General Information of Drug (ID: DMUNJZB)

Drug Name
UCN-01 Drug Info
Synonyms
UCN; UCN01; Ucn 01; KRX-0601; KW-2401; UCN-02; (5s,6r,7r,9r,16r)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-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-14-one; 7-Hydroxystaurosporine; 7-hydroxystaurosporine (UCN-01)
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Phase 2 [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
72271
CAS Number
CAS 112953-11-4
TTD Drug ID
DMUNJZB
VARIDT Drug ID
DR01437

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Approved Drug(s)
Drug(s) Targeting Checkpoint kinase-1 (CHK1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LY2603618 DMCXRZF Pancreatic cancer 2C10 Phase 2 [10]
SCH-900776 DM67EMK Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
LY2606368 DM4XMF7 Ovarian cancer 2C73 Phase 2 [12]
LY2880070 DMADEHZ Solid tumour/cancer 2A00-2F9Z Phase 1/2 [13]
RG7741 DMK6P9J Lymphoma 2A80-2A86 Phase 1 [14]
GDC-0425 DMDZ26X Lymphoma 2A80-2A86 Phase 1 [15]
AZD7762 DM1FW0C Solid tumour/cancer 2A00-2F9Z Phase 1 [16]
MK-8776 DMAS1RB Hodgkin lymphoma 2B30 Phase 1 [17]
Diamidothiazole derivative 1 DM02V5Q N. A. N. A. Patented [18]
XL844 DMHTG38 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [19]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [20]
Methotrexate DM2TEOL Anterior urethra cancer Approved [21]
Folic Acid DMEMBJC Colorectal carcinoma Approved [22]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [23]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [25]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [26]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [25]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [27]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [28]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [29]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [30]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [31]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [32]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [33]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [34]
Amiloride DMRTSGP Congestive heart failure BD10 Approved [35]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [36]
Carbamazepine DMZOLBI Epilepsy 8A60-8A68 Approved [33]
Paclitaxel DMLB81S Breast carcinoma Approved [37]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [38]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [39]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [40]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [41]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [42]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [43]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [44]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [45]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [46]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [47]
⏷ 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 [48]
Quercetin DM3NC4M Obesity 5B81 Approved [49]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [50]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [51]
Panobinostat DM58WKG Chronic graft versus host disease Approved [52]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [53]
Leflunomide DMR8ONJ Arthritis FA20 Approved [54]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [44]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [32]
Capsaicin DMGMF6V Back pain ME84.Z Approved [55]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [56]
Quercetin DM3NC4M Obesity 5B81 Approved [57]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [39]
Testosterone DM7HUNW Hot flushes GA30 Approved [58]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [58]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [59]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [44]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [32]
Capsaicin DMGMF6V Back pain ME84.Z Approved [60]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [61]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Floxuridine DM04LR2 Colorectal cancer 2B91.Z Approved [62]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [63]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [64]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [65]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [66]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [67]
Testosterone DM7HUNW Hot flushes GA30 Approved [58]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [58]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [44]
Capsaicin DMGMF6V Back pain ME84.Z Approved [68]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [69]
Methotrexate DM2TEOL Anterior urethra cancer Approved [70]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [71]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [72]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [73]
Paclitaxel DMLB81S Breast carcinoma Approved [74]
Floxuridine DM04LR2 Colorectal cancer 2B91.Z Approved [75]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [76]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [77]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [78]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indomethacin DMSC4A7 Bursitis Approved [79]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [80]
Gefitinib DM15F0X Colon adenocarcinoma Approved [81]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [82]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [83]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [84]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [85]
Methotrexate DM2TEOL Anterior urethra cancer Approved [86]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [87]
Quercetin DM3NC4M Obesity 5B81 Approved [88]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Transcription factor Sp1 (SP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fructose DM43AN2 Vomiting MD90 Approved [89]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [90]
Quercetin DM3NC4M Obesity 5B81 Approved [91]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [92]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [93]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [94]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y Approved [95]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [90]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [96]
Plicamycin DM7C8YV Hypercalcaemia 5B91.0 Approved [97]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [98]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [99]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [100]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [101]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [89]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [102]
Verapamil DMA7PEW Angina pectoris BA40 Approved [103]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [104]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [105]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [106]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [105]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [107]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [108]
Methotrexate DM2TEOL Anterior urethra cancer Approved [109]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [110]
Quercetin DM3NC4M Obesity 5B81 Approved [111]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [112]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [107]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [113]
Ethacrynic acid DM60QMR Edema MG29 Approved [114]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Selenium DM25CGV N. A. N. A. Approved [115]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [116]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [117]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [118]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [119]
Menthol DMG2KW7 Back pain ME84.Z Approved [120]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [121]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [122]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [123]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [124]
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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 [102]
Gefitinib DM15F0X Colon adenocarcinoma Approved [125]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [126]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [127]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [128]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [129]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [128]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [130]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [131]
Methotrexate DM2TEOL Anterior urethra cancer Approved [132]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [133]
Gefitinib DM15F0X Colon adenocarcinoma Approved [134]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [135]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [127]
Etretinate DM2CZFA Keratosis ED56 Approved [136]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [137]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [138]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [139]
Quercetin DM3NC4M Obesity 5B81 Approved [140]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [141]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Checkpoint kinase-1 (CHK1) TTTU902 CHK1_HUMAN Inhibitor [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
3-phosphoinositide-dependent protein kinase 1 (PDPK1) OTT09ZVP PDPK1_HUMAN Gene/Protein Processing [4]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [5]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Drug Response [6]
BAG family molecular chaperone regulator 1 (BAG1) OTRQNIA4 BAG1_HUMAN Gene/Protein Processing [5]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Gene/Protein Processing [7]
E3 ubiquitin-protein ligase XIAP OT24GP9B XIAP_HUMAN Gene/Protein Processing [5]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Gene/Protein Processing [5]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Drug Response [8]
Protein kinase C alpha type (PRKCA) OT5UWNRD KPCA_HUMAN Gene/Protein Processing [4]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Gene/Protein Processing [9]

References

1 ClinicalTrials.gov (NCT00082017) UCN-01 (7-Hydroxystaurosporine) to Treat Relapsed T-Cell Lymphomas. U.S. National Institutes of Health.
2 Characterization of an inhibitory dynamic pharmacophore for the ERCC1-XPA interaction using a combined molecular dynamics and virtual screening app... J Mol Graph Model. 2009 Sep;28(2):113-30.
3 Pharmacogenomic importance of ABCG2. Pharmacogenomics. 2008 Aug;9(8):1005-9.
4 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
5 Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia. Blood. 2000 Jul 15;96(2):393-7.
6 A study of cytotoxic synergy of UCN-01 and flavopiridol in syngeneic pair of cell lines. Invest New Drugs. 2005 Aug;23(4):299-309. doi: 10.1007/s10637-005-1438-y.
7 UCN-01 induces cytotoxicity toward human CLL cells through a p53-independent mechanism. Exp Hematol. 2001 Jun;29(6):703-8. doi: 10.1016/s0301-472x(01)00649-x.
8 The PARP inhibitor PJ34 causes a PARP1-independent, p21 dependent mitotic arrest. DNA Repair (Amst). 2011 Oct 10;10(10):1003-13. doi: 10.1016/j.dnarep.2011.07.006. Epub 2011 Aug 12.
9 The expression of retinoblastoma and Sp1 is increased by low concentrations of cyclin-dependent kinase inhibitors. Eur J Biochem. 2003 Dec;270(24):4809-22. doi: 10.1046/j.1432-1033.2003.03874.x.
10 Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26.
11 Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602.
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 A phase Ib study of oral Chk1 inhibitor LY2880070 in combination with gemcitabine in patients with advanced or metastatic cancer. Journal of Clinical Oncology 38, no. 15_suppl (May 20, 2020) 3581-3581.
14 National Cancer Institute Drug Dictionary (drug id 730054).
15 Quantitative assessment of BCL-2:BIM complexes as a pharmacodynamic marker for venetoclax (ABT-199).
16 Clinical pipeline report, company report or official report of AstraZeneca (2009).
17 Chk1 Inhibitor MK-8776 Restores the Sensitivity of Chemotherapeutics in P-glycoprotein Overexpressing Cancer Cells. Int J Mol Sci. 2019 Aug 22;20(17):4095.
18 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
19 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
20 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
21 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
22 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
23 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
24 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
25 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
26 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
27 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
28 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
29 Arsenic trioxide inhibits translation of mRNA of bcr-abl, resulting in attenuation of Bcr-Abl levels and apoptosis of human leukemia cells. Cancer Res. 2003 Nov 15;63(22):7950-8.
30 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
31 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
32 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.
33 Drug-induced endoplasmic reticulum and oxidative stress responses independently sensitize toward TNF-mediated hepatotoxicity. Toxicol Sci. 2014 Jul;140(1):144-59. doi: 10.1093/toxsci/kfu072. Epub 2014 Apr 20.
34 Mechanism of cisplatin proximal tubule toxicity revealed by integrating transcriptomics, proteomics, metabolomics and biokinetics. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):117-27.
35 Role of HER-2/neu signaling in sensitivity to tumor necrosis factor-related apoptosis-inducing ligand: enhancement of TRAIL-mediated apoptosis by amiloride. J Cell Biochem. 2005 Oct 1;96(2):376-89. doi: 10.1002/jcb.20512.
36 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.
37 Differential roles of phosphoinositide-dependent protein kinase-1 and akt1 expression and phosphorylation in breast cancer cell resistance to Paclitaxel, Doxorubicin, and gemcitabine. Mol Pharmacol. 2006 Sep;70(3):1045-52. doi: 10.1124/mol.106.023333. Epub 2006 Jun 16.
38 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.
39 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.
40 Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63. doi: 10.1021/jm2007613. Epub 2011 Aug 18.
41 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.
42 Expression profile analysis of human peripheral blood mononuclear cells in response to aspirin. Arch Immunol Ther Exp (Warsz). 2005 Mar-Apr;53(2):151-8.
43 Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo. Blood. 2004 Aug 15;104(4):1094-9. doi: 10.1182/blood-2003-12-4266. Epub 2004 Apr 20.
44 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.
45 LSD1 activates a lethal prostate cancer gene network independently of its demethylase function. Proc Natl Acad Sci U S A. 2018 May 1;115(18):E4179-E4188.
46 Sorafenib induces cell death in chronic lymphocytic leukemia by translational downregulation of Mcl-1. Leukemia. 2011 May;25(5):838-47. doi: 10.1038/leu.2011.2. Epub 2011 Feb 4.
47 Molecular mechanism of action of bisphenol and bisphenol A mediated by oestrogen receptor alpha in growth and apoptosis of breast cancer cells. Br J Pharmacol. 2013 May;169(1):167-78.
48 Activation of ERK1/2 by protein kinase C-alpha in response to hydrogen peroxide-induced cell death in human gingival fibroblasts. Toxicol In Vitro. 2010 Feb;24(1):319-26. doi: 10.1016/j.tiv.2009.08.007. Epub 2009 Aug 21.
49 Anticarcinogenic action of quercetin by downregulation of phosphatidylinositol 3-kinase (PI3K) and protein kinase C (PKC) via induction of p53 in hepatocellular carcinoma (HepG2) cell line. Mol Biol Rep. 2015 Sep;42(9):1419-29. doi: 10.1007/s11033-015-3921-7. Epub 2015 Aug 27.
50 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
51 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.
52 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.
53 Genomic and proteomic analysis of the effects of cannabinoids on normal human astrocytes. Brain Res. 2008 Jan 29;1191:1-11.
54 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
55 The vanilloid capsaicin induces IL-6 secretion in prostate PC-3 cancer cells. Cytokine. 2011 Jun;54(3):330-7. doi: 10.1016/j.cyto.2011.03.010. Epub 2011 Apr 6.
56 Sertraline induces endoplasmic reticulum stress in hepatic cells. Toxicology. 2014 Aug 1;322:78-88. doi: 10.1016/j.tox.2014.05.007. Epub 2014 May 24.
57 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.
58 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
59 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.
60 A comparative proteomic analysis for capsaicin-induced apoptosis between human hepatocarcinoma (HepG2) and human neuroblastoma (SK-N-SH) cells. Proteomics. 2008 Nov;8(22):4748-67. doi: 10.1002/pmic.200800094.
61 Extremely low copper concentrations affect gene expression profiles of human prostate epithelial cell lines. Chem Biol Interact. 2010 Oct 6;188(1):214-9.
62 Checkpoint signaling, base excision repair, and PARP promote survival of colon cancer cells treated with 5-fluorodeoxyuridine but not 5-fluorouracil. PLoS One. 2011;6(12):e28862. doi: 10.1371/journal.pone.0028862. Epub 2011 Dec 15.
63 Cannabidiol-induced transcriptomic changes and cellular senescence in human Sertoli cells. Toxicol Sci. 2023 Feb 17;191(2):227-238. doi: 10.1093/toxsci/kfac131.
64 Direct activation of ATM by resveratrol under oxidizing conditions. PLoS One. 2014 Jun 16;9(6):e97969. doi: 10.1371/journal.pone.0097969. eCollection 2014.
65 Long-term exposure to zidovudine delays cell cycle progression, induces apoptosis, and decreases telomerase activity in human hepatocytes. Toxicol Sci. 2009 Sep;111(1):120-30. doi: 10.1093/toxsci/kfp136. Epub 2009 Jun 18.
66 Chronic occupational exposure to arsenic induces carcinogenic gene signaling networks and neoplastic transformation in human lung epithelial cells. Toxicol Appl Pharmacol. 2012 Jun 1;261(2):204-16.
67 Lunasin, a novel seed peptide, sensitizes human breast cancer MDA-MB-231 cells to aspirin-arrested cell cycle and induced apoptosis. Chem Biol Interact. 2010 Jul 30;186(2):127-34. doi: 10.1016/j.cbi.2010.04.027. Epub 2010 May 21.
68 Triggering of transient receptor potential vanilloid type 1 (TRPV1) by capsaicin induces Fas/CD95-mediated apoptosis of urothelial cancer cells in an ATM-dependent manner. Carcinogenesis. 2009 Aug;30(8):1320-9. doi: 10.1093/carcin/bgp138. Epub 2009 Jun 5.
69 p53-R175H mutant gains new function in regulation of doxorubicin-induced apoptosis. Int J Cancer. 2005 Apr 10;114(3):331-6. doi: 10.1002/ijc.20818.
70 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
71 Azidothymidine and cisplatin increase p14ARF expression in OVCAR-3 ovarian cancer cell line. Toxicol Appl Pharmacol. 2006 Oct 1;216(1):89-97. doi: 10.1016/j.taap.2006.04.015. Epub 2006 May 19.
72 Quantitative analysis of gene expression changes in response to genotoxic compounds. Toxicol In Vitro. 2017 Mar;39:15-28. doi: 10.1016/j.tiv.2016.11.004. Epub 2016 Nov 5.
73 Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells. Oncol Res. 2000;12(9-10):397-408. doi: 10.3727/096504001108747855.
74 Gallic acid potentiates the apoptotic effect of paclitaxel and carboplatin via overexpression of Bax and P53 on the MCF-7 human breast cancer cell line. J Biochem Mol Toxicol. 2021 Feb;35(2):e22638. doi: 10.1002/jbt.22638. Epub 2020 Oct 1.
75 Regulation of human dUTPase gene expression and p53-mediated transcriptional repression in response to oxaliplatin-induced DNA damage. Nucleic Acids Res. 2009 Jan;37(1):78-95. doi: 10.1093/nar/gkn910. Epub 2008 Nov 16.
76 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.
77 Nitrogen Mustard Alkylates and Cross-Links p53 in Human Keratinocytes. Chem Res Toxicol. 2022 Apr 18;35(4):636-650. doi: 10.1021/acs.chemrestox.1c00420. Epub 2022 Mar 21.
78 Fulvestrant induces resistance by modulating GPER and CDK6 expression: implication of methyltransferases, deacetylases and the hSWI/SNF chromatin remodelling complex. Br J Cancer. 2013 Nov 12;109(10):2751-62. doi: 10.1038/bjc.2013.583. Epub 2013 Oct 29.
79 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.
80 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.
81 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
82 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.
83 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
84 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.
85 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.
86 Melanoma coordinates general and cell-specific mechanisms to promote methotrexate resistance. Exp Cell Res. 2012 Jun 10;318(10):1146-59.
87 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.
88 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.
89 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.
90 Arsenic trioxide downregulates specificity protein (Sp) transcription factors and inhibits bladder cancer cell and tumor growth. Exp Cell Res. 2010 Aug 1;316(13):2174-88. doi: 10.1016/j.yexcr.2010.04.027. Epub 2010 May 8.
91 Quercetin augments TRAIL-induced apoptotic death: involvement of the ERK signal transduction pathway. Biochem Pharmacol. 2008 May 15;75(10):1946-58. doi: 10.1016/j.bcp.2008.02.016. Epub 2008 Mar 10.
92 Peroxisome proliferator-activated receptor-gamma ligands suppress fibronectin gene expression in human lung carcinoma cells: involvement of both CRE and Sp1. Am J Physiol Lung Cell Mol Physiol. 2005 Sep;289(3):L419-28. doi: 10.1152/ajplung.00002.2005. Epub 2005 May 20.
93 Mechanistic basis for overcoming platinum resistance using copper chelating agents. Mol Cancer Ther. 2012 Nov;11(11):2483-94. doi: 10.1158/1535-7163.MCT-12-0580. Epub 2012 Aug 21.
94 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
95 Regulation of the high-affinity copper transporter (hCtr1) expression by cisplatin and heavy metals. J Biol Inorg Chem. 2014 Jan;19(1):17-27. doi: 10.1007/s00775-013-1051-z. Epub 2013 Oct 17.
96 Thalidomide and a thalidomide analogue inhibit endothelial cell proliferation in vitro. J Neurooncol. 1999 Jun;43(2):109-14. doi: 10.1023/a:1006202700039.
97 The activity of a novel mithramycin analog is related to its binding to DNA, cellular accumulation, and inhibition of Sp1-driven gene transcription. Chem Biol Interact. 2014 Aug 5;219:123-32. doi: 10.1016/j.cbi.2014.05.019. Epub 2014 Jun 4.
98 4.8% sevoflurane induces activation of autophagy in human neuroblastoma SH-SY5Y cells by the AMPK/mTOR signaling pathway. Neurotoxicology. 2022 May;90:256-264. doi: 10.1016/j.neuro.2022.04.008. Epub 2022 Apr 23.
99 Enhanced chemotherapeutic efficacy of docetaxel in human lung cancer cell line via GLUT1 inhibitor. J Biochem Mol Toxicol. 2023 Jun;37(6):e23348. doi: 10.1002/jbt.23348. Epub 2023 Mar 31.
100 Breast cancer cells response to the antineoplastic agents cisplatin, carboplatin, and doxorubicin at the mRNA expression levels of distinct apoptosis-related genes, including the new member, BCL2L12. Ann N Y Acad Sci. 2007 Jan;1095:35-44. doi: 10.1196/annals.1397.005.
101 Extracellular signal-regulated kinase activation and Bcl-2 downregulation mediate apoptosis after gemcitabine treatment partly via a p53-independent pathway. Eur J Pharmacol. 2004 Oct 19;502(3):169-83. doi: 10.1016/j.ejphar.2004.09.006.
102 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.
103 Verapamil potentiates anti-glioblastoma efficacy of temozolomide by modulating apoptotic signaling. Toxicol In Vitro. 2018 Oct;52:306-313. doi: 10.1016/j.tiv.2018.07.001. Epub 2018 Jul 9.
104 Inhibition of caspase-dependent mitochondrial permeability transition protects airway epithelial cells against mustard-induced apoptosis. Apoptosis. 2006 Sep;11(9):1545-59. doi: 10.1007/s10495-006-8764-1.
105 Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
106 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
107 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
108 The role of MITF and Mcl-1 proteins in the antiproliferative and proapoptotic effect of ciprofloxacin in amelanotic melanoma cells: In silico and in vitro study. Toxicol In Vitro. 2020 Aug;66:104884. doi: 10.1016/j.tiv.2020.104884. Epub 2020 May 8.
109 Peripheral blood expression of nuclear factor-kappab-regulated genes is associated with rheumatoid arthritis disease activity and responds differentially to anti-tumor necrosis factor-alpha versus methotrexate. J Rheumatol. 2007 Sep;34(9):1817-22. Epub 2007 Aug 1.
110 Quercetin downregulates Mcl-1 by acting on mRNA stability and protein degradation. Br J Cancer. 2011 Jul 12;105(2):221-30. doi: 10.1038/bjc.2011.229.
111 Multifaceted preventive effects of single agent quercetin on a human prostate adenocarcinoma cell line (PC-3): implications for nutritional transcriptomics and multi-target therapy. Med Oncol. 2011 Dec;28(4):1395-404. doi: 10.1007/s12032-010-9603-3. Epub 2010 Jul 2.
112 D-Penicillamine targets metastatic melanoma cells with induction of the unfolded protein response (UPR) and Noxa (PMAIP1)-dependent mitochondrial apoptosis. Apoptosis. 2012 Oct;17(10):1079-94.
113 Anti-cancer properties of glucosamine-hydrochloride in YD-8 human oral cancer cells: Induction of the caspase-dependent apoptosis and down-regulation of HIF-1. Toxicol In Vitro. 2012 Feb;26(1):42-50. doi: 10.1016/j.tiv.2011.10.005. Epub 2011 Oct 13.
114 Ethacrynic acid and a derivative enhance apoptosis in arsenic trioxide-treated myeloid leukemia and lymphoma cells: the role of glutathione S-transferase p1-1. Clin Cancer Res. 2012 Dec 15;18(24):6690-701. doi: 10.1158/1078-0432.CCR-12-0770. Epub 2012 Oct 18.
115 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.
116 Arsenic trioxide induces different gene expression profiles of genes related to growth and apoptosis in glioma cells dependent on the p53 status. Mol Biol Rep. 2008 Sep;35(3):421-9.
117 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.
118 Apoptosis induction by 1alpha,25-dihydroxyvitamin D3 in prostate cancer. Mol Cancer Ther. 2002 Jul;1(9):667-77.
119 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.
120 Repurposing L-menthol for systems medicine and cancer therapeutics? L-menthol induces apoptosis through caspase 10 and by suppressing HSP90. OMICS. 2016 Jan;20(1):53-64.
121 Effect of zoledronic acid on oral fibroblasts and epithelial cells: a potential mechanism of bisphosphonate-associated osteonecrosis. Br J Haematol. 2009 Mar;144(5):667-76. doi: 10.1111/j.1365-2141.2008.07504.x. Epub 2008 Nov 20.
122 Identification by automated screening of a small molecule that selectively eliminates neural stem cells derived from hESCs but not dopamine neurons. PLoS One. 2009 Sep 23;4(9):e7155.
123 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
124 The thioxotriazole copper(II) complex A0 induces endoplasmic reticulum stress and paraptotic death in human cancer cells. J Biol Chem. 2009 Sep 4;284(36):24306-19.
125 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.
126 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.
127 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.
128 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.
129 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.
130 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.
131 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
132 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.
133 mTOR inhibition reverses acquired endocrine therapy resistance of breast cancer cells at the cell proliferation and gene-expression levels. Cancer Sci. 2008 Oct;99(10):1992-2003. doi: 10.1111/j.1349-7006.2008.00955.x.
134 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.
135 Assessment of the cytotoxic, genotoxic, and apoptotic potential of flurbiprofen in HeLa and HepG2 cell lines. J Biochem Mol Toxicol. 2021 Jun;35(6):1-11. doi: 10.1002/jbt.22770. Epub 2021 Mar 11.
136 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.
137 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
138 Apoptotic induction by simvastatin in human lung cancer A549 cells via Akt signaling dependent down-regulation of survivin. Invest New Drugs. 2011 Oct;29(5):945-52. doi: 10.1007/s10637-010-9450-2. Epub 2010 May 13.
139 Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene. 2005 Sep 15;24(41):6213-21. doi: 10.1038/sj.onc.1208774.
140 Quercetin inhibit human SW480 colon cancer growth in association with inhibition of cyclin D1 and survivin expression through Wnt/beta-catenin signaling pathway. Cancer Invest. 2009 Jul;27(6):604-12. doi: 10.1080/07357900802337191.
141 Troglitazone sensitizes tumor cells to TRAIL-induced apoptosis via down-regulation of FLIP and Survivin. Apoptosis. 2006 Sep;11(9):1503-12. doi: 10.1007/s10495-006-8896-3.