General Information of Drug (ID: DMJDVW4)

Drug Name
GSK2816126 Drug Info
Synonyms GSK 126; GSK-126
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
Cross-matching ID
PubChem CID
68210102
ChEBI ID
CHEBI:124921
CAS Number
CAS 1346574-57-9
TTD Drug ID
DMJDVW4

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tazemetostat DMWP1BH Follicular lymphoma 2A80 Approved [6]
DS-3201b DMI69E5 T-cell leukaemia 2A90 Phase 2 [7]
CPI-1205 DM3XWJ8 Prostate cancer 2C82.0 Phase 1/2 [8]
SHR2554 DMMUCH0 Prostate cancer 2C82.0 Phase 1/2 [9]
CPI-0209 DMJEXLI Solid tumour/cancer 2A00-2F9Z Phase 1/2 [10]
DS-3201 DMRLPFG Acute lymphoblastic leukaemia 2A85 Phase 1 [8]
HH2853 DMQIE58 Non-hodgkin lymphoma 2B33.5 Phase 1 [11]
PF-06821497 DML3WT6 Diffuse large B-cell lymphoma 2A81 Phase 1 [12]
PMID28394193-Compound-56 DMQRFZK N. A. N. A. Patented [13]
PMID28394193-Compound-46 DMYMPNA N. A. N. A. Patented [13]
⏷ 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 [14]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [15]
Levonorgestrel DM1DP7T Atypical endometrial hyperplasia Approved [16]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [17]
Methotrexate DM2TEOL Anterior urethra cancer Approved [18]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [19]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [21]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [22]
Panobinostat DM58WKG Chronic graft versus host disease Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [24]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [25]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [26]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [27]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [28]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [22]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [29]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [30]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [31]
Aldosterone DM9S2JW Hypertension BA00-BA04 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [33]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [34]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [35]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [36]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [33]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [38]
Ursodeoxycholic acid DMCUT21 Cholelithiasis DC11 Approved [39]
Fenofibrate DMFKXDY Coronary atherosclerosis Approved [40]
Capsaicin DMGMF6V Back pain ME84.Z Approved [41]
⏷ 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 [42]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [43]
Methotrexate DM2TEOL Anterior urethra cancer Approved [44]
Quercetin DM3NC4M Obesity 5B81 Approved [45]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [46]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [47]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [48]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [49]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [50]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [51]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [52]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [53]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [54]
Calcidiol DMN4CV5 Hypophosphatemia Approved [53]
Magnesium DMU4ORS Ischemic stroke 8B11.5Z Approved [55]
Vitamin C DMXJ7O8 Adenocarcinoma 2D40 Approved [56]
Camptothecin DM6CHNJ Solid tumour/cancer 2A00-2F9Z Phase 3 [57]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [58]
EUGENOL DM7US1H Discovery agent N.A. Patented [59]
alpha-ketoglutaric acid DM5LFYN Discovery agent N.A. Investigative [60]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Homeobox protein MSX-2 (MSX2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [61]
Panobinostat DM58WKG Chronic graft versus host disease Approved [23]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [62]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [38]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [63]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [64]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [65]
Carbamazepine DMZOLBI Epilepsy 8A60-8A68 Approved [66]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [67]
SNDX-275 DMH7W9X Breast cancer 2C60-2C65 Phase 3 [23]
⏷ 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 [68]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [27]
Quercetin DM3NC4M Obesity 5B81 Approved [69]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [34]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [22]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [70]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [71]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [72]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [73]
Stavudine DM6DEK9 Human immunodeficiency virus infection 1C62 Approved [74]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [50]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [75]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [76]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [77]
Triclosan DMZUR4N Malaria 1F40-1F45 Approved [78]
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [79]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [58]
PMID28460551-Compound-2 DM4DOUB N. A. N. A. Patented [80]
⏷ Show the Full List of 8 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [26]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [81]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [82]
Quercetin DM3NC4M Obesity 5B81 Approved [83]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [84]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [30]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [50]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [85]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [62]
Clodronate DM9Y6X7 Hypercalcaemia 5B91.0 Approved [86]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Adiponectin (ADIPOQ)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [87]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [87]
Ramipril DM2R68E Acute heart failure BD10-BD13 Approved [88]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [89]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [87]
Cilazapril DM4V6JA Congestive heart failure BD10 Approved [90]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [91]
Stavudine DM6DEK9 Human immunodeficiency virus infection 1C62 Approved [87]
Nevirapine DM6HX9B Human immunodeficiency virus infection 1C62 Approved [92]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [93]
⏷ 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 [94]
Methotrexate DM2TEOL Anterior urethra cancer Approved [95]
Quercetin DM3NC4M Obesity 5B81 Approved [96]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [97]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [98]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [99]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [100]
Testosterone DM7HUNW Hot flushes GA30 Approved [101]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [101]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [22]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [102]
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [103]
Leflunomide DMR8ONJ Arthritis FA20 Approved [104]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [38]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [105]
Sodium lauryl sulfate DMLJ634 Constipation DD91.1 Approved [106]
Azathioprine DMMZSXQ Lupus nephritis 4A40.0Y Approved [107]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [76]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Polycomb protein EED (EED)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Leflunomide DMR8ONJ Arthritis FA20 Approved [104]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [75]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [108]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [4]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [109]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [76]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [110]
Methotrexate DM2TEOL Anterior urethra cancer Approved [111]
TAK-243 DM4GKV2 Solid tumour/cancer 2A00-2F9Z Phase 1 [112]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Apolipoprotein E (APOE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [113]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [114]
Selenium DM25CGV N. A. N. A. Approved [115]
Quercetin DM3NC4M Obesity 5B81 Approved [116]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [117]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [97]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [61]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [118]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [119]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
⏷ 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 [15]
Levonorgestrel DM1DP7T Atypical endometrial hyperplasia Approved [120]
Selenium DM25CGV N. A. N. A. Approved [121]
Quercetin DM3NC4M Obesity 5B81 Approved [122]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [123]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [124]
Nevirapine DM6HX9B Human immunodeficiency virus infection 1C62 Approved [125]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [126]
Testosterone DM7HUNW Hot flushes GA30 Approved [127]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [101]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Androgen receptor (AR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [128]
Nilutamide DMFN07X Prostate cancer 2C82.0 Approved [128]
Hydroxyflutamide DMGIZF5 Prostate cancer 2C82.0 Approved [128]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [129]
Bicalutamide DMZMSPF Prostate cancer 2C82.0 Approved [130]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [131]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [132]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [133]
Selenium DM25CGV N. A. N. A. Approved [121]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [134]
⏷ 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 [135]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [136]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [137]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [94]
Selenium DM25CGV N. A. N. A. Approved [138]
Etretinate DM2CZFA Keratosis ED56 Approved [139]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [140]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [141]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [142]
Methotrexate DM2TEOL Anterior urethra cancer Approved [143]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-3 (CASP3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [144]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [145]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [146]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [147]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [148]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [149]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [150]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [151]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [152]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [153]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-8 (CASP8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [154]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [155]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [156]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [14]
Gefitinib DM15F0X Colon adenocarcinoma Approved [157]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [158]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [159]
Selenium DM25CGV N. A. N. A. Approved [115]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [160]
Methotrexate DM2TEOL Anterior urethra cancer Approved [161]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Polycomb protein SUZ12 (SUZ12)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [162]
Selenium DM25CGV N. A. N. A. Approved [115]
Testosterone DM7HUNW Hot flushes GA30 Approved [163]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [164]
Demecolcine DMCZQGK Solid tumour/cancer 2A00-2F9Z Approved [165]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [108]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [4]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [166]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [110]
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [167]
⏷ 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
Enhancer of zeste homolog 2 (EZH2) TT9MZCQ EZH2_HUMAN Modulator [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Adiponectin (ADIPOQ) OTNX23LE ADIPO_HUMAN Gene/Protein Processing [3]
Alkaline phosphatase, tissue-nonspecific isozyme (ALPL) OTG7J4BP PPBT_HUMAN Gene/Protein Processing [3]
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Gene/Protein Processing [4]
Apolipoprotein E (APOE) OTFOWL2H APOE_HUMAN Gene/Protein Processing [5]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [4]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Gene/Protein Processing [4]
Early growth response protein 1 (EGR1) OTCP6XGZ EGR1_HUMAN Gene/Protein Processing [3]
Fatty acid-binding protein, adipocyte (FABP4) OT3DKFOU FABP4_HUMAN Gene/Protein Processing [3]
G2/mitotic-specific cyclin-B1 (CCNB1) OT19S7E5 CCNB1_HUMAN Gene/Protein Processing [4]
Hairy/enhancer-of-split related with YRPW motif protein 1 (HEY1) OTJQL0I3 HEY1_HUMAN Gene/Protein Processing [3]

References

1 ClinicalTrials.gov (NCT02082977) A Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics and Clinical Activity of GSK2816126 in Subjects With Relapsed/Refractory Diffuse Large B Cell and Transformed Follicular Lymphoma. U.S. National Institutes of Health.
2 National Cancer Institute Drug Dictionary (drug id 756211).
3 Epigenetic control of skeletal development by the histone methyltransferase Ezh2. J Biol Chem. 2015 Nov 13;290(46):27604-17.
4 Dual targeting of EZH2 and androgen receptor as a novel therapy for castration-resistant prostate cancer. Toxicol Appl Pharmacol. 2020 Oct 1;404:115200. doi: 10.1016/j.taap.2020.115200. Epub 2020 Aug 14.
5 Enhancer of zeste homolog 2 (EZH2) regulates adipocyte lipid metabolism independent of adipogenic differentiation: Role of apolipoprotein E. J Biol Chem. 2019 May 24;294(21):8577-8591. doi: 10.1074/jbc.RA118.006871. Epub 2019 Apr 10.
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
7 Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
10 ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
11 Clinical pipeline report, company report or official report of HaiHe Biopharma.
12 Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497). J Med Chem. 2018 Feb 8;61(3):650-665.
13 EZH2 inhibitors: a patent review (2014-2016).Expert Opin Ther Pat. 2017 Jul;27(7):797-813.
14 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.
15 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
16 [Effect of nylestriol and levonorgestrel on the expression of Opg/OPGL in human osteosarcoma MG-63 cell lines]. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2004 Dec;29(6):667-70.
17 Chronic senescent human mesenchymal stem cells as possible contributor to the wound healing disorder after exposure to the alkylating agent sulfur mustard. Arch Toxicol. 2021 Feb;95(2):727-747. doi: 10.1007/s00204-020-02946-5. Epub 2021 Jan 25.
18 Effects of disease-modifying antirheumatic drugs and antiinflammatory cytokines on human osteoclastogenesis through interaction with receptor activator of nuclear factor kappaB, osteoprotegerin, and receptor activator of nuclear factor kappaB ligand. Arthritis Rheum. 2004 Dec;50(12):3831-43. doi: 10.1002/art.20637.
19 [Effect of simvastatin on the function of MG63 cell line]. Shanghai Kou Qiang Yi Xue. 2010 Dec;19(6):658-62.
20 Integrated assessment by multiple gene expression analysis of quercetin bioactivity on anticancer-related mechanisms in colon cancer cells in vitro. Eur J Nutr. 2005 Mar;44(3):143-56. doi: 10.1007/s00394-004-0503-1. Epub 2004 Apr 30.
21 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
22 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
23 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.
24 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.
25 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
26 Investigation of in vitro odonto/osteogenic capacity of cannabidiol on human dental pulp cell. J Dent. 2021 Jun;109:103673. doi: 10.1016/j.jdent.2021.103673. Epub 2021 Apr 16.
27 Protective effects of myricitrin against osteoporosis via reducing reactive oxygen species and bone-resorbing cytokines. Toxicol Appl Pharmacol. 2014 Nov 1;280(3):550-60.
28 Hydroxychloroquine decreases human MSC-derived osteoblast differentiation and mineralization in vitro. J Cell Mol Med. 2018 Feb;22(2):873-882. doi: 10.1111/jcmm.13373. Epub 2017 Oct 3.
29 Sensitivity of human dental pulp cells to eighteen chemical agents used for endodontic treatments in dentistry. Odontology. 2013 Jan;101(1):43-51.
30 Glucosamine promotes osteogenic differentiation of dental pulp stem cells through modulating the level of the transforming growth factor-beta type I receptor. J Cell Physiol. 2010 Oct;225(1):140-51.
31 A highly potent 26,27-Hexafluoro-1a,25-dihydroxyvitamin D3 on calcification in SV40-transformed human fetal osteoblastic cells. Calcif Tissue Int. 2002 Jun;70(6):488-95.
32 Novel pathways of endocrine disruption through pesticides interference with human mineralocorticoid receptors. Toxicol Sci. 2018 Mar 1;162(1):53-63.
33 Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
34 Induction of solid tumor differentiation by the peroxisome proliferator-activated receptor-gamma ligand troglitazone in patients with liposarcoma. Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):3951-6. doi: 10.1073/pnas.96.7.3951.
35 Retinoic acid-induced downmodulation of telomerase activity in human cancer cells. Exp Mol Pathol. 2005 Oct;79(2):108-17.
36 Adipocyte differentiation, mitochondrial gene expression and fat distribution: differences between zidovudine and tenofovir after 6 months. Antivir Ther. 2009;14(8):1089-100. doi: 10.3851/IMP1457.
37 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.
38 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.
39 Ursodeoxycholic acid but not tauroursodeoxycholic acid inhibits proliferation and differentiation of human subcutaneous adipocytes. PLoS One. 2013 Dec 3;8(12):e82086. doi: 10.1371/journal.pone.0082086. eCollection 2013.
40 Differential effects of peroxisome proliferator-activated receptor activators on the mRNA levels of genes involved in lipid metabolism in primary human monocyte-derived macrophages. Metabolism. 2003 May;52(5):652-7. doi: 10.1053/meta.2003.50100.
41 Induction of the endoplasmic reticulum stress protein GADD153/CHOP by capsaicin in prostate PC-3 cells: a microarray study. Biochem Biophys Res Commun. 2008 Aug 8;372(4):785-91.
42 Inhibiting Heat Shock Proteins Can Potentiate the Cytotoxic Effect of Cannabidiol in Human Glioma Cells. Anticancer Res. 2015 Nov;35(11):5827-37.
43 Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
44 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
45 Quercetin and Its Fermented Extract as a Potential Inhibitor of Bisphenol A-Exposed HT-29 Colon Cancer Cells' Viability. Int J Mol Sci. 2023 Mar 15;24(6):5604. doi: 10.3390/ijms24065604.
46 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
47 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.
48 The retinoid anticancer signal: mechanisms of target gene regulation. Br J Cancer. 2005 Aug 8;93(3):310-8. doi: 10.1038/sj.bjc.6602700.
49 Genomic profiling uncovers a molecular pattern for toxicological characterization of mutagens and promutagens in vitro. Toxicol Sci. 2011 Jul;122(1):185-97.
50 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
51 Gene expression changes in human small airway epithelial cells exposed to Delta9-tetrahydrocannabinol. Toxicol Lett. 2005 Aug 14;158(2):95-107.
52 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.
53 Effects of 25-hydroxyvitamin D(3) on proliferation and osteoblast differentiation of human marrow stromal cells require CYP27B1/1alpha-hydroxylase. J Bone Miner Res. 2011 May;26(5):1145-53.
54 Zoledronic acid up-regulates bone sialoprotein expression in osteoblastic cells through Rho GTPase inhibition. Biochem J. 2004 Dec 15;384(Pt 3):591-8. doi: 10.1042/BJ20040380.
55 Effect of surface chemical modification of bioceramic on phenotype of human bone-derived cells. J Biomed Mater Res. 1999 Mar 15;44(4):389-96. doi: 10.1002/(sici)1097-4636(19990315)44:4<389::aid-jbm4>3.0.co;2-o.
56 Potential osteoinductive effects of calcitriol on the m-RNA of mesenchymal stem cells derived from human alveolar periosteum. Biomed Res Int. 2016;2016:3529561.
57 ATR inhibitors VE-821 and VX-970 sensitize cancer cells to topoisomerase i inhibitors by disabling DNA replication initiation and fork elongation responses. Cancer Res. 2014 Dec 1;74(23):6968-79.
58 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
59 Cytotoxic effect of eugenol on the expression of molecular markers related to the osteogenic differentiation of human dental pulp cells. Odontology. 2011 Jul;99(2):188-92. doi: 10.1007/s10266-011-0009-2. Epub 2011 Jun 26.
60 Alpha ketoglutarate exerts a pro-osteogenic effect in osteoblast cell lines through activation of JNK and mTOR/S6K1/S6 signaling pathways. Toxicol Appl Pharmacol. 2019 Jul 1;374:53-64.
61 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
62 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
63 Dissecting progressive stages of 5-fluorouracil resistance in vitro using RNA expression profiling. Int J Cancer. 2004 Nov 1;112(2):200-12. doi: 10.1002/ijc.20401.
64 Pleiotropic combinatorial transcriptomes of human breast cancer cells exposed to mixtures of dietary phytoestrogens. Food Chem Toxicol. 2009 Apr;47(4):787-95.
65 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
66 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.
67 The NRF2-mediated oxidative stress response pathway is associated with tumor cell resistance to arsenic trioxide across the NCI-60 panel. BMC Med Genomics. 2010 Aug 13;3:37. doi: 10.1186/1755-8794-3-37.
68 COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
69 The effect of quercetin and kaempferol aglycones and glucuronides on peroxisome proliferator-activated receptor-gamma (PPAR-). Food Funct. 2015 Apr;6(4):1098-107. doi: 10.1039/c5fo00076a.
70 Glucosamine sulfate reduces prostaglandin E(2) production in osteoarthritic chondrocytes through inhibition of microsomal PGE synthase-1. J Rheumatol. 2012 Mar;39(3):635-44. doi: 10.3899/jrheum.110621. Epub 2011 Nov 15.
71 Isoniazid suppresses antioxidant response element activities and impairs adipogenesis in mouse and human preadipocytes. Toxicol Appl Pharmacol. 2013 Dec 15;273(3):435-41. doi: 10.1016/j.taap.2013.10.005. Epub 2013 Oct 12.
72 Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
73 Aspirin inhibits MMP-9 mRNA expression and release via the PPARalpha/gamma and COX-2/mPGES-1-mediated pathways in macrophages derived from THP-1 cells. Biomed Pharmacother. 2010 Feb;64(2):118-23. doi: 10.1016/j.biopha.2009.04.033. Epub 2009 Oct 17.
74 Mitochondrial proliferation, DNA depletion and adipocyte differentiation in subcutaneous adipose tissue of HIV-positive HAART recipients. Antivir Ther. 2003 Aug;8(4):323-31.
75 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
76 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
77 17-Estradiol Activates HSF1 via MAPK Signaling in ER-Positive Breast Cancer Cells. Cancers (Basel). 2019 Oct 11;11(10):1533. doi: 10.3390/cancers11101533.
78 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
79 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.
80 Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.
81 Naringin protects human adipose-derived mesenchymal stem cells against hydrogen peroxide-induced inhibition of osteogenic differentiation. Chem Biol Interact. 2015 Dec 5;242:255-61. doi: 10.1016/j.cbi.2015.10.010. Epub 2015 Oct 19.
82 The role of simvastatin in the osteogenesis of injectable tissue-engineered bone based on human adipose-derived stromal cells and platelet-rich plasma. Biomaterials. 2010 Jul;31(20):5325-35. doi: 10.1016/j.biomaterials.2010.03.037. Epub 2010 Apr 9.
83 Quercetin, a flavonoid, inhibits proliferation and increases osteogenic differentiation in human adipose stromal cells. Biochem Pharmacol. 2006 Nov 15;72(10):1268-78. doi: 10.1016/j.bcp.2006.08.021. Epub 2006 Sep 22.
84 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.
85 How benzene and its metabolites affect human marrow derived mesenchymal stem cells. Toxicol Lett. 2012 Oct 17;214(2):145-53. doi: 10.1016/j.toxlet.2012.08.015. Epub 2012 Aug 30.
86 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
87 Some HIV antiretrovirals increase oxidative stress and alter chemokine, cytokine or adiponectin production in human adipocytes and macrophages. Antivir Ther. 2007;12(4):489-500.
88 Additive beneficial cardiovascular and metabolic effects of combination therapy with ramipril and candesartan in hypertensive patients. Eur Heart J. 2007 Jun;28(12):1440-7. doi: 10.1093/eurheartj/ehm101. Epub 2007 May 5.
89 Adipogenic Effects and Gene Expression Profiling of Firemaster? 550 Components in Human Primary Preadipocytes. Environ Health Perspect. 2017 Sep 14;125(9):097013. doi: 10.1289/EHP1318.
90 Combination of an ACE inhibitor and indapamide improves blood pressure control, but attenuates the beneficial effects of ACE inhibition on plasma adiponectin in patients with essential hypertension. Circ J. 2009 Dec;73(12):2282-7. doi: 10.1253/circj.cj-09-0387. Epub 2009 Sep 29.
91 Role of PML SUMOylation in arsenic trioxide-induced fibrosis in HSCs. Life Sci. 2020 Jun 15;251:117607. doi: 10.1016/j.lfs.2020.117607. Epub 2020 Mar 30.
92 Effects of nevirapine and efavirenz on human adipocyte differentiation, gene expression, and release of adipokines and cytokines. Antiviral Res. 2011 Aug;91(2):112-9. doi: 10.1016/j.antiviral.2011.04.018. Epub 2011 May 17.
93 (9)-Tetrahydrocannabinol upregulates fatty acid 2-hydroxylase (FA2H) via PPAR induction: A possible evidence for the cancellation of PPAR/-mediated inhibition of PPAR in MDA-MB-231?cells. Arch Biochem Biophys. 2019 Feb 15;662:219-225. doi: 10.1016/j.abb.2018.12.011. Epub 2018 Dec 13.
94 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
95 Methotrexate induces apoptosis through p53/p21-dependent pathway and increases E-cadherin expression through downregulation of HDAC/EZH2. Biochem Pharmacol. 2011 Feb 15;81(4):510-7. doi: 10.1016/j.bcp.2010.11.014. Epub 2010 Nov 27.
96 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.
97 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
98 Differential responses to retinoic acid and endocrine disruptor compounds of subpopulations within human embryonic stem cell lines. Differentiation. 2012 Nov;84(4):330-43. doi: 10.1016/j.diff.2012.07.006. Epub 2012 Aug 18.
99 Interaction of EZH2 and P65 is involved in the arsenic trioxide-induced anti-angiogenesis in human triple-negative breast cancer cells. Cell Biol Toxicol. 2019 Aug;35(4):361-371. doi: 10.1007/s10565-018-09458-0. Epub 2019 Jan 5.
100 In vitro hydroquinone-induced instauration of histone bivalent mark on human retroelements (LINE-1) in HL60 cells. Toxicol In Vitro. 2017 Apr;40:1-10. doi: 10.1016/j.tiv.2016.12.007. Epub 2016 Dec 13.
101 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
102 Arsenic trioxide inhibits Hedgehog, Notch and stem cell properties in glioblastoma neurospheres. Acta Neuropathol Commun. 2014 Mar 31;2:31. doi: 10.1186/2051-5960-2-31.
103 Ouabain impairs cell migration, and invasion and alters gene expression of human osteosarcoma U-2 OS cells. Environ Toxicol. 2017 Nov;32(11):2400-2413. doi: 10.1002/tox.22453. Epub 2017 Aug 10.
104 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
105 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.
106 CXCL14 downregulation in human keratinocytes is a potential biomarker for a novel in vitro skin sensitization test. Toxicol Appl Pharmacol. 2020 Jan 1;386:114828. doi: 10.1016/j.taap.2019.114828. Epub 2019 Nov 14.
107 A transcriptomics-based in vitro assay for predicting chemical genotoxicity in vivo. Carcinogenesis. 2012 Jul;33(7):1421-9.
108 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.
109 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.
110 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.
111 Gene expression profiling of 30 cancer cell lines predicts resistance towards 11 anticancer drugs at clinically achieved concentrations. Int J Cancer. 2006 Apr 1;118(7):1699-712. doi: 10.1002/ijc.21570.
112 Inhibiting ubiquitination causes an accumulation of SUMOylated newly synthesized nuclear proteins at PML bodies. J Biol Chem. 2019 Oct 18;294(42):15218-15234. doi: 10.1074/jbc.RA119.009147. Epub 2019 Jul 8.
113 Effects of rosiglitazone and atorvastatin on the expression of genes that control cholesterol homeostasis in differentiating monocytes. Biochem Pharmacol. 2006 Feb 28;71(5):605-14.
114 Tolerability of statins is not linked to CYP450 polymorphisms, but reduced CYP2D6 metabolism improves cholesteraemic response to simvastatin and fluvastatin. Pharmacol Res. 2007 Apr;55(4):310-7. doi: 10.1016/j.phrs.2006.12.009. Epub 2007 Jan 14.
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 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.
117 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
118 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.
119 Biological specificity of CDK4/6 inhibitors: dose response relationship, in vivo signaling, and composite response signature. Oncotarget. 2017 Jul 4;8(27):43678-43691. doi: 10.18632/oncotarget.18435.
120 Effects of natural products and nutraceuticals on steroid hormone-regulated gene expression. Clin Chim Acta. 2001 Oct;312(1-2):213-9. doi: 10.1016/s0009-8981(01)00626-x.
121 Prostate specific antigen expression is down-regulated by selenium through disruption of androgen receptor signaling. Cancer Res. 2004 Jan 1;64(1):19-22. doi: 10.1158/0008-5472.can-03-2789.
122 Quercetin inhibits the expression and function of the androgen receptor in LNCaP prostate cancer cells. Carcinogenesis. 2001 Mar;22(3):409-14. doi: 10.1093/carcin/22.3.409.
123 EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer. Oncotarget. 2015 Feb 28;6(6):3811-24.
124 Androgen receptor or estrogen receptor-beta blockade alters DHEA-, DHT-, and E(2)-induced proliferation and PSA production in human prostate cancer cells. Prostate. 2007 Aug 1;67(11):1152-62. doi: 10.1002/pros.20585.
125 Nevirapine restores androgen signaling in hormone-refractory human prostate carcinoma cells both in vitro and in vivo. Prostate. 2009 May 15;69(7):744-54. doi: 10.1002/pros.20923.
126 An open-label phase II study of low-dose thalidomide in androgen-independent prostate cancer. Br J Cancer. 2003 Mar 24;88(6):822-7. doi: 10.1038/sj.bjc.6600817.
127 Inhibition of 5alpha-reductase enhances testosterone-induced expression of U19/Eaf2 tumor suppressor during the regrowth of LNCaP xenograft tumor in nude mice. Prostate. 2010 Oct 1;70(14):1575-85. doi: 10.1002/pros.21193.
128 TBECH, 1,2-dibromo-4-(1,2 dibromoethyl) cyclohexane, alters androgen receptor regulation in response to mutations associated with prostate cancer. Toxicol Appl Pharmacol. 2016 Sep 15;307:91-101. doi: 10.1016/j.taap.2016.07.018. Epub 2016 Jul 27.
129 Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies. Nucleic Acids Res. 2015 Jul 13;43(12):5880-97. doi: 10.1093/nar/gkv262. Epub 2015 Apr 23.
130 Possible role of adaptive mutation in resistance to antiandrogen in prostate cancer cells. Prostate. 2005 Nov 1;65(3):268-75. doi: 10.1002/pros.20282.
131 Effects of the environmental estrogens bisphenol A, o,p'-DDT, p-tert-octylphenol and coumestrol on apoptosis induction, cell proliferation and the expression of estrogen sensitive molecular parameters in the human breast cancer cell line MCF-7. J Steroid Biochem Mol Biol. 2002 Jan;80(1):61-70. doi: 10.1016/s0960-0760(01)00173-x.
132 Identifying environmental chemicals as agonists of the androgen receptor by using a quantitative high-throughput screening platform. Toxicology. 2017 Jun 15;385:48-58. doi: 10.1016/j.tox.2017.05.001. Epub 2017 May 4.
133 Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor. Sci Rep. 2014 Sep 26;4:6437. doi: 10.1038/srep06437.
134 Comparison of the Hershberger assay and androgen receptor binding assay of twelve chemicals. Toxicology. 2004 Feb 15;195(2-3):177-86. doi: 10.1016/j.tox.2003.09.012.
135 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.
136 G2 delay induced by nitrogen mustard in human cells affects cyclin A/cdk2 and cyclin B1/cdc2-kinase complexes differently. J Biol Chem. 1993 Apr 15;268(11):8298-308.
137 Gene expression profiles with activation of the estrogen receptor alpha-selective estrogen receptor modulator complex in breast cancer cells expressing wild-type estrogen receptor. Cancer Res. 2002 Aug 1;62(15):4419-26.
138 Selenite and selenomethionine promote HL-60 cell cycle progression. J Nutr. 2002 Apr;132(4):674-9. doi: 10.1093/jn/132.4.674.
139 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.
140 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.
141 Synthesis and antitumor evaluation of nitrovinyl biphenyls: anticancer agents based on allocolchicines. ChemMedChem. 2011 May 2;6(5):859-68. doi: 10.1002/cmdc.201100019. Epub 2011 Apr 6.
142 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
143 Methotrexate modulates folate phenotype and inflammatory profile in EA.hy 926 cells. Eur J Pharmacol. 2014 Jun 5;732:60-7.
144 Different apoptosis ratios and gene expressions in two human cell lines after sevoflurane anaesthesia. Acta Anaesthesiol Scand. 2009 Oct;53(9):1192-9. doi: 10.1111/j.1399-6576.2009.02036.x. Epub 2009 Jun 30.
145 [Mechanisms underlying the effect of arsenic trioxide on proliferation inhibition and apoptosis induction in myeloma cell line u266]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2007 Oct;15(5):982-5.
146 Lovastatin lactone elicits human lung cancer cell apoptosis via a COX-2/PPAR-dependent pathway. Oncotarget. 2016 Mar 1;7(9):10345-62. doi: 10.18632/oncotarget.7213.
147 Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells. Oncol Res. 2000;12(9-10):397-408. doi: 10.3727/096504001108747855.
148 Comparison of burst of reactive oxygen species and activation of caspase-3 in apoptosis of K562 and HL-60 cells induced by docetaxel. Cancer Lett. 2004 Oct 8;214(1):103-13. doi: 10.1016/j.canlet.2004.03.047.
149 Induction of mitochondrial manganese superoxide dismutase confers resistance to apoptosis in acute myeloblastic leukaemia cells exposed to etoposide. Br J Haematol. 2000 Mar;108(3):574-81. doi: 10.1046/j.1365-2141.2000.01852.x.
150 Cisplatin-enhanced sensitivity of glioblastoma multiforme U251 cells to adenovirus-delivered TRAIL in vitro. Tumour Biol. 2010 Dec;31(6):613-22. doi: 10.1007/s13277-010-0077-x. Epub 2010 Jul 11.
151 Insulin-like growth factor I is the key growth factor in serum that protects neuroblastoma cells from hyperosmotic-induced apoptosis. J Cell Physiol. 2000 Jan;182(1):24-32. doi: 10.1002/(SICI)1097-4652(200001)182:1<24::AID-JCP3>3.0.CO;2-6.
152 mRNA expression analysis of a variety of apoptosis-related genes, including the novel gene of the BCL2-family, BCL2L12, in HL-60 leukemia cells after treatment with carboplatin and doxorubicin. Biol Chem. 2004 Nov;385(11):1099-103. doi: 10.1515/BC.2004.143.
153 Neurokinin-1 receptor (NK1R) inhibition sensitizes APL cells to anti-tumor effect of arsenic trioxide via restriction of NF-B axis: Shedding new light on resistance to Aprepitant. Int J Biochem Cell Biol. 2018 Oct;103:105-114. doi: 10.1016/j.biocel.2018.08.010. Epub 2018 Aug 23.
154 Statins activate the mitochondrial pathway of apoptosis in human lymphoblasts and myeloma cells. Carcinogenesis. 2005 May;26(5):883-91. doi: 10.1093/carcin/bgi036. Epub 2005 Feb 10.
155 Drug-induced caspase 8 upregulation sensitises cisplatin-resistant ovarian carcinoma cells to rhTRAIL-induced apoptosis. Br J Cancer. 2011 Apr 12;104(8):1278-87. doi: 10.1038/bjc.2011.84.
156 Essential role of caspase-8 in p53/p73-dependent apoptosis induced by etoposide in head and neck carcinoma cells. Mol Cancer. 2011 Jul 31;10:95. doi: 10.1186/1476-4598-10-95.
157 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.
158 Melatonin enhances hydrogen peroxide-induced apoptosis in human promyelocytic leukaemia HL-60 cells. Mol Cell Biochem. 2011 Jul;353(1-2):167-76. doi: 10.1007/s11010-011-0783-8. Epub 2011 Mar 23.
159 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.
160 Ciprofloxacin induces apoptosis and inhibits proliferation of human colorectal carcinoma cells. Br J Cancer. 2002 Feb 1;86(3):443-8. doi: 10.1038/sj.bjc.6600079.
161 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
162 Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802.
163 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
164 Design principles of concentration-dependent transcriptome deviations in drug-exposed differentiating stem cells. Chem Res Toxicol. 2014 Mar 17;27(3):408-20.
165 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
166 Low doses of cisplatin induce gene alterations, cell cycle arrest, and apoptosis in human promyelocytic leukemia cells. Biomark Insights. 2016 Aug 24;11:113-21.
167 Curcumin restores corticosteroid function in monocytes exposed to oxidants by maintaining HDAC2. Am J Respir Cell Mol Biol. 2008 Sep;39(3):312-23. doi: 10.1165/rcmb.2008-0012OC. Epub 2008 Apr 17.