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

General Information of Drug (ID: DMI6E0R)

Drug Name
Midostaurin Drug Info
Synonyms
PKC412; 120685-11-2; Cgp 41251; 4'-N-Benzoylstaurosporine; CGP-41251; Benzoylstaurosporine; PKC-412; RYDAPT; PKC 412; UNII-ID912S5VON; N-Benzoylstaurosporine; ID912S5VON; CHEMBL608533; CHEBI:63452; Cgp 41 251; N-[(5S,6R,7R,9R)-6-methoxy-5-methyl-14-oxo-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-7-yl]-N-methylbenzamide; PKC-412(Midostaurin); Midostaurin (PKC412); Midostaurin (USAN/INN); Midostaurin [USAN:INN]; CGP 41231; Rydapt (TN); CPG 41251
Indication
Disease Entry ICD 11 Status REF
Acute myeloid leukaemia 2A60 Approved [1]
Systemic mastocytosis 2A21.0 Approved [2]
Chronic myelomonocytic leukaemia 2A40 Phase 2 [3]
Colorectal cancer 2B91.Z Phase 1 [3]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
9829523
ChEBI ID
CHEBI:63452
CAS Number
CAS 120685-11-2
TTD Drug ID
DMI6E0R
VARIDT Drug ID
DR01370
INTEDE Drug ID
DR1090
ACDINA Drug ID
D00431

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Protein kinase C gamma (PRKCG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BALANOL DMDLN9E N. A. N. A. Terminated [12]
RO-320432 DMFZ1YW N. A. N. A. Terminated [13]
LY-317644 DMM20PI N. A. N. A. Terminated [14]
RO-316233 DMAGLPW Discovery agent N.A. Investigative [15]
Bisindolylmaleimide-I DMOQJZC Discovery agent N.A. Investigative [16]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione DMDO175 Discovery agent N.A. Investigative [17]
3,4-diphenyl-1H-pyrrole-2,5-dione DMPK6YT Discovery agent N.A. Investigative [17]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione DMGC7RY Discovery agent N.A. Investigative [17]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione DM3EV9N Discovery agent N.A. Investigative [17]
LY-326449 DMN53M4 Discovery agent N.A. Investigative [18]
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Drug(s) Targeting Fms-like tyrosine kinase 3 (FLT-3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [19]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [20]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [21]
Gilteritinib DMTI0ZO Acute myeloid leukaemia 2A60 Approved [22]
Pexidartinib DMS2J0Z Tenosynovial giant cell tumour 2F7B Approved [23]
Pacritinib DM1T6ZN Myelofibrosis 2A20.2 Approved [19]
Quizartinib DM8Y4JS Acute myeloid leukaemia 2A60 Approved [24]
Lestaurtinib DMQ2AIJ Acute myeloid leukaemia 2A60 Approved (orphan drug) [25]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [26]
BMS-690514 DMX302C Chronic pain MG30 Phase 2 [27]
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Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [5]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [28]
Methotrexate DM2TEOL Anterior urethra cancer Approved [29]
Folic Acid DMEMBJC Colorectal carcinoma Approved [30]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [29]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [29]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [31]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [29]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [32]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [33]
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Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [34]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [36]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [37]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [38]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [39]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [40]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [41]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [35]
Verapamil DMA7PEW Angina pectoris BA40 Approved [42]
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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 [43]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [44]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [45]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [46]
Cepharanthine DM9Y5JB N. A. N. A. Approved [47]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [48]
Clozapine DMFC71L Schizophrenia 6A20 Approved [49]
Trifluoperazine DMKBYWI Anxiety Approved [50]
Olanzapine DMPFN6Y Bipolar depression Approved [49]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [46]
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Drug(s) Affected By Receptor-type tyrosine-protein kinase FLT3 (FLT3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quizartinib DM8Y4JS Acute myeloid leukaemia 2A60 Approved [51]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [52]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [53]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [54]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [55]
Venetoclax DM8I94Y Chronic lymphocytic leukaemia 2A82.0 Approved [56]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [57]
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [58]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [59]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [60]
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Drug(s) Affected By Glycophorin-A (GYPA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [61]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [62]
Dihydroartemisinin DMBXVMZ Malaria 1F40-1F45 Approved [63]
Teriflunomide DMQ2FKJ Hyperlipidaemia 5C80 Approved [64]
Arsenic DMTL2Y1 N. A. N. A. Approved [65]
Allopurinol DMLPAOB Gout FA25 Approved [66]
Resveratrol DM3RWXL Giant cell arteritis 4A44.2 Phase 3 [67]
phorbol 12-myristate 13-acetate DMJWD62 Acute myeloid leukaemia 2A60 Phase 2 [68]
APIGENIN DMI3491 Discovery agent N.A. Investigative [69]
Butanoic Acid DMTAJP7 Discovery agent N.A. Investigative [70]
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Drug(s) Affected By Fibroblast growth factor receptor 3 (FGFR3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [71]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [72]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [73]
Panobinostat DM58WKG Chronic graft versus host disease Approved [74]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [75]
Lenalidomide DM6Q7U4 Adult T-cell leukemia/lymphoma Approved [76]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [76]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [77]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [78]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [79]
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Drug(s) Affected By Thrombopoietin receptor (MPL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [80]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [81]
Urethane DM7NSI0 N. A. N. A. Phase 4 [82]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [83]
Milchsaure DM462BT Pruritus EC90 Investigative [84]
Drug(s) Affected By Aldo-keto reductase family 1 member C3 (AKR1C3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [85]
Meclofenamic acid DM05FXR Ankylosing spondylitis FA92.0 Approved [86]
Diazepam DM08E9O Alcohol withdrawal Approved [87]
Levonorgestrel DM1DP7T Atypical endometrial hyperplasia Approved [88]
Desogestrel DM27U4Y Contraception QA21 Approved [88]
Salicyclic acid DM2F8XZ Acne vulgaris ED80 Approved [86]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [86]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [89]
Quercetin DM3NC4M Obesity 5B81 Approved [90]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [91]
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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
Fms-like tyrosine kinase 3 (FLT-3) TTGJCWZ FLT3_HUMAN Inhibitor [4]
Protein kinase C gamma (PRKCG) TTRFOXJ KPCG_HUMAN Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Aldo-keto reductase family 1 member C3 (AKR1C3) OTU2SXBA AK1C3_HUMAN Gene/Protein Processing [7]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [8]
Fibroblast growth factor receptor 3 (FGFR3) OTSAXDIL FGFR3_HUMAN Gene/Protein Processing [9]
Glycophorin-A (GYPA) OTABU4YV GLPA_HUMAN Gene/Protein Processing [10]
Receptor-type tyrosine-protein kinase FLT3 (FLT3) OTMSRYMK FLT3_HUMAN Drug Response [11]
Thrombopoietin receptor (MPL) OTZEN192 TPOR_HUMAN Gene/Protein Processing [10]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018
2 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
3 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: 5702).
4 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
5 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
6 Midostaurin, a novel protein kinase inhibitor for the treatment of acute myelogenous leukemia: insights from human absorption, metabolism, and excretion studies of a BDDCS II drug. Drug Metab Dispos. 2017 May;45(5):540-555.
7 Selective inhibition of aldo-keto reductase 1C3: a novel mechanism involved in midostaurin and daunorubicin synergism. Arch Toxicol. 2021 Jan;95(1):67-78. doi: 10.1007/s00204-020-02884-2. Epub 2020 Oct 6.
8 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
9 FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies. Oncogene. 2005 Dec 15;24(56):8259-67. doi: 10.1038/sj.onc.1208989.
10 Oral small-molecule tyrosine kinase inhibitor midostaurin (PKC412) inhibits growth and induces megakaryocytic differentiation in human leukemia cells. Toxicol In Vitro. 2009 Sep;23(6):979-85. doi: 10.1016/j.tiv.2009.06.027. Epub 2009 Jun 30.
11 Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells. PLoS One. 2011;6(9):e25351. doi: 10.1371/journal.pone.0025351. Epub 2011 Sep 28.
12 Evaluation of differential hypoxic cytotoxicity and electrochemical studies of nitro 5-deazaflavins, Bioorg. Med. Chem. Lett. 5(18):2155-2160 (1995).
13 Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain, Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994).
14 Synthesis of bisindolylmaleimide macrocycles, Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995).
15 Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
16 Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63.
17 Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.
18 (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H... J Med Chem. 1996 Jul 5;39(14):2664-71.
19 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. (Target id: 1807).
20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
21 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
22 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
23 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
24 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
25 Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with ... Blood. 2008 Jun 15;111(12):5663-71.
26 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
27 Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.
28 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
29 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
30 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
31 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
32 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
33 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
34 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
35 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
36 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
37 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
38 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
39 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
40 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
41 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
42 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
43 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
44 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.
45 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.
46 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.
47 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.
48 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.
49 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.
50 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.
51 Inhibitors of class I HDACs and of FLT3 combine synergistically against leukemia cells with mutant FLT3. Arch Toxicol. 2022 Jan;96(1):177-193. doi: 10.1007/s00204-021-03174-1. Epub 2021 Oct 19.
52 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.
53 SU5416, a small molecule tyrosine kinase receptor inhibitor, has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes. Blood. 2003 Aug 1;102(3):795-801. doi: 10.1182/blood-2002-10-3023. Epub 2003 Mar 20.
54 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.
55 Arsenic trioxide affects signal transducer and activator of transcription proteins through alteration of protein tyrosine kinase phosphorylation. Clin Cancer Res. 2006 Nov 15;12(22):6817-25. doi: 10.1158/1078-0432.CCR-06-1354.
56 HSP90 Inhibitor PU-H71 in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. Curr Issues Mol Biol. 2023 Aug 23;45(9):7011-7026. doi: 10.3390/cimb45090443.
57 Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6. Blood. 2016 Jun 9;127(23):2890-902. doi: 10.1182/blood-2015-11-683581. Epub 2016 Apr 20.
58 Dasatinib inhibits the growth of molecularly heterogeneous myeloid leukemias. Clin Cancer Res. 2010 Feb 15;16(4):1149-58. doi: 10.1158/1078-0432.CCR-09-2416. Epub 2010 Feb 9.
59 Neuronal and cardiac toxicity of pharmacological compounds identified through transcriptomic analysis of human pluripotent stem cell-derived embryoid bodies. Toxicol Appl Pharmacol. 2021 Dec 15;433:115792. doi: 10.1016/j.taap.2021.115792. Epub 2021 Nov 3.
60 Low doses of cisplatin induce gene alterations, cell cycle arrest, and apoptosis in human promyelocytic leukemia cells. Biomark Insights. 2016 Aug 24;11:113-21.
61 In vitro dual effect of arsenic trioxide on hemopoiesis: inhibition of erythropoiesis and stimulation of megakaryocytic maturation. Blood Cells Mol Dis. 2006 Jan-Feb;36(1):59-76. doi: 10.1016/j.bcmd.2005.10.005. Epub 2005 Dec 15.
62 Phenolic metabolites of benzene inhibited the erythroid differentiation of K562 cells. Toxicol Lett. 2011 Jun 24;203(3):190-9. doi: 10.1016/j.toxlet.2011.03.012. Epub 2011 Mar 23.
63 Selective toxicity of dihydroartemisinin on human CD34+ erythroid cell differentiation. Toxicology. 2010 Oct 9;276(2):128-34. doi: 10.1016/j.tox.2010.07.016. Epub 2010 Aug 3.
64 A77 1726 induces differentiation of human myeloid leukemia K562 cells by depletion of intracellular CTP pools. Mol Pharmacol. 2002 Sep;62(3):463-72. doi: 10.1124/mol.62.3.463.
65 Increased glycophorin A somatic cell variant frequency in arsenic-exposed patients of Guizhou, China. Toxicol Lett. 2006 Nov 1;167(1):47-53. doi: 10.1016/j.toxlet.2006.08.008. Epub 2006 Sep 1.
66 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.
67 Resveratrol induces human K562 cell apoptosis, erythroid differentiation, and autophagy. Tumour Biol. 2014 Jun;35(6):5381-8. doi: 10.1007/s13277-014-1701-y. Epub 2014 Feb 15.
68 p22phox-dependent NADPH oxidase activity is required for megakaryocytic differentiation. Cell Death Differ. 2010 Dec;17(12):1842-54. doi: 10.1038/cdd.2010.67. Epub 2010 Jun 4.
69 Analysis of the erythroid differentiation effect of flavonoid apigenin on K562 human chronic leukemia cells. Chem Biol Interact. 2014 Sep 5;220:269-77. doi: 10.1016/j.cbi.2014.07.006. Epub 2014 Jul 21.
70 Inhibitory effect of tellimagrandin I on chemically induced differentiation of human leukemia K562 cells. Toxicol Lett. 2004 Mar 1;147(2):109-19. doi: 10.1016/j.toxlet.2003.12.008.
71 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.
72 Retinoic acid receptor alpha amplifications and retinoic acid sensitivity in breast cancers. Clin Breast Cancer. 2013 Oct;13(5):401-8.
73 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.
74 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.
75 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
76 Thalidomide and Its Analogs Differentially Target Fibroblast Growth Factor Receptors: Thalidomide Suppresses FGFR Gene Expression while Pomalidomide Dampens FGFR2 Activity. Chem Res Toxicol. 2019 Apr 15;32(4):589-602. doi: 10.1021/acs.chemrestox.8b00286. Epub 2019 Mar 15.
77 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.
78 Increased expression of fibroblast growth factor receptor 3 in CD34+ BCR-ABL+ cells from patients with chronic myeloid leukemia. Leukemia. 2003 Dec;17(12):2418-25. doi: 10.1038/sj.leu.2403152.
79 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.
80 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
81 Hypomethylation mediated by decreased DNMTs involves in the activation of proto-oncogene MPL in TK6 cells treated with hydroquinone. Toxicol Lett. 2012 Mar 25;209(3):239-45. doi: 10.1016/j.toxlet.2011.12.020. Epub 2012 Jan 8.
82 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
83 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
84 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.
85 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.
86 Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3): role in breast cancer and inhibition by non-steroidal anti-inflammatory drug analogs. Chem Biol Interact. 2009 Mar 16;178(1-3):221-7.
87 Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5.
88 Progestins as inhibitors of the human 20-ketosteroid reductases, AKR1C1 and AKR1C3. Chem Biol Interact. 2011 May 30;191(1-3):227-33.
89 In-vivo effects of simvastatin and rosuvastatin on global gene expression in peripheral blood leucocytes in a human inflammation model. Pharmacogenet Genomics. 2008 Feb;18(2):109-20.
90 AKR1C3 as a potential target for the inhibitory effect of dietary flavonoids. Chem Biol Interact. 2009 Mar 16;178(1-3):138-44.
91 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.