General Information of Drug Off-Target (DOT) (ID: OTW8V2V1)

DOT Name Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2)
Synonyms
EC 7.6.2.2; ATP-binding cassette sub-family G member 2; Breast cancer resistance protein; CDw338; Mitoxantrone resistance-associated protein; Placenta-specific ATP-binding cassette transporter; Urate exporter; CD antigen CD338
Gene Name ABCG2
UniProt ID
ABCG2_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
5NJ3; 5NJG; 6ETI; 6FEQ; 6FFC; 6HBU; 6HCO; 6HIJ; 6HZM; 6VXF; 6VXH; 6VXI; 6VXJ; 7NEQ; 7NEZ; 7NFD; 7OJ8; 7OJH; 7OJI; 8BHT; 8BI0; 8P7W; 8P8A; 8P8J; 8U2C
EC Number
7.6.2.2
Pfam ID
PF01061 ; PF19055 ; PF00005
Sequence
MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
Function
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells. Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme. Also mediates the efflux of sphingosine-1-P from cells. Acts as a urate exporter functioning in both renal and extrarenal urate excretion. In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate. Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates. Mediates the secretion of the riboflavin and biotin vitamins into milk. Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability. Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux. In placenta, it limits the penetration of drugs from the maternal plasma into the fetus. May play a role in early stem cell self-renewal by blocking differentiation.
Tissue Specificity Highly expressed in placenta . Low expression in small intestine, liver and colon . Expressed in brain (at protein level) .
KEGG Pathway
Antifolate resistance (hsa01523 )
ABC transporters (hsa02010 )
Bile secretion (hsa04976 )
Reactome Pathway
Heme degradation (R-HSA-189483 )
Abacavir transmembrane transport (R-HSA-2161517 )
Iron uptake and transport (R-HSA-917937 )
Paracetamol ADME (R-HSA-9753281 )
Ciprofloxacin ADME (R-HSA-9793528 )
NFE2L2 regulating MDR associated enzymes (R-HSA-9818032 )
Heme biosynthesis (R-HSA-189451 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 12 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Fulvestrant DM0YZC6 Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the response to substance of Fulvestrant. [71]
Aspirin DM672AH Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the Diarrhoea ADR of Aspirin. [72]
Irinotecan DMP6SC2 Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the response to substance of Irinotecan. [73]
Topotecan DMP6G8T Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) decreases the response to substance of Topotecan. [74]
Gefitinib DM15F0X Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the Diarrhea ADR of Gefitinib. [72]
Warfarin DMJYCVW Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the response to substance of Warfarin. [76]
Nilotinib DM7HXWT Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the response to substance of Nilotinib. [77]
Epirubicin DMPDW6T Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) decreases the response to substance of Epirubicin. [74]
Rosuvastatin DMMIQ7G Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the LDL cholesterol decreased ADR of Rosuvastatin. [83]
Sunitinib DMCBJSR Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the Vomiting ADR of Sunitinib. [84]
PHA-739358 DMGYBZI Phase 2 Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) decreases the response to substance of PHA-739358. [87]
3R14S-OCHRATOXIN A DM2KEW6 Investigative Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the response to substance of 3R14S-OCHRATOXIN A. [88]
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⏷ Show the Full List of 12 Drug(s)
This DOT Affected the Biotransformations of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Adenosine triphosphate DM79F6G Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the hydrolysis of Adenosine triphosphate. [75]
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This DOT Affected the Regulation of Drug Effects of 12 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Cimetidine DMH61ZB Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the transport of Cimetidine. [36]
Pitavastatin DMJH792 Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the transport of Pitavastatin. [78]
Aciclovir DMYLOVR Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the transport of Aciclovir. [79]
Nitrofurantoin DM7PQIK Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the transport of Nitrofurantoin. [80]
Sulfapyridine DMIUYFH Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the transport of Sulfapyridine. [81]
Sulpiride DMF54ZG Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the transport of Sulpiride. [82]
Moxidectin DMYGHX5 Approved Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the export of Moxidectin . [85]
CP-724714 DMUJ0W7 Phase 2 Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) affects the transport of CP-724714. [86]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE DMNQL17 Investigative Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) decreases the transport of 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE. [89]
Ginsenoside Re DM46FVD Investigative Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the transport of Ginsenoside Re. [90]
[3H]estrone-3-sulphate DMGPF0N Investigative Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the export of [3H]estrone-3-sulphate. [91]
[3H]estradiol-17beta-glucuronide DM3KJ45 Investigative Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) increases the transport of [3H]estradiol-17beta-glucuronide. [92]
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⏷ Show the Full List of 12 Drug(s)
91 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [2]
Tretinoin DM49DUI Approved Tretinoin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [3]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [4]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [5]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [6]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [7]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [8]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [9]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide affects the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [10]
Testosterone DM7HUNW Approved Testosterone decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [11]
Triclosan DMZUR4N Approved Triclosan increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [12]
Carbamazepine DMZOLBI Approved Carbamazepine increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [13]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [14]
Decitabine DMQL8XJ Approved Decitabine affects the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [15]
Zoledronate DMIXC7G Approved Zoledronate increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [16]
Phenobarbital DMXZOCG Approved Phenobarbital increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [17]
Progesterone DMUY35B Approved Progesterone decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [11]
Menadione DMSJDTY Approved Menadione affects the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [18]
Folic acid DMEMBJC Approved Folic acid increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [19]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [20]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [21]
Ethanol DMDRQZU Approved Ethanol increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [22]
Paclitaxel DMLB81S Approved Paclitaxel decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [23]
Permethrin DMZ0Q1G Approved Permethrin decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [24]
Rifampicin DM5DSFZ Approved Rifampicin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [17]
Mitoxantrone DMM39BF Approved Mitoxantrone increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [25]
Zidovudine DM4KI7O Approved Zidovudine increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [26]
Daunorubicin DMQUSBT Approved Daunorubicin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [27]
Lindane DMB8CNL Approved Lindane increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [28]
Imatinib DM7RJXL Approved Imatinib increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [29]
Estrone DM5T6US Approved Estrone increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [7]
Crizotinib DM4F29C Approved Crizotinib decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [30]
Ciprofloxacin XR DM2NLS9 Approved Ciprofloxacin XR increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [31]
Omeprazole DM471KJ Approved Omeprazole increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [20]
Estriol DMOEM2I Approved Estriol increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [7]
Romidepsin DMT5GNL Approved Romidepsin affects the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [15]
Nelfinavir mesylate DMFX6G8 Approved Nelfinavir mesylate decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [32]
LY2835219 DM93VBZ Approved LY2835219 decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [33]
Naproxen DMZ5RGV Approved Naproxen affects the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [34]
Methoxsalen DME8FZ9 Approved Methoxsalen increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [35]
Digoxin DMQCTIH Approved Digoxin decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [36]
Dabrafenib DMX6OE3 Approved Dabrafenib increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [37]
Novobiocin DMRFWGK Approved Novobiocin decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [39]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [40]
Beclomethasone dipropionate DM5NW1E Phase 4 Beclomethasone dipropionate increases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [41]
Silymarin DMXBYQR Phase 4 Silymarin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [42]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [43]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [44]
Curcumin DMQPH29 Phase 3 Curcumin decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [45]
Chloroquine DMSI5CB Phase 3 Trial Chloroquine decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [46]
I3C DMIGFOR Phase 3 I3C increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [42]
5-methoxypsoralen DME2A8X Phase 3 5-methoxypsoralen increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [35]
MLN8237 DMO8PT9 Phase 3 MLN8237 affects the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [47]
TAK-875 DMIM5AP Phase 3 TAK-875 decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [48]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [49]
ANW-32821 DMMJOZD Phase 2 ANW-32821 increases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [50]
Pyrethroids DM1794O Phase 2 Pyrethroids decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [24]
Oxfendazole DMSNL51 Phase 2 Oxfendazole decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [51]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [53]
PMID26394986-Compound-22 DM43Z1G Patented PMID26394986-Compound-22 decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [54]
Flavonoid derivative 1 DMCQP0B Patented Flavonoid derivative 1 affects the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [55]
PMID26560530-Compound-34 DMLGZPO Patented PMID26560530-Compound-34 increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [17]
Elacridar DMURVE8 Discontinued in Phase 1 Elacridar decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [56]
Nimesulide DMR1NMD Terminated Nimesulide decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [34]
WIN-55212-2 DMACBIW Terminated WIN-55212-2 affects the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [57]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [58]
Trichostatin A DM9C8NX Investigative Trichostatin A increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [59]
Butanoic acid DMTAJP7 Investigative Butanoic acid increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [60]
Forskolin DM6ITNG Investigative Forskolin increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [61]
Okadaic acid DM47CO1 Investigative Okadaic acid increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [62]
Chlorpyrifos DMKPUI6 Investigative Chlorpyrifos increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [63]
CH-223191 DMMJZYC Investigative CH-223191 decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [64]
Chrysin DM7V2LG Investigative Chrysin decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [65]
CATECHIN DMY38SB Investigative CATECHIN decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [42]
AM251 DMTAWHL Investigative AM251 increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [66]
Oleic acid DM54O1Z Investigative Oleic acid increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [67]
2-tert-butylbenzene-1,4-diol DMNXI1E Investigative 2-tert-butylbenzene-1,4-diol increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [42]
N-nonylphenol DMH3OUX Investigative N-nonylphenol decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [58]
Flavone DMEQH6J Investigative Flavone increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [42]
Chlorphrifos oxon DMGBT68 Investigative Chlorphrifos oxon increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [68]
Ginsenoside RG3 DMFN58T Investigative Ginsenoside RG3 decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [69]
Anandamide DMCKH3P Investigative Anandamide decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [70]
4-ANDROSTENE-3-17-DIONE DMSE8NU Investigative 4-ANDROSTENE-3-17-DIONE decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [11]
chlordane DMMHU8G Investigative chlordane increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [28]
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE DMTPQ84 Investigative (11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE decreases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [36]
2-chloro-5-nitro-N-phenylbenzamide DMUGQIV Investigative 2-chloro-5-nitro-N-phenylbenzamide affects the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [68]
6-bromoindirubin-3-oxime DM12WYV Investigative 6-bromoindirubin-3-oxime increases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [8]
T0070907 DMTKSVO Investigative T0070907 decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [21]
Racemic DOI DM39FSQ Investigative Racemic DOI increases the activity of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [57]
CID16020046 DMLWZRT Investigative CID16020046 decreases the expression of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [66]
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⏷ Show the Full List of 91 Drug(s)
2 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Sulfasalazine DMICA9H Approved Sulfasalazine decreases the methylation of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [27]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the methylation of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [52]
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3 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Venetoclax DM8I94Y Approved Venetoclax affects the binding of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [38]
Pibrentasvir DM27BL1 Approved Pibrentasvir affects the binding of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [38]
GS-5885 DMSL3DX Phase 2 GS-5885 affects the binding of Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2). [38]
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References

1 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
2 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
3 All-trans retinoic acid enhances the transport of phase II metabolites of benzo[a]pyrene by inducing the Breast Cancer Resistance Protein expression in Caco-2 cells. Toxicol Lett. 2010 Aug 16;197(2):151-5. doi: 10.1016/j.toxlet.2010.05.018. Epub 2010 Jun 1.
4 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.
5 Single-step doxorubicin-selected cancer cells overexpress the ABCG2 drug transporter through epigenetic changes. Br J Cancer. 2008 May 6;98(9):1515-24.
6 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
7 Effects of sex hormones on regulation of ABCG2 expression in the placental cell line BeWo. J Pharm Pharm Sci. 2006;9(1):133-9.
8 Activation of beta-catenin signalling by GSK-3 inhibition increases p-glycoprotein expression in brain endothelial cells. J Neurochem. 2008 Aug;106(4):1855-65. doi: 10.1111/j.1471-4159.2008.05537.x. Epub 2008 Jul 4.
9 Arsenic trioxide induces differentiation of cancer stem cells in hepatocellular carcinoma through inhibition of LIF/JAK1/STAT3 and NF-kB signaling pathways synergistically. Clin Transl Med. 2021 Feb;11(2):e335. doi: 10.1002/ctm2.335.
10 Chronic Oxidative Stress Increases Resistance to Doxorubicin-Induced Cytotoxicity in Renal Carcinoma Cells Potentially Through Epigenetic Mechanism. Mol Pharmacol. 2016 Jan;89(1):27-41. doi: 10.1124/mol.115.100206. Epub 2015 Oct 30.
11 Localization of breast cancer resistance protein (Bcrp) in endocrine organs and inhibition of its transport activity by steroid hormones. Cell Tissue Res. 2012 Aug;349(2):551-63. doi: 10.1007/s00441-012-1417-5. Epub 2012 May 13.
12 Triclosan treatment decreased the antitumor effect of sorafenib on hepatocellular carcinoma cells. Onco Targets Ther. 2018 May 18;11:2945-2954.
13 Transcriptional profiling of genes induced in the livers of patients treated with carbamazepine. Clin Pharmacol Ther. 2006 Nov;80(5):440-456.
14 Proteomic identification of differentially expressed proteins associated with the multiple drug resistance in methotrexate-resistant human breast cancer cells. Int J Oncol. 2014 Jul;45(1):448-58.
15 Aberrant promoter methylation of the ABCG2 gene in renal carcinoma. Mol Cell Biol. 2006 Nov;26(22):8572-85.
16 In vitro evaluation of zoledronic acid resistance developed in MCF-7 cells. Anticancer Res. 2007 Nov-Dec;27(6B):4031-7.
17 Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Drug Metab Dispos. 2006 Oct;34(10):1756-63. doi: 10.1124/dmd.106.010033. Epub 2006 Jul 12.
18 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.
19 Folate deprivation induces BCRP (ABCG2) expression and mitoxantrone resistance in Caco-2 cells. Int J Cancer. 2008 Oct 1;123(7):1712-20.
20 A novel xenobiotic responsive element regulated by aryl hydrocarbon receptor is involved in the induction of BCRP/ABCG2 in LS174T cells. Biochem Pharmacol. 2010 Dec 1;80(11):1754-61.
21 Regulation of the placental BCRP transporter by PPAR gamma. J Biochem Mol Toxicol. 2017 May;31(5):10.1002/jbt.21880. doi: 10.1002/jbt.21880. Epub 2016 Nov 23.
22 Prenatal ethanol exposure increases maternal bile acids through placental transport pathway. Toxicology. 2021 Jun 30;458:152848. doi: 10.1016/j.tox.2021.152848. Epub 2021 Jul 2.
23 FaDu cell characteristics induced by multidrug resistance. Oncol Rep. 2011 Nov;26(5):1189-95. doi: 10.3892/or.2011.1418. Epub 2011 Aug 10.
24 Inhibition of human MDR1 and BCRP transporter ATPase activity by organochlorine and pyrethroid insecticides. J Biochem Mol Toxicol. 2013 Feb;27(2):157-64.
25 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.
26 Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
27 Chemotherapeutic drug-induced ABCG2 promoter demethylation as a novel mechanism of acquired multidrug resistance. Neoplasia. 2009 Dec;11(12):1359-70. doi: 10.1593/neo.91314.
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