-5 production in anti-CD3 plus anti-CD28-stimulated T cells from patients with atopic dermatitis. J Invest Dermatol. 2001 Dec;117(6):1635-46. doi: 10.1046/j.0022-202x.2001.01566.x.
69 Ribavirin polarizes human T cell responses towards a Type 1 cytokine profile. J Hepatol. 1999 Mar;30(3):376-82. doi: 10.1016/s0168-8278(99)80093-2.
70 Cytokine abnormalities in a patient with eosinophilic fasciitis. Ann Allergy Asthma Immunol. 2003 Apr;90(4):452-5. doi: 10.1016/S1081-1206(10)61832-7.
71 Expression of PPARgamma in eosinophils and its functional role in survival and chemotaxis. Immunol Lett. 2003 Apr 3;86(2):183-9. doi: 10.1016/s0165-2478(03)00003-8.
72 Direct and indirect effects of retinoic acid on human Th2 cytokine and chemokine expression by human T lymphocytes. BMC Immunol. 2006 Nov 21;7:27. doi: 10.1186/1471-2172-7-27.
73 Glucosamine improved atopic dermatitis-like skin lesions in NC/Nga mice by inhibition of Th2 cell development. Scand J Immunol. 2011 Jun;73(6):536-45. doi: 10.1111/j.1365-3083.2011.02526.x.
74 Delta 9-Tetrahydrocannabinol regulates Th1/Th2 cytokine balance in activated human T cells. J Neuroimmunol. 2002 Dec;133(1-2):124-31. doi: 10.1016/s0165-5728(02)00370-3.
75 IL-5 production by CD4+ T cells of asthmatic patients is suppressed by glucocorticoids and the immunosuppressants FK506 and cyclosporin A. Int Immunol. 1995 Mar;7(3):449-57. doi: 10.1093/intimm/7.3.449.
76 Limited effect of selected organic pollutants on cytokine production by peripheral blood leukocytes. Eur Cytokine Netw. 2004 Apr-Jun;15(2):145-51.
77 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.
78 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.
79 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.
80 A comprehensive analysis of Wnt/beta-catenin signaling pathway-related genes and crosstalk pathways in the treatment of As2O3 in renal cancer. Ren Fail. 2018 Nov;40(1):331-339.
81 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
82 Depletion of RLIP76 sensitizes lung cancer cells to doxorubicin. Biochem Pharmacol. 2005 Aug 1;70(3):481-8. doi: 10.1016/j.bcp.2005.05.005.
83 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.
84 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
85 Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes. Front Pharmacol. 2016 Apr 26;7:111.
86 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.
87 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.
88 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.
89 Evaluation of developmental toxicity using undifferentiated human embryonic stem cells. J Appl Toxicol. 2015 Feb;35(2):205-18.
90 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.
91 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.
92 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.
93 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
94 Characterization of multidrug transporter-mediated efflux of avermectins in human and mouse neuroblastoma cell lines. Toxicol Lett. 2015 Jun 15;235(3):189-98. doi: 10.1016/j.toxlet.2015.04.005. Epub 2015 Apr 9.
95 Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
96 Methotrexate normalizes up-regulated folate pathway genes in rheumatoid arthritis. Arthritis Rheum. 2013 Nov;65(11):2791-802.
97 Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression. Toxicology. 2002 Feb 28;171(2-3):137-46.
98 Enhanced in vitro invasiveness and drug resistance with altered gene expression patterns in a human lung carcinoma cell line after pulse selection with anticancer drugs. Int J Cancer. 2004 Sep 10;111(4):484-93. doi: 10.1002/ijc.20230.
99 Clinical determinants of response to irinotecan-based therapy derived from cell line models. Clin Cancer Res. 2008 Oct 15;14(20):6647-55.
100 Co-encapsulation of chrysophsin-1 and epirubicin in PEGylated liposomes circumvents multidrug resistance in HeLa cells. Chem Biol Interact. 2015 Dec 5;242:13-23. doi: 10.1016/j.cbi.2015.08.023. Epub 2015 Sep 1.
101 Upregulation of multi drug resistance genes in doxorubicin resistant human acute myelogeneous leukemia cells and reversal of the resistance. Hematology. 2007 Dec;12(6):511-7. doi: 10.1080/10245330701562535.
102 Functional analysis of MRP1 cloned from bovine. FEBS Lett. 2002 Jun 19;521(1-3):211-3. doi: 10.1016/s0014-5793(02)02816-8.
103 Functional defect caused by the 4544G>A SNP in ABCC2: potential impact for drug cellular disposition. Pharmacogenet Genomics. 2011 Dec;21(12):884-93. doi: 10.1097/FPC.0b013e32834d672b.
104 Role of multidrug resistance protein 2 (MRP2, ABCC2) in alkylating agent detoxification: MRP2 potentiates glutathione S-transferase A1-1-mediated resistance to chlorambucil cytotoxicity. J Pharmacol Exp Ther. 2004 Jan;308(1):260-7. doi: 10.1124/jpet.103.057729. Epub 2003 Oct 20.
105 MRP2 (ABCC2) transports taxanes and confers paclitaxel resistance and both processes are stimulated by probenecid. Int J Cancer. 2005 Sep 20;116(5):824-9. doi: 10.1002/ijc.21013.
106 Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci. 2008 May;99(5):967-72.
107 In vitro study of transporters involved in intestinal absorption of inorganic arsenic. Chem Res Toxicol. 2012 Feb 20;25(2):446-53. doi: 10.1021/tx200491f. Epub 2012 Jan 26.
108 Potency of individual bile acids to regulate bile acid synthesis and transport genes in primary human hepatocyte cultures. Toxicol Sci. 2014 Oct;141(2):538-46. doi: 10.1093/toxsci/kfu151. Epub 2014 Jul 23.
109 Evaluation of drug transporters' significance for multidrug resistance in head and neck squamous cell carcinoma. Head Neck. 2011 Jul;33(7):959-68. doi: 10.1002/hed.21559. Epub 2010 Aug 24.
110 Multidrug resistance protein-6 (MRP6) in human dermal fibroblasts. Comparison between cells from normal subjects and from Pseudoxanthoma elasticum patients. Matrix Biol. 2003 Nov;22(6):491-500. doi: 10.1016/j.matbio.2003.09.001.
111 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.
112 Expression of the human ABCC6 gene is induced by retinoids through the retinoid X receptor. Biochem Biophys Res Commun. 2006 Dec 1;350(4):1082-7. doi: 10.1016/j.bbrc.2006.10.007. Epub 2006 Oct 10.
113 Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.