Details of the Drug Combination

General Information of Drug Combination (ID: DCESN2X)

Drug Combination Name
Gefitinib Dactinomycin
Indication
Disease Entry Status REF
High grade ovarian serous adenocarcinoma Investigative [1]
Component Drugs Gefitinib   DM15F0X Dactinomycin   DM2YGNW
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL is unavailable
High-throughput Screening Result Testing Cell Line: OVCAR-5
Zero Interaction Potency (ZIP) Score: 8.23
Bliss Independence Score: 11.21
Loewe Additivity Score: 11.47
LHighest Single Agent (HSA) Score: 10.74

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Gefitinib
Disease Entry ICD 11 Status REF
Colon adenocarcinoma N.A. Approved [2]
Glioblastoma 2A00 Approved [2]
Lung cancer 2C25.0 Approved [2]
Non-small-cell lung cancer 2C25.Y Approved [2]
Rectal adenocarcinoma 2B92 Approved [2]
Rectum mucinous adenocarcinoma N.A. Approved [2]
Solid tumour/cancer 2A00-2F9Z Approved [3]
Head and neck cancer 2D42 Phase 3 [3]
Urethral cancer 2C93 Phase 2 [3]
Colon cancer 2B90.Z Investigative [2]
Colon mucinous adenocarcinoma N.A. Investigative [2]
Gefitinib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [11]
------------------------------------------------------------------------------------
Gefitinib Interacts with 4 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [12]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [13]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [14]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [14]
------------------------------------------------------------------------------------
Gefitinib Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [15]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [16]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [15]
------------------------------------------------------------------------------------
Gefitinib Interacts with 64 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Increases ADR [17]
Sulfhydryl oxidase 1 (QSOX1) OT4ZPK4P QSOX1_HUMAN Increases Expression [18]
Growth arrest and DNA damage-inducible protein GADD45 gamma (GADD45G) OT8V1J4M GA45G_HUMAN Decreases Expression [18]
Interferon alpha-inducible protein 6 (IFI6) OTWOOAM4 IFI6_HUMAN Decreases Expression [18]
Fibroblast growth factor 6 (FGF6) OTRJ679P FGF6_HUMAN Increases Expression [18]
Ski oncogene (SKI) OT4KJ8F6 SKI_HUMAN Increases Expression [18]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Decreases Expression [18]
Tumor necrosis factor receptor superfamily member 1B (TNFRSF1B) OTDS2EAR TNR1B_HUMAN Decreases Expression [18]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [18]
Replication protein A 70 kDa DNA-binding subunit (RPA1) OT76POLP RFA1_HUMAN Increases Expression [18]
Adenosine receptor A1 (ADORA1) OTI7X39E AA1R_HUMAN Decreases Expression [18]
14-3-3 protein sigma (SFN) OTLJCZ1U 1433S_HUMAN Decreases Expression [18]
Glycine--tRNA ligase (GARS1) OT5B6R9Y GARS_HUMAN Increases Expression [18]
Epidermal growth factor receptor substrate 15 (EPS15) OT7NPP8U EPS15_HUMAN Increases Expression [18]
Neural retina-specific leucine zipper protein (NRL) OT65MFKQ NRL_HUMAN Decreases Expression [18]
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-2 (GNB2) OT3JPRCQ GBB2_HUMAN Decreases Expression [18]
Retinal guanylyl cyclase 1 (GUCY2D) OT81UJI0 GUC2D_HUMAN Decreases Expression [18]
Cell growth regulator with RING finger domain protein 1 (CGRRF1) OTLMNRCL CGRF1_HUMAN Increases Expression [18]
Dual specificity protein phosphatase 9 (DUSP9) OTZZWEQL DUS9_HUMAN Decreases Expression [18]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [19]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Decreases Expression [20]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [21]
Ubiquitin-like modifier-activating enzyme ATG7 (ATG7) OTVT4YA1 ATG7_HUMAN Increases Expression [22]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [23]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Decreases Phosphorylation [24]
HLA class II histocompatibility antigen, DO alpha chain (HLA-DOA) OTZE5Q7R DOA_HUMAN Affects Expression [25]
Heat shock protein HSP 90-alpha (HSP90AA1) OTLG1WPK HS90A_HUMAN Increases Secretion [26]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [27]
C-C motif chemokine 2 (CCL2) OTAD2HEL CCL2_HUMAN Increases Secretion [28]
DnaJ homolog subfamily B member 1 (DNAJB1) OTCOSEVH DNJB1_HUMAN Increases Secretion [26]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Expression [29]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Expression [29]
G1/S-specific cyclin-D3 (CCND3) OTNKPQ22 CCND3_HUMAN Decreases Expression [30]
HLA class I histocompatibility antigen, alpha chain F (HLA-F) OT76CM19 HLAF_HUMAN Affects Expression [25]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Decreases Expression [21]
Cyclin-dependent kinase 4 inhibitor B (CDKN2B) OTAG24N1 CDN2B_HUMAN Increases Expression [23]
Mitogen-activated protein kinase 8 (MAPK8) OTEREYS5 MK08_HUMAN Decreases Phosphorylation [7]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [30]
Tumor necrosis factor ligand superfamily member 6 (FASLG) OTZARCHH TNFL6_HUMAN Increases Response To Substance [31]
Cytochrome c (CYCS) OTBFALJD CYC_HUMAN Affects Localization [27]
Transcription factor E2F1 (E2F1) OTLKYBBC E2F1_HUMAN Decreases Expression [32]
Kelch-like ECH-associated protein 1 (KEAP1) OTFHOD0C KEAP1_HUMAN Increases Expression [33]
MHC class I polypeptide-related sequence B (MICB) OTS2DVDW MICB_HUMAN Increases Expression [34]
MHC class I polypeptide-related sequence A (MICA) OTPEIEAR MICA_HUMAN Increases Expression [34]
Major histocompatibility complex class I-related gene protein (MR1) OTZU3XX7 HMR1_HUMAN Affects Expression [25]
Autophagy protein 5 (ATG5) OT4T5SMS ATG5_HUMAN Increases Expression [22]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [35]
MARVEL domain-containing protein 1 (MARVELD1) OT5CPOJE MALD1_HUMAN Decreases Response To Substance [36]
Zinc finger protein SNAI2 (SNAI2) OT7Y8EJ2 SNAI2_HUMAN Affects Response To Substance [37]
Membrane-associated progesterone receptor component 1 (PGRMC1) OTBE6WAC PGRC1_HUMAN Decreases Response To Substance [38]
RNA-binding protein 7 (RBM7) OTFIWTMF RBM7_HUMAN Affects Response To Substance [39]
Cell death regulator Aven (AVEN) OTGIN5YK AVEN_HUMAN Affects Response To Substance [39]
Forkhead box protein O3 (FOXO3) OTHXQG4P FOXO3_HUMAN Increases Response To Substance [40]
Phospholipase B-like 1 (PLBD1) OTHYEB4W PLBL1_HUMAN Affects Response To Substance [39]
Securin (PTTG1) OTIMYS4W PTTG1_HUMAN Decreases Response To Substance [27]
Pleckstrin homology-like domain family A member 2 (PHLDA2) OTMV9DPP PHLA2_HUMAN Affects Response To Substance [39]
DNA excision repair protein ERCC-1 (ERCC1) OTNPYQHI ERCC1_HUMAN Affects Response To Substance [10]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Response To Substance [41]
Ceramide transfer protein (CERT1) OTNUCNHX CERT_HUMAN Affects Response To Substance [39]
Dual specificity protein phosphatase 3 (DUSP3) OTPJX9B4 DUS3_HUMAN Affects Response To Substance [39]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Response To Substance [42]
Pericentrin (PCNT) OTW4Z65J PCNT_HUMAN Decreases Response To Substance [38]
Coronin-1C (CORO1C) OTXDF9T3 COR1C_HUMAN Affects Response To Substance [39]
Ribonucleoside-diphosphate reductase large subunit (RRM1) OTXGQOR9 RIR1_HUMAN Affects Response To Substance [10]
------------------------------------------------------------------------------------
⏷ Show the Full List of 64 DOT(s)
Indication(s) of Dactinomycin
Disease Entry ICD 11 Status REF
Adult kidney Wilms tumor N.A. Approved [4]
Advanced cancer 2A00-2F9Z Approved [4]
Beckwith-Wiedemann syndrome N.A. Approved [4]
Childhood kidney Wilms tumor N.A. Approved [4]
Gestational trophoblastic neoplasia 2F33-2F76 Approved [4]
Hamartoma N.A. Approved [4]
Solid tumour/cancer 2A00-2F9Z Approved [5]
Wilms tumor N.A. Approved [4]
Dactinomycin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human Deoxyribonucleic acid (hDNA) TTUTN1I NOUNIPROTAC Breaker [46]
------------------------------------------------------------------------------------
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 [47]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [48]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [49]
------------------------------------------------------------------------------------
Dactinomycin Interacts with 58 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Decreases Response To Substance [50]
Dihydropyrimidinase-related protein 4 (DPYSL4) OT3SBS2S DPYL4_HUMAN Increases Expression [43]
Integral membrane protein GPR137B (GPR137B) OT1CINQQ G137B_HUMAN Increases Expression [43]
Integrin alpha-IIb (ITGA2B) OT4Y17PY ITA2B_HUMAN Increases Expression [43]
Ras-related protein R-Ras (RRAS) OTBBF28C RRAS_HUMAN Increases Expression [43]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [43]
Stomatin (STOM) OTC8R6EH STOM_HUMAN Increases Expression [43]
Cellular retinoic acid-binding protein 2 (CRABP2) OTY01V9G RABP2_HUMAN Increases Expression [43]
Tyrosine-protein kinase receptor UFO (AXL) OTKA2SUX UFO_HUMAN Increases Expression [43]
14-3-3 protein sigma (SFN) OTLJCZ1U 1433S_HUMAN Increases Expression [43]
Tumor necrosis factor ligand superfamily member 9 (TNFSF9) OTV9L89D TNFL9_HUMAN Increases Expression [43]
Galectin-7 (LGALS7) OTMSVI7R LEG7_HUMAN Increases Expression [43]
Large ribosomal subunit protein eL34 (RPL34) OT0U9VMQ RL34_HUMAN Increases Expression [43]
Rho GDP-dissociation inhibitor 2 (ARHGDIB) OT9PD6CS GDIR2_HUMAN Increases Expression [43]
Epithelial membrane protein 1 (EMP1) OTSZHUHQ EMP1_HUMAN Increases Expression [43]
Epithelial membrane protein 3 (EMP3) OTODMJ1D EMP3_HUMAN Increases Expression [43]
Protein ripply3 (RIPPLY3) OT1HK35I DSCR6_HUMAN Increases Expression [43]
Endonuclease III-like protein 1 (NTHL1) OTPQXPT1 NTH_HUMAN Decreases Expression [43]
Kinesin-like protein KIF1A (KIF1A) OT3JVEGV KIF1A_HUMAN Increases Expression [43]
Protein AF1q (MLLT11) OTG5RVHC AF1Q_HUMAN Increases Expression [43]
Laminin subunit gamma-2 (LAMC2) OTJMTM72 LAMC2_HUMAN Increases Expression [43]
Filamin-C (FLNC) OT3F8J6Y FLNC_HUMAN Increases Expression [43]
Immediate early response gene 5 protein (IER5) OTJPTXMD IER5_HUMAN Increases Expression [43]
Keratin, type II cytoskeletal 80 (KRT80) OTAU54U3 K2C80_HUMAN Increases Expression [43]
All-trans-retinol 13,14-reductase (RETSAT) OTC3AOPX RETST_HUMAN Increases Expression [43]
Interleukin-27 receptor subunit alpha (IL27RA) OTSQBAKI I27RA_HUMAN Increases Expression [43]
Neuropilin and tolloid-like protein 2 (NETO2) OT0YAMC0 NETO2_HUMAN Increases Expression [43]
Mitochondria-eating protein (SPATA18) OTOEHTHU MIEAP_HUMAN Increases Expression [43]
Phospholipase ABHD3 (ABHD3) OTH8P977 ABHD3_HUMAN Increases Expression [43]
Homer protein homolog 3 (HOMER3) OTQ6D9X1 HOME3_HUMAN Increases Expression [43]
BSD domain-containing protein 1 (BSDC1) OT853CP9 BSDC1_HUMAN Increases Expression [43]
Stathmin-3 (STMN3) OT20F289 STMN3_HUMAN Increases Expression [43]
Endothelial protein C receptor (PROCR) OTRHED17 EPCR_HUMAN Increases Expression [43]
Fatty acid desaturase 3 (FADS3) OT9RVXGE FADS3_HUMAN Increases Expression [43]
Protein O-mannosyl-transferase 1 (POMT1) OTGQSHL5 POMT1_HUMAN Increases Expression [43]
Tumor protein p53-inducible protein 11 (TP53I11) OTFPDYZU P5I11_HUMAN Decreases Expression [51]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Decreases Expression [52]
CASP8 and FADD-like apoptosis regulator (CFLAR) OTX14BAS CFLAR_HUMAN Decreases Expression [53]
Mitogen-activated protein kinase kinase kinase 7 (MAP3K7) OTUXEASC M3K7_HUMAN Decreases Expression [54]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [54]
Collagen alpha-1(I) chain (COL1A1) OTI31178 CO1A1_HUMAN Decreases Expression [55]
Proto-oncogene tyrosine-protein kinase ROS (ROS1) OTDSKUGE ROS1_HUMAN Increases Expression [54]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Increases Expression [56]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [57]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Decreases Expression [54]
Lamin-B1 (LMNB1) OT100T3P LMNB1_HUMAN Decreases Expression [54]
rRNA 2'-O-methyltransferase fibrillarin (FBL) OTRODIE5 FBRL_HUMAN Affects Localization [58]
DNA-directed RNA polymerase II subunit RPB1 (POLR2A) OTHJQ1DZ RPB1_HUMAN Decreases Phosphorylation [59]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Decreases Expression [60]
Dual specificity mitogen-activated protein kinase kinase 4 (MAP2K4) OTZPZX11 MP2K4_HUMAN Decreases Expression [54]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [61]
Son of sevenless homolog 1 (SOS1) OTTCWXC3 SOS1_HUMAN Decreases Expression [54]
FAS-associated death domain protein (FADD) OTV7GFHH FADD_HUMAN Decreases Expression [54]
Growth arrest-specific protein 6 (GAS6) OTPOPUUE GAS6_HUMAN Increases Degradation [62]
Bcl-2-binding component 3, isoforms 3/4 (BBC3) OTUAXDAY BBC3B_HUMAN Increases Expression [63]
Transcription factor SOX-17 (SOX17) OT9H4WWE SOX17_HUMAN Decreases Localization [35]
Hyaluronidase-1 (HYAL1) OT2SJN0X HYAL1_HUMAN Increases ADR [64]
Complement component 1 Q subcomponent-binding protein, mitochondrial (C1QBP) OTPYQX3K C1QBP_HUMAN Decreases Response To Substance [65]
------------------------------------------------------------------------------------
⏷ Show the Full List of 58 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Adenocarcinoma DCZJYWW DU-145 Investigative [1]
Adenocarcinoma DCDTVQD OVCAR3 Investigative [1]
Adenocarcinoma DCD6SV0 A549 Investigative [1]
Adenocarcinoma DC1AVS1 NCIH23 Investigative [1]
Adenocarcinoma DCSPJG1 HT29 Investigative [1]
Adenocarcinoma DCHSZQ1 HCT116 Investigative [1]
Adenocarcinoma DCIH5KN HCT-15 Investigative [1]
Adenocarcinoma DCOBCXC HCC-2998 Investigative [1]
Adenocarcinoma DC23JHU SW-620 Investigative [1]
Adult acute myeloid leukemia DCNFDGX HL-60(TB) Investigative [1]
Adult T acute lymphoblastic leukemia DCNPB7T MOLT-4 Investigative [1]
Amelanotic melanoma DCPQA58 MDA-MB-435 Investigative [1]
Amelanotic melanoma DCD04G4 M14 Investigative [1]
Anaplastic large cell lymphoma DCNNHH3 SR Investigative [1]
Astrocytoma DCXCTN6 U251 Investigative [1]
Astrocytoma DCMP4I7 SNB-19 Investigative [1]
Childhood T acute lymphoblastic leukemia DCXUN37 CCRF-CEM Investigative [1]
Chronic myelogenous leukemia DC6JKOJ K-562 Investigative [1]
Clear cell renal cell carcinoma DCCA14W A498 Investigative [1]
Clear cell renal cell carcinoma DCHIEML 786-0 Investigative [1]
Clear cell renal cell carcinoma DCX0IJY TK-10 Investigative [1]
Clear cell renal cell carcinoma DCHEKA6 CAKI-1 Investigative [1]
Cutaneous melanoma DCWH58V SK-MEL-28 Investigative [1]
Cutaneous melanoma DCV43UF SK-MEL-5 Investigative [1]
Glioma DCEVRV0 SF-295 Investigative [1]
Glioma DCE293G SF-268 Investigative [1]
Glioma DCLL7CU SF-539 Investigative [1]
High grade ovarian serous adenocarcinoma DCNN452 OVCAR-8 Investigative [1]
High grade ovarian serous adenocarcinoma DCVL31D OVCAR-4 Investigative [1]
Large cell lung carcinoma DCRH1T7 NCI-H460 Investigative [1]
Lung adenocarcinoma DC191W0 HOP-62 Investigative [1]
Lung adenocarcinoma DCD9SER MDA-MB-231 Investigative [1]
Lung adenocarcinoma DCVTZLI NCI-H522 Investigative [1]
Malignant melanoma DCL9SEI LOX IMVI Investigative [1]
Malignant melanoma DCXS3QO UACC62 Investigative [1]
Melanoma DC40PR3 MALME-3M Investigative [1]
Melanoma DCDGENV UACC-257 Investigative [1]
Melanoma DCX00O2 SK-MEL-2 Investigative [1]
Minimally invasive lung adenocarcinoma DCD8PRJ NCI-H322M Investigative [1]
Mixed endometrioid and clear cell carcinoma DCR7BXB IGROV1 Investigative [1]
Non-small cell lung carcinoma DC6E349 HOP-92 Investigative [1]
Ovarian serous cystadenocarcinoma DC579FP SK-OV-3 Investigative [1]
Papillary renal cell carcinoma DCWVN3U ACHN Investigative [1]
Plasma cell myeloma DCX59FM RPMI-8226 Investigative [1]
Pleural epithelioid mesothelioma DC46KCT NCI-H226 Investigative [1]
Prostate carcinoma DCMQDPJ PC-3 Investigative [1]
Renal cell carcinoma DCZLV8N UO-31 Investigative [1]
Renal cell carcinoma DC100Z8 SN12C Investigative [1]
Breast adenocarcinoma DCOCZA2 MDA-MB-468 Investigative [66]
Carcinoma DCZVP6W RXF 393 Investigative [66]
Carcinoma DCKLLD9 MCF7 Investigative [66]
Colon adenocarcinoma DCJ60LW COLO 205 Investigative [66]
Colon carcinoma DCAIFIO KM12 Investigative [66]
Invasive ductal carcinoma DCNVGBP BT-549 Investigative [66]
Invasive ductal carcinoma DCGNPVV T-47D Investigative [66]
Invasive ductal carcinoma DCP78ZD HS 578T Investigative [66]
------------------------------------------------------------------------------------
⏷ Show the Full List of 56 DrugCom(s)

References

1 CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1125966
2 Gefitinib FDA Label
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: 4941).
4 Dactinomycin FDA Label
5 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050682.
6 Synergistic antitumor effect of S-1 and the epidermal growth factor receptor inhibitor gefitinib in non-small cell lung cancer cell lines: role of gefitinib-induced down-regulation of thymidylate synthase. Mol Cancer Ther. 2008 Mar;7(3):599-606.
7 Frankincense myrrh attenuates hepatocellular carcinoma by regulating tumor blood vessel development through multiple epidermal growth factor receptor-mediated signaling pathways. World J Gastrointest Oncol. 2022 Feb 15;14(2):450-477. doi: 10.4251/wjgo.v14.i2.450.
8 EGFR inhibitors enhanced the susceptibility to NK cell-mediated lysis of lung cancer cells. J Immunother. 2011 May;34(4):372-81. doi: 10.1097/CJI.0b013e31821b724a.
9 Overcoming acquired resistance of gefitinib in lung cancer cells without T790M by AZD9291 or Twist1 knockdown in vitro and in vivo. Arch Toxicol. 2019 Jun;93(6):1555-1571. doi: 10.1007/s00204-019-02453-2. Epub 2019 Apr 16.
10 DNA repair gene polymorphisms and benefit from gefitinib in never-smokers with lung adenocarcinoma. Cancer. 2011 Jul 15;117(14):3201-8. doi: 10.1002/cncr.25863. Epub 2011 Jan 24.
11 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
12 Gefitinib-phenytoin interaction is not correlated with the C-erythromycin breath test in healthy male volunteers. Br J Clin Pharmacol. 2009 Aug;68(2):226-37.
13 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.
14 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
15 Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007 Jun 15;13(12):3731-7.
16 Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clin Pharmacokinet. 2005;44(10):1067-81.
17 Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. J Natl Cancer Inst. 2006 Dec 6;98(23):1739-42.
18 Identification of genes linked to gefitinib treatment in prostate cancer cell lines with or without resistance to androgen: a clue to application of gefitinib to hormone-resistant prostate cancer. Oncol Rep. 2006 Jun;15(6):1453-60.
19 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.
20 Effects and mechanisms of betulinic acid on improving EGFR TKI-resistance of lung cancer cells. Environ Toxicol. 2018 Nov;33(11):1153-1159.
21 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.
22 EGFR tyrosine kinase inhibitors activate autophagy as a cytoprotective response in human lung cancer cells. PLoS One. 2011;6(6):e18691. doi: 10.1371/journal.pone.0018691. Epub 2011 Jun 2.
23 ZD1839 induces p15INK4b and causes G1 arrest by inhibiting the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway. Mol Cancer Ther. 2007 May;6(5):1579-87. doi: 10.1158/1535-7163.MCT-06-0814.
24 Epidermal growth factor receptor activity determines response of colorectal cancer cells to gefitinib alone and in combination with chemotherapy. Clin Cancer Res. 2005 Oct 15;11(20):7480-9. doi: 10.1158/1078-0432.CCR-05-0328.
25 Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. Chem Res Toxicol. 2015 May 18;28(5):927-34. doi: 10.1021/tx5005248. Epub 2015 Apr 3.
26 Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction. J Toxicol Sci. 2020;45(11):673-680. doi: 10.2131/jts.45.673.
27 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.
28 Crosstalk between alveolar macrophages and alveolar epithelial cells/fibroblasts contributes to the pulmonary toxicity of gefitinib. Toxicol Lett. 2021 Mar 1;338:1-9. doi: 10.1016/j.toxlet.2020.11.011. Epub 2020 Nov 25.
29 Growth of hormone-dependent MCF-7 breast cancer cells is promoted by constitutive caveolin-1 whose expression is lost in an EGF-R-mediated manner during development of tamoxifen resistance. Breast Cancer Res Treat. 2010 Feb;119(3):575-91. doi: 10.1007/s10549-009-0355-8. Epub 2009 Mar 15.
30 Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
31 The anti-cancer drug gefitinib accelerates Fas-mediated apoptosis by enhancing caspase-8 activation in cancer cells. J Toxicol Sci. 2019;44(6):435-440. doi: 10.2131/jts.44.435.
32 Antiproliferative effects of gefitinib are associated with suppression of E2F-1 expression and telomerase activity. Anticancer Res. 2006 Sep-Oct;26(5A):3387-91.
33 Nrf2 but not autophagy inhibition is associated with the survival of wild-type epidermal growth factor receptor non-small cell lung cancer cells. Toxicol Appl Pharmacol. 2016 Nov 1;310:140-149. doi: 10.1016/j.taap.2016.09.010. Epub 2016 Sep 14.
34 Susceptibility to natural killer cell-mediated lysis of colon cancer cells is enhanced by treatment with epidermal growth factor receptor inhibitors through UL16-binding protein-1 induction. Cancer Sci. 2012 Jan;103(1):7-16. doi: 10.1111/j.1349-7006.2011.02109.x. Epub 2011 Nov 15.
35 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.
36 Inhibition of SREBP increases gefitinib sensitivity in non-small cell lung cancer cells. Oncotarget. 2016 Aug 9;7(32):52392-52403.
37 Slug confers resistance to the epidermal growth factor receptor tyrosine kinase inhibitor. Am J Respir Crit Care Med. 2011 Apr 15;183(8):1071-9. doi: 10.1164/rccm.201009-1440OC. Epub 2010 Oct 29.
38 Identification of protein expression alterations in gefitinib-resistant human lung adenocarcinoma: PCNT and mPR play key roles in the development of gefitinib-associated resistance. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):359-73. doi: 10.1016/j.taap.2015.08.008. Epub 2015 Aug 20.
39 Prediction of sensitivity of advanced non-small cell lung cancers to gefitinib (Iressa, ZD1839). Hum Mol Genet. 2004 Dec 15;13(24):3029-43. doi: 10.1093/hmg/ddh331. Epub 2004 Oct 20.
40 The transcription factor FOXO3a is a crucial cellular target of gefitinib (Iressa) in breast cancer cells. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3169-79. doi: 10.1158/1535-7163.MCT-07-0507.
41 BIM induction of apoptosis triggered by EGFR-sensitive and resistance cell lines of non-small-cell lung cancer. Med Oncol. 2011 Jun;28(2):572-7. doi: 10.1007/s12032-010-9470-y. Epub 2010 Mar 17.
42 Aurora-A promotes gefitinib resistance via a NF-B signaling pathway in p53 knockdown lung cancer cells. Biochem Biophys Res Commun. 2011 Feb 11;405(2):168-72. doi: 10.1016/j.bbrc.2011.01.001. Epub 2011 Jan 7.
43 Genomic profiling uncovers a molecular pattern for toxicological characterization of mutagens and promutagens in vitro. Toxicol Sci. 2011 Jul;122(1):185-97.
44 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.
45 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.
46 Structural studies of atom-specific anticancer drugs acting on DNA. Pharmacol Ther. 1999 Sep;83(3):181-215.
47 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.
48 Potential role of drug transporters in the pathogenesis of medically intractable epilepsy. Epilepsia. 2005 Feb;46(2):224-35.
49 Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. Mol Pharmacol. 2003 Jan;63(1):65-72.
50 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.
51 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.
52 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.
53 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.
54 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.
55 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.
56 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.
57 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.
58 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.
59 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.
60 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.
61 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.
62 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.
63 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.
64 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.
65 [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.
66 CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1126165