General Information of Drug (ID: DMEK4TJ)

Drug Name
PI-103 Drug Info
Synonyms
PI-103; 371935-74-9; PI103; 3-(4-morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol; UNII-YQX02F616F; PI 103; PIK-103; Phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-; YQX02F616F; CHEBI:90524; AK163162; 3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol; 3-(4-Morpholin-4-Ylpyrido[3',2':4,5]furo[3,2-D]pyrimidin-2-Yl)phenol; Phenol, 3-(4-(4-morpholinyl)pyrido(3',2':4,5)furo(3,2-d)pyrimidin-2-yl)-; 3-(4-(4-Morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol
Indication
Disease Entry ICD 11 Status REF
Haematological malignancy 2B33.Y Investigative [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
9884685
ChEBI ID
CHEBI:90524
CAS Number
CAS 371935-74-9
TTD Drug ID
DMEK4TJ

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting PI3-kinase gamma (PIK3CG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [7]
IPI-145 DMWA24P Follicular lymphoma 2A80 Approved [8]
Buparlisib DM1WEHC Breast cancer 2C60-2C65 Phase 3 [9]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [10]
Rigosertib DMOSTXF Myelodysplastic syndrome 2A37 Phase 3 [11]
GDC-0032 DMT4QHD Breast cancer 2C60-2C65 Phase 3 [10]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [12]
SAR245409 DMQM7IL Solid tumour/cancer 2A00-2F9Z Phase 2 [13]
XL147 DMML7BE Solid tumour/cancer 2A00-2F9Z Phase 2 [13]
SF1126 DML10K3 Head and neck cancer 2D42 Phase 2 [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [15]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [16]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [17]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [18]
Cepharanthine DM9Y5JB N. A. N. A. Approved [19]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [20]
Clozapine DMFC71L Schizophrenia 6A20 Approved [21]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [22]
Trifluoperazine DMKBYWI Anxiety Approved [23]
Olanzapine DMPFN6Y Bipolar depression Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [24]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [25]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [26]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [27]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [28]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Verapamil DMA7PEW Angina pectoris BA40 Approved [30]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [31]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [32]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [33]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [34]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [36]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [32]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [37]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [38]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [39]
Gefitinib DM15F0X Colon adenocarcinoma Approved [40]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [41]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [43]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [44]
Paclitaxel DMLB81S Breast carcinoma Approved [45]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [46]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [34]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [28]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [47]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [32]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [48]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [49]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [50]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [33]
Gefitinib DM15F0X Colon adenocarcinoma Approved [51]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [52]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [53]
Selenium DM25CGV N. A. N. A. Approved [54]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [55]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [56]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [57]
Folic Acid DMEMBJC Colorectal carcinoma Approved [58]
Methotrexate DM2TEOL Anterior urethra cancer Approved [59]
Quercetin DM3NC4M Obesity 5B81 Approved [60]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [61]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [62]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [63]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [64]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [65]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [65]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [66]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [67]
Selenium DM25CGV N. A. N. A. Approved [54]
Quercetin DM3NC4M Obesity 5B81 Approved [68]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [69]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [70]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [71]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [72]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [73]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [74]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [66]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [75]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [76]
Ethacrynic acid DM60QMR Edema MG29 Approved [77]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [78]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [79]
Testosterone DM7HUNW Hot flushes GA30 Approved [80]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [81]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [74]
Menthol DMG2KW7 Back pain ME84.Z Approved [82]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Bcl-2-like protein 1 (BCL2L1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [50]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [83]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [84]
Selenium DM25CGV N. A. N. A. Approved [54]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [85]
Methotrexate DM2TEOL Anterior urethra cancer Approved [86]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [87]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [88]
Quercetin DM3NC4M Obesity 5B81 Approved [89]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [90]
⏷ 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 [32]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [91]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [92]
Methotrexate DM2TEOL Anterior urethra cancer Approved [93]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [94]
Quercetin DM3NC4M Obesity 5B81 Approved [95]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [96]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [91]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [97]
Ethacrynic acid DM60QMR Edema MG29 Approved [98]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [99]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [100]
Prednisone DM2HG4X Acute asthma CA23 Approved [101]
Triamterene DM2HU9I Congestive heart failure BD10 Approved [101]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [102]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [103]
Epinephrine DM3KJBC Acute asthma CA23 Approved [104]
Quercetin DM3NC4M Obesity 5B81 Approved [95]
Fluoxetine DM3PD2C Bipolar depression Approved [105]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [106]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Carbonic anhydrase 9 (CA9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetazolamide DM1AF5U Absence epilepsy Approved [107]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [102]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [108]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [109]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [110]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [111]
Ampicillin DMHWE7P Acute epiglottitis Approved [112]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [113]
Bortezomib DMNO38U Leukemia Approved [114]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [115]
⏷ 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
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [3]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [4]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Gene/Protein Processing [3]
Carbonic anhydrase 9 (CA9) OTNA51XT CAH9_HUMAN Post-Translational Modifications [5]
Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) OT4Y9NQI MP2K1_HUMAN Post-Translational Modifications [6]
Dual specificity mitogen-activated protein kinase kinase 2 (MAP2K2) OTUE7Z91 MP2K2_HUMAN Post-Translational Modifications [6]
Hypoxia-inducible factor 1-alpha (HIF1A) OTADSC03 HIF1A_HUMAN Post-Translational Modifications [5]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Gene/Protein Processing [3]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [6]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [6]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5701).
2 The PI3K/Akt pathway as a target in the treatment of hematologic malignancies. Anticancer Agents Med Chem. 2009 Jun;9(5):550-9.
3 The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of sorafenib-treated melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61. doi: 10.1002/ijc.24926.
4 PI3K inhibition enhances doxorubicin-induced apoptosis in sarcoma cells. PLoS One. 2012;7(12):e52898. doi: 10.1371/journal.pone.0052898. Epub 2012 Dec 31.
5 GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1 (HIF-1) pathways. J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. doi: 10.1210/jc.2011-1426. Epub 2011 Oct 12.
6 PI-103 and sorafenib inhibit hepatocellular carcinoma cell proliferation by blocking Ras/Raf/MAPK and PI3K/AKT/mTOR pathways. Anticancer Res. 2010 Dec;30(12):4951-8.
7 BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines and xenograft models.Mol Cancer Ther.2013 Nov;12(11):2319-30.
8 PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
9 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
11 Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
12 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2155).
13 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2156).
14 An integrin-targeted, pan-isoform, phosphoinositide-3 kinase inhibitor, SF1126, has activity against multiple myeloma in vivo.Cancer Chemother Pharmacol.2013 Apr;71(4):867-81.
15 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
16 Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
17 Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
18 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
19 Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
20 Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
21 Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
22 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
23 Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.
24 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.
25 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.
26 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.
27 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.
28 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.
29 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.
30 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.
31 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.
32 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.
33 -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.
34 Treatment with anticancer agents induces dysregulation of specific Wnt signaling pathways in human ovarian luteinized granulosa cells in vitro. Toxicol Sci. 2013 Nov;136(1):183-92. doi: 10.1093/toxsci/kft175. Epub 2013 Aug 16.
35 Progesterone increases csk homologous kinase in HMC-1560 human mast cells and reduces cell proliferation. J Cell Biochem. 2007 Dec 1;102(5):1271-80. doi: 10.1002/jcb.21357.
36 Cannabidiol upregulates melanogenesis through CB1 dependent pathway by activating p38 MAPK and p42/44 MAPK. Chem Biol Interact. 2017 Aug 1;273:107-114. doi: 10.1016/j.cbi.2017.06.005. Epub 2017 Jun 7.
37 Growth stimulation of human pulmonary adenocarcinoma cells and small airway epithelial cells by beta-carotene via activation of cAMP, PKA, CREB and ERK1/2. Int J Cancer. 2006 Mar 15;118(6):1370-80. doi: 10.1002/ijc.21537.
38 Estrogen and pure antiestrogen fulvestrant (ICI 182 780) augment cell-matrigel adhesion of MCF-7 breast cancer cells through a novel G protein coupled estrogen receptor (GPR30)-to-calpain signaling axis. Toxicol Appl Pharmacol. 2014 Mar 1;275(2):176-81. doi: 10.1016/j.taap.2014.01.005. Epub 2014 Jan 17.
39 Inhibition of activator protein 1 by barbiturates is mediated by differential effects on mitogen-activated protein kinases and the small G proteins ras and rac-1. J Pharmacol Exp Ther. 2004 Dec;311(3):1232-40. doi: 10.1124/jpet.104.071332. Epub 2004 Jul 19.
40 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.
41 Effect of histamine H1 receptor antagonists on TARC/CCL17 and MDC/CCL22 production from CD14+ cells induced by antigenic stimulation in vitro. Int Arch Allergy Immunol. 2011;155(1):38-51. doi: 10.1159/000318720. Epub 2010 Nov 25.
42 SIRT3 Mediates the Antioxidant Effect of Hydrogen Sulfide in Endothelial Cells. Antioxid Redox Signal. 2016 Feb 20;24(6):329-43. doi: 10.1089/ars.2015.6331. Epub 2015 Nov 10.
43 Downregulation of mitogen-activated protein kinases (MAPKs) in chronic ethanol-induced fatty liver. Toxicol Mech Methods. 2020 Jul;30(6):407-416. doi: 10.1080/15376516.2020.1747126. Epub 2020 Apr 1.
44 A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling. Proc Natl Acad Sci U S A. 2007 Oct 16;104(42):16657-62. doi: 10.1073/pnas.0707936104. Epub 2007 Oct 9.
45 The stent-eluting drugs sirolimus and paclitaxel suppress healing of the endothelium by induction of autophagy. Am J Pathol. 2009 Nov;175(5):2226-34.
46 Modulation of apoptosis in HaCaT keratinocytes via differential regulation of ERK signaling pathway by flavonoids. J Biol Chem. 2005 Sep 9;280(36):31498-507. doi: 10.1074/jbc.M505537200. Epub 2005 Jul 13.
47 Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
48 Inhibition of cholesterol metabolism underlies synergy between mTOR pathway inhibition and chloroquine in bladder cancer cells. Oncogene. 2016 Aug 25;35(34):4518-28. doi: 10.1038/onc.2015.511. Epub 2016 Feb 8.
49 Nicotine-induced survival signaling in lung cancer cells is dependent on their p53 status while its down-regulation by curcumin is independent. Mol Cancer. 2010 Aug 20;9:220.
50 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.
51 Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
52 Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 2009 Aug;110(2):376-88. doi: 10.1093/toxsci/kfp101. Epub 2009 May 18.
53 Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2015 Mar;35(3):1063-76. doi: 10.1111/liv.12626. Epub 2014 Jul 30.
54 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.
55 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
56 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
57 Characterization of multidrug transporter-mediated efflux of avermectins in human and mouse neuroblastoma cell lines. Toxicol Lett. 2015 Jun 15;235(3):189-98. doi: 10.1016/j.toxlet.2015.04.005. Epub 2015 Apr 9.
58 Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
59 Methotrexate normalizes up-regulated folate pathway genes in rheumatoid arthritis. Arthritis Rheum. 2013 Nov;65(11):2791-802.
60 Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression. Toxicology. 2002 Feb 28;171(2-3):137-46.
61 Enhanced in vitro invasiveness and drug resistance with altered gene expression patterns in a human lung carcinoma cell line after pulse selection with anticancer drugs. Int J Cancer. 2004 Sep 10;111(4):484-93. doi: 10.1002/ijc.20230.
62 Clinical determinants of response to irinotecan-based therapy derived from cell line models. Clin Cancer Res. 2008 Oct 15;14(20):6647-55.
63 Co-encapsulation of chrysophsin-1 and epirubicin in PEGylated liposomes circumvents multidrug resistance in HeLa cells. Chem Biol Interact. 2015 Dec 5;242:13-23. doi: 10.1016/j.cbi.2015.08.023. Epub 2015 Sep 1.
64 Upregulation of multi drug resistance genes in doxorubicin resistant human acute myelogeneous leukemia cells and reversal of the resistance. Hematology. 2007 Dec;12(6):511-7. doi: 10.1080/10245330701562535.
65 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.
66 Cannabidiol and Oxygen-Ozone Combination Induce Cytotoxicity in Human Pancreatic Ductal Adenocarcinoma Cell Lines. Cancers (Basel). 2020 Sep 27;12(10):2774. doi: 10.3390/cancers12102774.
67 trans-Resveratrol inhibits H2O2-induced adenocarcinoma gastric cells proliferation via inactivation of MEK1/2-ERK1/2-c-Jun signalling axis. Biochem Pharmacol. 2009 Feb 1;77(3):337-47. doi: 10.1016/j.bcp.2008.10.034. Epub 2008 Nov 6.
68 Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.
69 Regulation of genistein-induced differentiation in human acute myeloid leukaemia cells (HL60, NB4) Protein kinase modulation and reactive oxygen species generation. Biochem Pharmacol. 2009 Feb 1;77(3):384-96. doi: 10.1016/j.bcp.2008.10.035. Epub 2008 Nov 6.
70 Apoptosis induced by arsenic trioxide in leukemia U937 cells is dependent on activation of p38, inactivation of ERK and the Ca2+-dependent production of superoxide. Int J Cancer. 2001 May 15;92(4):518-26. doi: 10.1002/ijc.1220.
71 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.
72 Cannabis-induced cytotoxicity in leukemic cell lines: the role of the cannabinoid receptors and the MAPK pathway. Blood. 2005 Feb 1;105(3):1214-21. doi: 10.1182/blood-2004-03-1182. Epub 2004 Sep 28.
73 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
74 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.
75 Inhibition of phosphatidylinostol 3-kinase uncouples H2O2-induced senescent phenotype and cell cycle arrest in normal human diploid fibroblasts. Exp Cell Res. 2004 Aug 1;298(1):188-96. doi: 10.1016/j.yexcr.2004.04.012.
76 Combination of all-trans retinoic acid and paclitaxel-induced differentiation and apoptosis in human glioblastoma U87MG xenografts in nude mice. Cancer. 2008 Feb 1;112(3):596-607. doi: 10.1002/cncr.23223.
77 Characterization of cell death induced by ethacrynic acid in a human colon cancer cell line DLD-1 and suppression by N-acetyl-L-cysteine. Cancer Sci. 2003 Oct;94(10):886-93.
78 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.
79 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.
80 Dominant roles of the Raf/MEK/ERK pathway in cell cycle progression, prevention of apoptosis and sensitivity to chemotherapeutic drugs. Cell Cycle. 2010 Apr 15;9(8):1629-38. doi: 10.4161/cc.9.8.11487. Epub 2010 Apr 15.
81 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
82 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.
83 Expression of the retinoic acid-metabolizing enzyme CYP26A1 limits programmed cell death. Mol Pharmacol. 2005 May;67(5):1808-17. doi: 10.1124/mol.104.005769. Epub 2005 Feb 9.
84 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.
85 Role of BAX in the apoptotic response to anticancer agents. Science. 2000 Nov 3;290(5493):989-92. doi: 10.1126/science.290.5493.989.
86 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
87 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.
88 Simvastatin induces apoptosis in human colon cancer cells and in tumor xenografts, and attenuates colitis-associated colon cancer in mice. Int J Cancer. 2008 Aug 15;123(4):951-7. doi: 10.1002/ijc.23593.
89 Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
90 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
91 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
92 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.
93 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.
94 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.
95 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.
96 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.
97 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.
98 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.
99 Cannabidiol disrupts apoptosis, autophagy and invasion processes of placental trophoblasts. Arch Toxicol. 2021 Oct;95(10):3393-3406. doi: 10.1007/s00204-021-03122-z. Epub 2021 Jul 24.
100 AMP-activated protein kinase activity is required for vanadate-induced hypoxia-inducible factor 1alpha expression in DU145 cells. Carcinogenesis. 2004 Dec;25(12):2497-507. doi: 10.1093/carcin/bgh253. Epub 2004 Aug 5.
101 Identification of chemical compounds that induce HIF-1alpha activity. Toxicol Sci. 2009 Nov;112(1):153-63.
102 NO-sulindac inhibits the hypoxia response of PC-3 prostate cancer cells via the Akt signalling pathway. Int J Cancer. 2009 Jan 1;124(1):223-32. doi: 10.1002/ijc.23934.
103 Simvastatin stimulates vascular endothelial growth factor production by hypoxia-inducible factor-1alpha upregulation in endothelial cells. J Cardiovasc Pharmacol. 2008 Mar;51(3):267-73. doi: 10.1097/FJC.0b013e3181624b44.
104 Epinephrine facilitates the growth of T cell lymphoma by altering cell proliferation, apoptosis, and glucose metabolism. Chem Biol Interact. 2023 Jan 5;369:110278. doi: 10.1016/j.cbi.2022.110278. Epub 2022 Nov 22.
105 Screening autism-associated environmental factors in differentiating human neural progenitors with fractional factorial design-based transcriptomics. Sci Rep. 2023 Jun 29;13(1):10519. doi: 10.1038/s41598-023-37488-0.
106 SU5416 inhibited VEGF and HIF-1alpha expression through the PI3K/AKT/p70S6K1 signaling pathway. Biochem Biophys Res Commun. 2004 Nov 12;324(2):471-80. doi: 10.1016/j.bbrc.2004.09.082.
107 Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. J Med Chem. 2011 Oct 13;54(19):6905-18.
108 Synergistic effects of arsenic trioxide and silibinin on apoptosis and invasion in human glioblastoma U87MG cell line. Neurochem Res. 2012 Feb;37(2):370-80. doi: 10.1007/s11064-011-0620-1. Epub 2011 Oct 4.
109 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.
110 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
111 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.
112 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.
113 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
114 A phase II trial with pharmacodynamic endpoints of the proteasome inhibitor bortezomib in patients with metastatic colorectal cancer. Clin Cancer Res. 2005 Aug 1;11(15):5526-33. doi: 10.1158/1078-0432.CCR-05-0081.
115 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.