Details of the Drug Combination

General Information of Drug Combination (ID: DCSTMDQ)

Drug Combination Name
Dactinomycin Lapatinib
Indication
Disease Entry Status REF
Renal cell carcinoma Investigative [1]
Component Drugs Dactinomycin   DM2YGNW Lapatinib   DM3BH1Y
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL is unavailable 3D MOL
High-throughput Screening Result Testing Cell Line: SN12C
Zero Interaction Potency (ZIP) Score: 15.06
Bliss Independence Score: 18.36
Loewe Additivity Score: 10.94
LHighest Single Agent (HSA) Score: 15.5

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Dactinomycin
Disease Entry ICD 11 Status REF
Adult kidney Wilms tumor N.A. Approved [2]
Advanced cancer 2A00-2F9Z Approved [2]
Beckwith-Wiedemann syndrome N.A. Approved [2]
Childhood kidney Wilms tumor N.A. Approved [2]
Gestational trophoblastic neoplasia 2F33-2F76 Approved [2]
Hamartoma N.A. Approved [2]
Solid tumour/cancer 2A00-2F9Z Approved [3]
Wilms tumor N.A. Approved [2]
Dactinomycin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human Deoxyribonucleic acid (hDNA) TTUTN1I NOUNIPROTAC Breaker [9]
------------------------------------------------------------------------------------
Dactinomycin Interacts with 3 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [10]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [11]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [12]
------------------------------------------------------------------------------------
Dactinomycin Interacts with 85 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Multidrug resistance-associated protein 1 (ABCC1) OTGUN89S MRP1_HUMAN Decreases Response To Substance [13]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Decreases Response To Substance [14]
Urokinase-type plasminogen activator (PLAU) OTX0QGKK UROK_HUMAN Increases Expression [6]
Dihydropyrimidinase-related protein 4 (DPYSL4) OT3SBS2S DPYL4_HUMAN Increases Expression [6]
Integral membrane protein GPR137B (GPR137B) OT1CINQQ G137B_HUMAN Increases Expression [6]
Integrin alpha-IIb (ITGA2B) OT4Y17PY ITA2B_HUMAN Increases Expression [6]
Ras-related protein R-Ras (RRAS) OTBBF28C RRAS_HUMAN Increases Expression [6]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [6]
Stomatin (STOM) OTC8R6EH STOM_HUMAN Increases Expression [6]
Cellular retinoic acid-binding protein 2 (CRABP2) OTY01V9G RABP2_HUMAN Increases Expression [6]
Tyrosine-protein kinase receptor UFO (AXL) OTKA2SUX UFO_HUMAN Increases Expression [6]
14-3-3 protein sigma (SFN) OTLJCZ1U 1433S_HUMAN Increases Expression [6]
Tumor necrosis factor ligand superfamily member 9 (TNFSF9) OTV9L89D TNFL9_HUMAN Increases Expression [6]
Galectin-7 (LGALS7) OTMSVI7R LEG7_HUMAN Increases Expression [6]
Large ribosomal subunit protein eL34 (RPL34) OT0U9VMQ RL34_HUMAN Increases Expression [6]
Rho GDP-dissociation inhibitor 2 (ARHGDIB) OT9PD6CS GDIR2_HUMAN Increases Expression [6]
Epithelial membrane protein 1 (EMP1) OTSZHUHQ EMP1_HUMAN Increases Expression [6]
Epithelial membrane protein 3 (EMP3) OTODMJ1D EMP3_HUMAN Increases Expression [6]
Protein ripply3 (RIPPLY3) OT1HK35I DSCR6_HUMAN Increases Expression [6]
Endonuclease III-like protein 1 (NTHL1) OTPQXPT1 NTH_HUMAN Decreases Expression [6]
Antigen peptide transporter 1 (TAP1) OTJL27PW TAP1_HUMAN Increases Expression [6]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [6]
Kinesin-like protein KIF1A (KIF1A) OT3JVEGV KIF1A_HUMAN Increases Expression [6]
Protein AF1q (MLLT11) OTG5RVHC AF1Q_HUMAN Increases Expression [6]
Laminin subunit gamma-2 (LAMC2) OTJMTM72 LAMC2_HUMAN Increases Expression [6]
Filamin-C (FLNC) OT3F8J6Y FLNC_HUMAN Increases Expression [6]
Immediate early response gene 5 protein (IER5) OTJPTXMD IER5_HUMAN Increases Expression [6]
Keratin, type II cytoskeletal 80 (KRT80) OTAU54U3 K2C80_HUMAN Increases Expression [6]
All-trans-retinol 13,14-reductase (RETSAT) OTC3AOPX RETST_HUMAN Increases Expression [6]
Interleukin-27 receptor subunit alpha (IL27RA) OTSQBAKI I27RA_HUMAN Increases Expression [6]
Neuropilin and tolloid-like protein 2 (NETO2) OT0YAMC0 NETO2_HUMAN Increases Expression [6]
Mitochondria-eating protein (SPATA18) OTOEHTHU MIEAP_HUMAN Increases Expression [6]
Phospholipase ABHD3 (ABHD3) OTH8P977 ABHD3_HUMAN Increases Expression [6]
Homer protein homolog 3 (HOMER3) OTQ6D9X1 HOME3_HUMAN Increases Expression [6]
BSD domain-containing protein 1 (BSDC1) OT853CP9 BSDC1_HUMAN Increases Expression [6]
Stathmin-3 (STMN3) OT20F289 STMN3_HUMAN Increases Expression [6]
Endothelial protein C receptor (PROCR) OTRHED17 EPCR_HUMAN Increases Expression [6]
Fatty acid desaturase 3 (FADS3) OT9RVXGE FADS3_HUMAN Increases Expression [6]
Protein O-mannosyl-transferase 1 (POMT1) OTGQSHL5 POMT1_HUMAN Increases Expression [6]
Tissue factor (F3) OT3MSU3B TF_HUMAN Decreases Expression [15]
Tumor protein p53-inducible protein 11 (TP53I11) OTFPDYZU P5I11_HUMAN Decreases Expression [16]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Decreases Expression [17]
CASP8 and FADD-like apoptosis regulator (CFLAR) OTX14BAS CFLAR_HUMAN Decreases Expression [18]
Mitogen-activated protein kinase kinase kinase 7 (MAP3K7) OTUXEASC M3K7_HUMAN Decreases Expression [19]
Prominin-1 (PROM1) OTBHV8NX PROM1_HUMAN Decreases Expression [20]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [19]
Low-density lipoprotein receptor (LDLR) OTH559LU LDLR_HUMAN Decreases Expression [21]
Tumor necrosis factor (TNF) OT4IE164 TNFA_HUMAN Increases Response To Substance [22]
Collagen alpha-1(I) chain (COL1A1) OTI31178 CO1A1_HUMAN Decreases Expression [23]
Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) OTBPMIMW G3P_HUMAN Increases Expression [19]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Increases Activity [24]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Decreases Expression [25]
Interleukin-6 (IL6) OTUOSCCU IL6_HUMAN Decreases Secretion [23]
Proto-oncogene tyrosine-protein kinase ROS (ROS1) OTDSKUGE ROS1_HUMAN Increases Expression [19]
Fibroblast growth factor 2 (FGF2) OT7YUJ9F FGF2_HUMAN Decreases Expression [26]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Decreases Expression [27]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Increases Expression [28]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [29]
Endoplasmic reticulum chaperone BiP (HSPA5) OTFUIRAO BIP_HUMAN Decreases Expression [30]
Matrix metalloproteinase-9 (MMP9) OTB2QDAV MMP9_HUMAN Decreases Expression [31]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [20]
CCAAT/enhancer-binding protein beta (CEBPB) OTM9MQIA CEBPB_HUMAN Decreases Expression [19]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Decreases Expression [19]
Lamin-B1 (LMNB1) OT100T3P LMNB1_HUMAN Decreases Expression [19]
rRNA 2'-O-methyltransferase fibrillarin (FBL) OTRODIE5 FBRL_HUMAN Affects Localization [32]
DNA-directed RNA polymerase II subunit RPB1 (POLR2A) OTHJQ1DZ RPB1_HUMAN Decreases Phosphorylation [33]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Decreases Expression [34]
Signal transducer and activator of transcription 1-alpha/beta (STAT1) OTLMBUZ6 STAT1_HUMAN Increases Expression [19]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Decreases Expression [19]
Caspase-2 (CASP2) OTUDYSPP CASP2_HUMAN Increases Cleavage [35]
Dual specificity mitogen-activated protein kinase kinase 4 (MAP2K4) OTZPZX11 MP2K4_HUMAN Decreases Expression [19]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Decreases Expression [19]
DNA repair protein RAD51 homolog 1 (RAD51) OTNVWGC1 RAD51_HUMAN Decreases Expression [36]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [37]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Decreases Expression [38]
Son of sevenless homolog 1 (SOS1) OTTCWXC3 SOS1_HUMAN Decreases Expression [19]
FAS-associated death domain protein (FADD) OTV7GFHH FADD_HUMAN Decreases Expression [19]
Growth arrest-specific protein 6 (GAS6) OTPOPUUE GAS6_HUMAN Increases Degradation [39]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Decreases Expression [19]
Bcl-2-binding component 3, isoforms 3/4 (BBC3) OTUAXDAY BBC3B_HUMAN Increases Expression [29]
Proheparin-binding EGF-like growth factor (HBEGF) OTLU00JS HBEGF_HUMAN Decreases Expression [26]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [40]
Cystine/glutamate transporter (SLC7A11) OTKJ6PXW XCT_HUMAN Decreases Expression [20]
Hyaluronidase-1 (HYAL1) OT2SJN0X HYAL1_HUMAN Increases ADR [41]
Complement component 1 Q subcomponent-binding protein, mitochondrial (C1QBP) OTPYQX3K C1QBP_HUMAN Decreases Response To Substance [42]
------------------------------------------------------------------------------------
⏷ Show the Full List of 85 DOT(s)
Indication(s) of Lapatinib
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [4]
Gastroesophageal junction adenocarcinoma 2B71 Approved [5]
Melanoma 2C30 Approved [5]
Lapatinib Interacts with 3 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Erbb2 tyrosine kinase receptor (HER2) TT6EO5L ERBB2_HUMAN Inhibitor [44]
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [44]
Eukaryotic elongation factor 2 kinase (eEF-2K) TT1QFLA EF2K_HUMAN Inhibitor [45]
------------------------------------------------------------------------------------
Lapatinib Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [46]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [47]
------------------------------------------------------------------------------------
Lapatinib Interacts with 4 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [48]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [49]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [48]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [49]
------------------------------------------------------------------------------------
Lapatinib Interacts with 36 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Activity [50]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [51]
Superoxide dismutase , mitochondrial (SOD2) OTIWXGZ9 SODM_HUMAN Increases Expression [52]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Increases Expression [52]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Increases Expression [52]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Increases Activity [52]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [53]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Decreases Activity [50]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [54]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [55]
DNA topoisomerase 1 (TOP1) OT51O0CF TOP1_HUMAN Decreases Expression [56]
DNA topoisomerase 2-alpha (TOP2A) OT6LPS08 TOP2A_HUMAN Decreases Expression [56]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [56]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [54]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Decreases Activity [57]
Receptor tyrosine-protein kinase erbB-3 (ERBB3) OTRSST0A ERBB3_HUMAN Decreases Activity [58]
Alanine aminotransferase 1 (GPT) OTOXOA0Q ALAT1_HUMAN Increases Secretion [59]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [50]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Activity [54]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Activity [54]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Activity [50]
DNA replication licensing factor MCM7 (MCM7) OT6FXC6K MCM7_HUMAN Decreases Expression [54]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [56]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [50]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Increases Activity [56]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Increases Activity [56]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [55]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [60]
GTPase KRas (KRAS) OT78QCN8 RASK_HUMAN Decreases Response To Substance [61]
HLA class II histocompatibility antigen, DQ alpha 1 chain (HLA-DQA1) OTC6GISG DQA1_HUMAN Increases ADR [62]
Zinc finger protein SNAI1 (SNAI1) OTDPYAMC SNAI1_HUMAN Decreases Response To Substance [63]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Metabolism [56]
Cytochrome P450 3A7 (CYP3A7) OTTCDHHM CP3A7_HUMAN Increases Metabolism [56]
Transforming growth factor beta-1 proprotein (TGFB1) OTV5XHVH TGFB1_HUMAN Decreases Response To Substance [63]
Tenascin-X (TNXB) OTVBWAV5 TENX_HUMAN Increases ADR [62]
HLA class II histocompatibility antigen, DQ beta 1 chain (HLA-DQB1) OTVVI3UI DQB1_HUMAN Increases ADR [62]
------------------------------------------------------------------------------------
⏷ Show the Full List of 36 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Breast adenocarcinoma DCEGI6A MDA-MB-468 Investigative [64]
Carcinoma DC72B95 MCF7 Investigative [64]
Colon carcinoma DCN7ZQY KM12 Investigative [64]
Invasive ductal carcinoma DC3VS3A HS 578T Investigative [64]
Invasive ductal carcinoma DCB3QBD T-47D Investigative [64]
Adenocarcinoma DCY0WYS DU-145 Investigative [1]
Adenocarcinoma DC2GC4U OVCAR3 Investigative [1]
Adenocarcinoma DCRUBNY A549 Investigative [1]
Adenocarcinoma DC01KB0 NCIH23 Investigative [1]
Adenocarcinoma DC5UK6I HT29 Investigative [1]
Adenocarcinoma DCVOYJ1 HCT116 Investigative [1]
Adenocarcinoma DCLRBC3 HCC-2998 Investigative [1]
Adult acute myeloid leukemia DCFSJU5 HL-60(TB) Investigative [1]
Amelanotic melanoma DCHHRYC M14 Investigative [1]
Anaplastic large cell lymphoma DC0I8RR SR Investigative [1]
Astrocytoma DC5QKTX SNB-19 Investigative [1]
Chronic myelogenous leukemia DC53MRX K-562 Investigative [1]
Clear cell renal cell carcinoma DCUWY3F 786-0 Investigative [1]
Clear cell renal cell carcinoma DC18LJG A498 Investigative [1]
Clear cell renal cell carcinoma DCVAOTO CAKI-1 Investigative [1]
Glioblastoma DCYVNN4 SNB-75 Investigative [1]
Glioma DC30J9C SF-539 Investigative [1]
High grade ovarian serous adenocarcinoma DCWGTB4 OVCAR-5 Investigative [1]
High grade ovarian serous adenocarcinoma DCBBQES OVCAR-4 Investigative [1]
High grade ovarian serous adenocarcinoma DCHPYAH NCI\\/ADR-RES Investigative [1]
Lung adenocarcinoma DCTBK26 HOP-62 Investigative [1]
Lung adenocarcinoma DCRW0DN EKVX Investigative [1]
Lung adenocarcinoma DCRWWHI MDA-MB-231 Investigative [1]
Lung adenocarcinoma DCP9HY3 NCI-H522 Investigative [1]
Malignant melanoma DCCGWYK UACC62 Investigative [1]
Malignant melanoma DCJA8U8 LOX IMVI Investigative [1]
Mixed endometrioid and clear cell carcinoma DCF1S8Z IGROV1 Investigative [1]
Non-small cell lung carcinoma DC941RD HOP-92 Investigative [1]
Papillary renal cell carcinoma DCNO2GN ACHN Investigative [1]
Plasma cell myeloma DCW7SEY RPMI-8226 Investigative [1]
Pleural epithelioid mesothelioma DC9XRW4 NCI-H226 Investigative [1]
Renal cell carcinoma DCB6EQB UO-31 Investigative [1]
------------------------------------------------------------------------------------
⏷ Show the Full List of 37 DrugCom(s)

References

1 Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
2 Dactinomycin FDA Label
3 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050682.
4 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: 5692).
5 Lapatinib FDA Label
6 Genomic profiling uncovers a molecular pattern for toxicological characterization of mutagens and promutagens in vitro. Toxicol Sci. 2011 Jul;122(1):185-97.
7 Synergy is achieved by complementation with Apo2L/TRAIL and actinomycin D in Apo2L/TRAIL-mediated apoptosis of prostate cancer cells: role of XIAP in resistance. Prostate. 2002 Dec 1;53(4):286-99. doi: 10.1002/pros.10155.
8 Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells. Toxicol Sci. 2013 Jan;131(1):71-83. doi: 10.1093/toxsci/kfs290. Epub 2012 Oct 10.
9 Structural studies of atom-specific anticancer drugs acting on DNA. Pharmacol Ther. 1999 Sep;83(3):181-215.
10 Expression of multidrug resistance-associated protein in NIH/3T3 cells confers multidrug resistance associated with increased drug efflux and altered intracellular drug distribution. Cancer Res. 1995 Nov 15;55(22):5342-7.
11 Potential role of drug transporters in the pathogenesis of medically intractable epilepsy. Epilepsia. 2005 Feb;46(2):224-35.
12 Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. Mol Pharmacol. 2003 Jan;63(1):65-72.
13 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.
14 Establishment and characterization of new cellular lymphoma model expressing transgenic human MDR1. Leuk Res. 2005 Apr;29(4):407-14. doi: 10.1016/j.leukres.2004.09.001.
15 Mechanisms of tissue factor induction by the uremic toxin indole-3 acetic acid through aryl hydrocarbon receptor/nuclear factor-kappa B signaling pathway in human endothelial cells. Arch Toxicol. 2019 Jan;93(1):121-136.
16 Possible roles of a tumor suppressor gene PIG11 in hepatocarcinogenesis and As2O3-induced apoptosis in liver cancer cells. J Gastroenterol. 2009;44(5):460-9. doi: 10.1007/s00535-009-0030-1. Epub 2009 Apr 1.
17 Death receptor regulation and celecoxib-induced apoptosis in human lung cancer cells. J Natl Cancer Inst. 2004 Dec 1;96(23):1769-80. doi: 10.1093/jnci/djh322.
18 Combination of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) and actinomycin D induces apoptosis even in TRAIL-resistant human pancreatic cancer cells. Clin Cancer Res. 2001 Feb;7(2):407-14.
19 Response rate of fibrosarcoma cells to cytotoxic drugs on the expression level correlates to the therapeutic response rate of fibrosarcomas and is mediated by regulation of apoptotic pathways. BMC Cancer. 2005 Jul 7;5:74. doi: 10.1186/1471-2407-5-74.
20 Actinomycin D inhibits the expression of the cystine/glutamate transporter xCT via attenuation of CD133 synthesis in CD133(+) HCC. Chem Biol Interact. 2019 Aug 25;309:108713. doi: 10.1016/j.cbi.2019.06.026. Epub 2019 Jun 19.
21 Ascorbic acid enhances low-density lipoprotein receptor expression by suppressing proprotein convertase subtilisin/kexin 9 expression. J Biol Chem. 2020 Nov 20;295(47):15870-15882. doi: 10.1074/jbc.RA120.015623. Epub 2020 Sep 10.
22 Heme oxygenase-1-derived carbon monoxide requires the activation of transcription factor NF-kappa B to protect endothelial cells from tumor necrosis factor-alpha-mediated apoptosis. J Biol Chem. 2002 May 17;277(20):17950-61. doi: 10.1074/jbc.M108317200. Epub 2002 Mar 5.
23 The effects of particulate wear debris, cytokines, and growth factors on the functions of MG-63 osteoblasts. J Bone Joint Surg Am. 2001 Feb;83(2):201-11. doi: 10.2106/00004623-200102000-00007.
24 The effect of potent iron chelators on the regulation of p53: examination of the expression, localization and DNA-binding activity of p53 and the transactivation of WAF1. Carcinogenesis. 2003 Oct;24(10):1601-14. doi: 10.1093/carcin/bgg116. Epub 2003 Jul 17.
25 T-2 toxin upregulates the expression of human cytochrome P450 1A1 (CYP1A1) by enhancing NRF1 and Sp1 interaction. Toxicol Lett. 2019 Oct 15;315:77-86. doi: 10.1016/j.toxlet.2019.08.021. Epub 2019 Aug 27.
26 Osmotic Induction of Angiogenic Growth Factor Expression in Human Retinal Pigment Epithelial Cells. PLoS One. 2016 Jan 22;11(1):e0147312. doi: 10.1371/journal.pone.0147312. eCollection 2016.
27 Ammonia promotes endothelial cell survival via the heme oxygenase-1-mediated release of carbon monoxide. Free Radic Biol Med. 2017 Jan;102:37-46. doi: 10.1016/j.freeradbiomed.2016.11.029. Epub 2016 Nov 17.
28 Profiling the immunotoxicity of chemicals based on in vitro evaluation by a combination of the Multi-ImmunoTox assay and the IL-8 Luc assay. Arch Toxicol. 2018 Jun;92(6):2043-2054. doi: 10.1007/s00204-018-2199-7. Epub 2018 Mar 29.
29 Actinomycin D upregulates proapoptotic protein Puma and downregulates Bcl-2 mRNA in normal peripheral blood lymphocytes. Anticancer Drugs. 2007 Aug;18(7):763-72. doi: 10.1097/CAD.0b013e3280adc905.
30 Enhanced GRP78 protein expression via the IRE1/ASK1/p38 MAPK pathway during As(2)O(3)-induced endoplasmic reticulum stress in BEAS-2B cells. Toxicology. 2021 Oct;462:152962. doi: 10.1016/j.tox.2021.152962. Epub 2021 Sep 21.
31 Matrix metalloproteinase-9 is involved in chronic lymphocytic leukemia cell response to fludarabine and arsenic trioxide. PLoS One. 2014 Jun 23;9(6):e99993. doi: 10.1371/journal.pone.0099993. eCollection 2014.
32 Specific inhibition of rRNA transcription and dynamic relocation of fibrillarin induced by mercury. Exp Cell Res. 2000 Aug 25;259(1):225-38. doi: 10.1006/excr.2000.4923.
33 Phosphorylation of the RNA polymerase II largest subunit during heat shock and inhibition of transcription in HeLa cells. J Cell Physiol. 1994 Mar;158(3):417-26. doi: 10.1002/jcp.1041580305.
34 Selective and nonselective toxicity of TRAIL/Apo2L combined with chemotherapy in human bone tumour cells vs. normal human cells. Int J Cancer. 2003 Dec 20;107(6):929-40. doi: 10.1002/ijc.11503.
35 Actinomycin D and staurosporine, potent apoptosis inducers in vitro, are potentially effective chemotherapeutic agents against glioblastoma multiforme. Cancer Chemother Pharmacol. 2000;45(2):149-56. doi: 10.1007/s002800050023.
36 Unpredicted Downregulation of RAD51 Suggests Genome Instability Induced by Tetrachlorobenzoquinone. Chem Res Toxicol. 2016 Dec 19;29(12):2184-2193. doi: 10.1021/acs.chemrestox.6b00369. Epub 2016 Nov 21.
37 Mechanisms of thymidine kinase/ganciclovir and cytosine deaminase/ 5-fluorocytosine suicide gene therapy-induced cell death in glioma cells. Oncogene. 2005 Feb 10;24(7):1231-43. doi: 10.1038/sj.onc.1208290.
38 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.
39 Androgen receptor-dependent transactivation of growth arrest-specific gene 6 mediates inhibitory effects of testosterone on vascular calcification. J Biol Chem. 2010 Mar 5;285(10):7537-44. doi: 10.1074/jbc.M109.055087. Epub 2010 Jan 4.
40 A high-throughput screen for teratogens using human pluripotent stem cells. Toxicol Sci. 2014 Jan;137(1):76-90. doi: 10.1093/toxsci/kft239. Epub 2013 Oct 23.
41 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.
42 [Expression of C1QBP gene and its correlation with drug resistance in human resistance choriocarcinoma cell line]. Zhonghua Fu Chan Ke Za Zhi. 2014 Aug;49(8):616-20.
43 UGT-dependent regioselective glucuronidation of ursodeoxycholic acid and obeticholic acid and selective transport of the consequent acyl glucuronides by OATP1B1 and 1B3. Chem Biol Interact. 2019 Sep 1;310:108745. doi: 10.1016/j.cbi.2019.108745. Epub 2019 Jul 9.
44 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
45 Inhibition of eEF-2 kinase sensitizes human nasopharyngeal carcinoma cells to lapatinib-induced apoptosis through the Src and Erk pathways.BMC Cancer. 2016 Oct 19;16(1):813.
46 Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition.
47 The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Drug Metab Dispos. 2008 Apr;36(4):695-701.
48 Mechanism-based inactivation of cytochrome P450 3A4 by lapatinib. Mol Pharmacol. 2010 Oct;78(4):693-703.
49 Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706.
50 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
51 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
52 P450 3A-catalyzed O-dealkylation of lapatinib induces mitochondrial stress and activates Nrf2. Chem Res Toxicol. 2016 May 16;29(5):784-96.
53 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.
54 CDK4/6 inhibition provides a potent adjunct to Her2-targeted therapies in preclinical breast cancer models. Genes Cancer. 2014 Jul;5(7-8):261-72. doi: 10.18632/genesandcancer.24.
55 Effects of lapatinib on cell proliferation and apoptosis in NB4 cells. Oncol Lett. 2018 Jan;15(1):235-242. doi: 10.3892/ol.2017.7342. Epub 2017 Nov 3.
56 The involvement of hepatic cytochrome P450s in the cytotoxicity of lapatinib. Toxicol Sci. 2023 Dec 21;197(1):69-78. doi: 10.1093/toxsci/kfad099.
57 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
58 Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab. Clin Cancer Res. 2009 Jun 15;15(12):4147-56. doi: 10.1158/1078-0432.CCR-08-2814. Epub 2009 Jun 9.
59 Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes. Toxicol Lett. 2018 Jul;291:138-148. doi: 10.1016/j.toxlet.2018.04.010. Epub 2018 Apr 12.
60 Association of CYP1A1 and CYP1B1 inhibition in in vitro assays with drug-induced liver injury. J Toxicol Sci. 2021;46(4):167-176. doi: 10.2131/jts.46.167.
61 The K-Ras effector p38 MAPK confers intrinsic resistance to tyrosine kinase inhibitors by stimulating EGFR transcription and EGFR dephosphorylation. J Biol Chem. 2017 Sep 8;292(36):15070-15079. doi: 10.1074/jbc.M117.779488. Epub 2017 Jul 24.
62 HLA-DQA1*02:01 is a major risk factor for lapatinib-induced hepatotoxicity in women with advanced breast cancer. J Clin Oncol. 2011 Feb 20;29(6):667-73. doi: 10.1200/JCO.2010.31.3197. Epub 2011 Jan 18.
63 Niclosamide inhibits epithelial-mesenchymal transition and tumor growth in lapatinib-resistant human epidermal growth factor receptor 2-positive breast cancer. Int J Biochem Cell Biol. 2016 Feb;71:12-23. doi: 10.1016/j.biocel.2015.11.014. Epub 2015 Nov 28.
64 Biologically active neutrophil chemokine pattern in tonsillitis.Clin Exp Immunol. 2004 Mar;135(3):511-8. doi: 10.1111/j.1365-2249.2003.02390.x.