General Information of Drug Off-Target (DOT) (ID: OTJSIGV5)

DOT Name ATP-binding cassette sub-family C member 2 (ABCC2)
Synonyms EC 7.6.2.-; EC 7.6.2.2; EC 7.6.2.3; Canalicular multidrug resistance protein; Canalicular multispecific organic anion transporter 1; Multidrug resistance-associated protein 2
Gene Name ABCC2
Related Disease
Dubin-Johnson syndrome ( )
UniProt ID
MRP2_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
EC Number
7.6.2.-; 7.6.2.2; 7.6.2.3
Pfam ID
PF00664 ; PF00005
Sequence
MLEKFCNSTFWNSSFLDSPEADLPLCFEQTVLVWIPLGYLWLLAPWQLLHVYKSRTKRSS
TTKLYLAKQVFVGFLLILAAIELALVLTEDSGQATVPAVRYTNPSLYLGTWLLVLLIQYS
RQWCVQKNSWFLSLFWILSILCGTFQFQTLIRTLLQGDNSNLAYSCLFFISYGFQILILI
FSAFSENNESSNNPSSIASFLSSITYSWYDSIILKGYKRPLTLEDVWEVDEEMKTKTLVS
KFETHMKRELQKARRALQRRQEKSSQQNSGARLPGLNKNQSQSQDALVLEDVEKKKKKSG
TKKDVPKSWLMKALFKTFYMVLLKSFLLKLVNDIFTFVSPQLLKLLISFASDRDTYLWIG
YLCAILLFTAALIQSFCLQCYFQLCFKLGVKVRTAIMASVYKKALTLSNLARKEYTVGET
VNLMSVDAQKLMDVTNFMHMLWSSVLQIVLSIFFLWRELGPSVLAGVGVMVLVIPINAIL
STKSKTIQVKNMKNKDKRLKIMNEILSGIKILKYFAWEPSFRDQVQNLRKKELKNLLAFS
QLQCVVIFVFQLTPVLVSVVTFSVYVLVDSNNILDAQKAFTSITLFNILRFPLSMLPMMI
SSMLQASVSTERLEKYLGGDDLDTSAIRHDCNFDKAMQFSEASFTWEHDSEATVRDVNLD
IMAGQLVAVIGPVGSGKSSLISAMLGEMENVHGHITIKGTTAYVPQQSWIQNGTIKDNIL
FGTEFNEKRYQQVLEACALLPDLEMLPGGDLAEIGEKGINLSGGQKQRISLARATYQNLD
IYLLDDPLSAVDAHVGKHIFNKVLGPNGLLKGKTRLLVTHSMHFLPQVDEIVVLGNGTIV
EKGSYSALLAKKGEFAKNLKTFLRHTGPEEEATVHDGSEEEDDDYGLISSVEEIPEDAAS
ITMRRENSFRRTLSRSSRSNGRHLKSLRNSLKTRNVNSLKEDEELVKGQKLIKKEFIETG
KVKFSIYLEYLQAIGLFSIFFIILAFVMNSVAFIGSNLWLSAWTSDSKIFNSTDYPASQR
DMRVGVYGALGLAQGIFVFIAHFWSAFGFVHASNILHKQLLNNILRAPMRFFDTTPTGRI
VNRFAGDISTVDDTLPQSLRSWITCFLGIISTLVMICMATPVFTIIVIPLGIIYVSVQMF
YVSTSRQLRRLDSVTRSPIYSHFSETVSGLPVIRAFEHQQRFLKHNEVRIDTNQKCVFSW
ITSNRWLAIRLELVGNLTVFFSALMMVIYRDTLSGDTVGFVLSNALNITQTLNWLVRMTS
EIETNIVAVERITEYTKVENEAPWVTDKRPPPDWPSKGKIQFNNYQVRYRPELDLVLRGI
TCDIGSMEKIGVVGRTGAGKSSLTNCLFRILEAAGGQIIIDGVDIASIGLHDLREKLTII
PQDPILFSGSLRMNLDPFNNYSDEEIWKALELAHLKSFVASLQLGLSHEVTEAGGNLSIG
QRQLLCLGRALLRKSKILVLDEATAAVDLETDNLIQTTIQNEFAHCTVITIAHRLHTIMD
SDKVMVLDNGKIIECGSPEELLQIPGPFYFMAKEAGIENVNSTKF
Function
ATP-dependent transporter of the ATP-binding cassette (ABC) family that binds and hydrolyzes ATP to enable active transport of various substrates including many drugs, toxicants and endogenous compound across cell membranes. Transports a wide variety of conjugated organic anions such as sulfate-, glucuronide- and glutathione (GSH)-conjugates of endo- and xenobiotics substrates. Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification. Mediates also hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4. Transports sulfated bile salt such as taurolithocholate sulfate. Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors. Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine.
Tissue Specificity Expressed by polarized cells in liver, kidney and intestine. The highest expression is found in liver. Expressed in small intestine .
KEGG Pathway
Antifolate resistance (hsa01523 )
Platinum drug resistance (hsa01524 )
ABC transporters (hsa02010 )
Bile secretion (hsa04976 )
Reactome Pathway
ABC-family proteins mediated transport (R-HSA-382556 )
Defective ABCC2 causes DJS (R-HSA-5679001 )
Aspirin ADME (R-HSA-9749641 )
Paracetamol ADME (R-HSA-9753281 )
Atorvastatin ADME (R-HSA-9754706 )
Heme degradation (R-HSA-189483 )

Molecular Interaction Atlas (MIA) of This DOT

1 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Dubin-Johnson syndrome DISM8TG9 Strong Autosomal recessive [1]
------------------------------------------------------------------------------------
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
Ivermectin DMDBX5F Approved ATP-binding cassette sub-family C member 2 (ABCC2) increases the Cell-mediated cytotoxicity ADR of Ivermectin. [68]
Temozolomide DMKECZD Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the response to substance of Temozolomide. [69]
Fluorouracil DMUM7HZ Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the response to substance of Fluorouracil. [70]
Irinotecan DMP6SC2 Approved ATP-binding cassette sub-family C member 2 (ABCC2) decreases the response to substance of Irinotecan. [72]
Paclitaxel DMLB81S Approved ATP-binding cassette sub-family C member 2 (ABCC2) decreases the response to substance of Paclitaxel. [41]
DTI-015 DMXZRW0 Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the response to substance of DTI-015. [69]
Daunorubicin DMQUSBT Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the response to substance of Daunorubicin. [73]
Phenytoin DMNOKBV Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the response to substance of Phenytoin. [74]
Sorafenib DMS8IFC Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the response to substance of Sorafenib. [75]
Docetaxel DMDI269 Approved ATP-binding cassette sub-family C member 2 (ABCC2) increases the Leukopenia ADR of Docetaxel. [76]
Fosinopril DM9NJ52 Approved ATP-binding cassette sub-family C member 2 (ABCC2) decreases the response to substance of Fosinopril. [82]
DNCB DMDTVYC Phase 2 ATP-binding cassette sub-family C member 2 (ABCC2) decreases the response to substance of DNCB. [84]
------------------------------------------------------------------------------------
⏷ Show the Full List of 12 Drug(s)
This DOT Affected the Regulation of Drug Effects of 18 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Etoposide DMNH3PG Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of Etoposide. [71]
Vinblastine DM5TVS3 Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of Vinblastine. [41]
Adenosine triphosphate DM79F6G Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the metabolism of Adenosine triphosphate. [77]
Glutathione DMAHMT9 Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of Glutathione. [78]
Chlorambucil DMRKE63 Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the export of Chlorambucil. [42]
Nelfinavir mesylate DMFX6G8 Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of Nelfinavir mesylate. [79]
Ethacrynic acid DM60QMR Approved ATP-binding cassette sub-family C member 2 (ABCC2) increases the transport of Ethacrynic acid. [80]
Lopinavir DMITQS0 Approved ATP-binding cassette sub-family C member 2 (ABCC2) increases the abundance of Lopinavir. [77]
Pitavastatin DMJH792 Approved ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of Pitavastatin. [81]
Succimer DME81IY Approved ATP-binding cassette sub-family C member 2 (ABCC2) increases the transport of Succimer. [83]
Vadimezan DMK7CYX Phase 2 ATP-binding cassette sub-family C member 2 (ABCC2) affects the export of Vadimezan. [85]
PKI166 DMSQ794 Discontinued in Phase 2 ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of PKI166. [86]
Microcystin-LR DMTMLRN Investigative ATP-binding cassette sub-family C member 2 (ABCC2) increases the export of Microcystin-LR. [87]
[3H]estrone-3-sulphate DMGPF0N Investigative ATP-binding cassette sub-family C member 2 (ABCC2) affects the export of [3H]estrone-3-sulphate. [88]
Ginsenoside Re DM46FVD Investigative ATP-binding cassette sub-family C member 2 (ABCC2) increases the transport of Ginsenoside Re. [89]
G418 DMKTJBU Investigative ATP-binding cassette sub-family C member 2 (ABCC2) increases the transport of G418. [90]
LTC4 DM702WR Investigative ATP-binding cassette sub-family C member 2 (ABCC2) affects the transport of LTC4. [91]
6-Carboxyfluorescein DMWTMDH Investigative ATP-binding cassette sub-family C member 2 (ABCC2) affects the export of 6-Carboxyfluorescein. [92]
------------------------------------------------------------------------------------
⏷ Show the Full List of 18 Drug(s)
4 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of ATP-binding cassette sub-family C member 2 (ABCC2). [2]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the methylation of ATP-binding cassette sub-family C member 2 (ABCC2). [52]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 increases the phosphorylation of ATP-binding cassette sub-family C member 2 (ABCC2). [54]
Coumarin DM0N8ZM Investigative Coumarin decreases the phosphorylation of ATP-binding cassette sub-family C member 2 (ABCC2). [54]
------------------------------------------------------------------------------------
83 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [3]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [4]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [5]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [6]
Estradiol DMUNTE3 Approved Estradiol increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [7]
Arsenic DMTL2Y1 Approved Arsenic increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [8]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [9]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide affects the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [10]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [11]
Triclosan DMZUR4N Approved Triclosan decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [12]
Carbamazepine DMZOLBI Approved Carbamazepine increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [13]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [14]
Decitabine DMQL8XJ Approved Decitabine increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [15]
Phenobarbital DMXZOCG Approved Phenobarbital increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [16]
Progesterone DMUY35B Approved Progesterone decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [17]
Fulvestrant DM0YZC6 Approved Fulvestrant increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [18]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [19]
Bortezomib DMNO38U Approved Bortezomib increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [20]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [21]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [22]
Azathioprine DMMZSXQ Approved Azathioprine increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [23]
Diclofenac DMPIHLS Approved Diclofenac increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [21]
Sodium lauryl sulfate DMLJ634 Approved Sodium lauryl sulfate increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [24]
Indomethacin DMSC4A7 Approved Indomethacin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [25]
Ethinyl estradiol DMODJ40 Approved Ethinyl estradiol decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [26]
Simvastatin DM30SGU Approved Simvastatin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [27]
Topotecan DMP6G8T Approved Topotecan increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [28]
Rifampicin DM5DSFZ Approved Rifampicin increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [29]
Ursodeoxycholic acid DMCUT21 Approved Ursodeoxycholic acid increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [30]
Fluoxetine DM3PD2C Approved Fluoxetine increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [31]
Chenodiol DMQ8JIK Approved Chenodiol increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [32]
Bosentan DMIOGBU Approved Bosentan decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [33]
Lovastatin DM9OZWQ Approved Lovastatin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [27]
Bezafibrate DMZDCS0 Approved Bezafibrate increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [34]
Ximelegatran DMU8ANS Approved Ximelegatran increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [35]
Atazanavir DMSYRBX Approved Atazanavir decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [36]
Clotrimazole DMMFCIH Approved Clotrimazole increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [29]
Clavulanate DM2FGRT Approved Clavulanate increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [37]
Epirubicin DMPDW6T Approved Epirubicin increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [38]
Citalopram DM2G9AE Approved Citalopram increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [39]
Methoxsalen DME8FZ9 Approved Methoxsalen decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [40]
Benzbromarone DMC3YUA Approved Benzbromarone decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [25]
Cholic acid DM7OKQV Approved Cholic acid increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [32]
Paroxetine DM5PVQE Approved Paroxetine increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [39]
Probenecid DMMFWOJ Approved Probenecid increases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [41]
Bromfenac DMKB79O Approved Bromfenac decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [25]
Sulfinpyrazone DMEV954 Approved Sulfinpyrazone decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [42]
Tolvaptan DMIWFRL Approved Tolvaptan decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [43]
Macitentan DMP79A1 Approved Macitentan decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [33]
Norgestimate DMYP4XC Approved Norgestimate decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [17]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [44]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [45]
Curcumin DMQPH29 Phase 3 Curcumin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [46]
Atorvastatin DMF28YC Phase 3 Trial Atorvastatin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [27]
Chloroquine DMSI5CB Phase 3 Trial Chloroquine decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [47]
Triptolide DMCMDVR Phase 3 Triptolide decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [48]
5-methoxypsoralen DME2A8X Phase 3 5-methoxypsoralen decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [40]
Rubitecan DMDWU1S Phase 3 Rubitecan increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [49]
TAK-875 DMIM5AP Phase 3 TAK-875 decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [50]
Genistein DM0JETC Phase 2/3 Genistein increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [51]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [53]
PMID26394986-Compound-22 DM43Z1G Patented PMID26394986-Compound-22 decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [25]
PMID26560530-Compound-34 DMLGZPO Patented PMID26560530-Compound-34 increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [16]
FINROZOLE DM06SC9 Discontinued in Phase 2 FINROZOLE increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [55]
BMS 536924 DMDJH2L Preclinical BMS 536924 decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [45]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [56]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [57]
Sulforaphane DMQY3L0 Investigative Sulforaphane increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [58]
3R14S-OCHRATOXIN A DM2KEW6 Investigative 3R14S-OCHRATOXIN A decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [59]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE DMNQL17 Investigative 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [60]
Forskolin DM6ITNG Investigative Forskolin increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [7]
Chrysin DM7V2LG Investigative Chrysin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [28]
2-tert-butylbenzene-1,4-diol DMNXI1E Investigative 2-tert-butylbenzene-1,4-diol increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [29]
DM9CEI5 increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [19]
Myricetin DMTV4L0 Investigative Myricetin decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [61]
DEMETHOXYCURCUMIN DMO5UGV Investigative DEMETHOXYCURCUMIN decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [46]
Icariside II DM3DB8X Investigative Icariside II decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [62]
Formononetin DM7WFZ8 Investigative Formononetin decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [63]
chlordane DMMHU8G Investigative chlordane increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [64]
6-bromoindirubin-3-oxime DM12WYV Investigative 6-bromoindirubin-3-oxime increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [65]
7,3',4'-trihydroxyisoflavone DM5JV8G Investigative 7,3',4'-trihydroxyisoflavone decreases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [66]
GINKGOLIDE A DMKZJ7T Investigative GINKGOLIDE A increases the expression of ATP-binding cassette sub-family C member 2 (ABCC2). [67]
ROBINETIN DMASOWP Investigative ROBINETIN decreases the activity of ATP-binding cassette sub-family C member 2 (ABCC2). [61]
------------------------------------------------------------------------------------
⏷ Show the Full List of 83 Drug(s)

References

1 Neonatal Dubin-Johnson syndrome: long-term follow-up and MRP2 mutations study. Pediatr Res. 2006 Apr;59(4 Pt 1):584-9. doi: 10.1203/01.pdr.0000203093.10908.bb.
2 Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
3 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.
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 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
6 Evaluation of drug transporters' significance for multidrug resistance in head and neck squamous cell carcinoma. Head Neck. 2011 Jul;33(7):959-68. doi: 10.1002/hed.21559. Epub 2010 Aug 24.
7 Induction of cells differentiation and ABC transporters expression by a myco-estrogen, zearalenone, in human choriocarcinoma cell line (BeWo). Toxicology. 2009 Sep 19;263(2-3):100-7. doi: 10.1016/j.tox.2009.06.023. Epub 2009 Jul 4.
8 Combined effects of arsenic and palmitic acid on oxidative stress and lipid metabolism disorder in human hepatoma HepG2 cells. Sci Total Environ. 2021 May 15;769:144849. doi: 10.1016/j.scitotenv.2020.144849. Epub 2021 Jan 19.
9 In vitro study of transporters involved in intestinal absorption of inorganic arsenic. Chem Res Toxicol. 2012 Feb 20;25(2):446-53. doi: 10.1021/tx200491f. Epub 2012 Jan 26.
10 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.
11 Vitamin D3 transactivates the zinc and manganese transporter SLC30A10 via the Vitamin D receptor. J Steroid Biochem Mol Biol. 2016 Oct;163:77-87.
12 Primary Human Hepatocyte Spheroids as Tools to Study the Hepatotoxic Potential of Non-Pharmaceutical Chemicals. Int J Mol Sci. 2021 Oct 12;22(20):11005. doi: 10.3390/ijms222011005.
13 Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of talinolol in humans. Clin Pharmacol Ther. 2004 Sep;76(3):192-200.
14 Methotrexate normalizes up-regulated folate pathway genes in rheumatoid arthritis. Arthritis Rheum. 2013 Nov;65(11):2791-802.
15 Methylation-dependent silencing of the reduced folate carrier gene in inherently methotrexate-resistant human breast cancer cells. J Biol Chem. 2001 Oct 26;276(43):39990-40000.
16 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.
17 Interaction of progestins with the human multidrug resistance-associated protein 2 (MRP2). Drug Metab Dispos. 2005 Nov;33(11):1576-9.
18 Regulation of expression and activity of multidrug resistance proteins MRP2 and MDR1 by estrogenic compounds in Caco-2 cells. Role in prevention of xenobiotic-induced cytotoxicity. Toxicology. 2014 Jun 5;320:46-55. doi: 10.1016/j.tox.2014.03.007. Epub 2014 Mar 28.
19 The role of lithocholic acid in the regulation of bile acid detoxication, synthesis, and transport proteins in rat and human intestine and liver slices. Toxicol In Vitro. 2011 Feb;25(1):80-90.
20 Proteasome inhibitors MG-132 and bortezomib induce AKR1C1, AKR1C3, AKR1B1, and AKR1B10 in human colon cancer cell lines SW-480 and HT-29. Chem Biol Interact. 2011 May 30;191(1-3):239-49.
21 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
22 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.
23 A transcriptomics-based in vitro assay for predicting chemical genotoxicity in vivo. Carcinogenesis. 2012 Jul;33(7):1421-9.
24 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.
25 In vitro approach to assess the potential for risk of idiosyncratic adverse reactions caused by candidate drugs. Chem Res Toxicol. 2012 Aug 20;25(8):1616-32. doi: 10.1021/tx300091x. Epub 2012 May 31.
26 UDCA and CDCA alleviate 17-ethinylestradiol-induced cholestasis through PKA-AMPK pathways in rats. Toxicol Appl Pharmacol. 2016 Nov 15;311:12-25. doi: 10.1016/j.taap.2016.10.011. Epub 2016 Oct 12.
27 Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos. 2005 Apr;33(4):537-46.
28 Chrysin blocks topotecan-induced apoptosis in Caco-2 cells in spite of inhibition of ABC-transporters. Biochem Pharmacol. 2010 Aug 15;80(4):471-9. doi: 10.1016/j.bcp.2010.04.038. Epub 2010 May 8.
29 Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression. Toxicology. 2002 Feb 28;171(2-3):137-46.
30 Chemiluminescence quantitative immunohistochemical determination of MRP2 in liver biopsies. J Histochem Cytochem. 2005 Dec;53(12):1451-7. doi: 10.1369/jhc.5A6621.2005. Epub 2005 Jun 13.
31 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.
32 Potency of individual bile acids to regulate bile acid synthesis and transport genes in primary human hepatocyte cultures. Toxicol Sci. 2014 Oct;141(2):538-46. doi: 10.1093/toxsci/kfu151. Epub 2014 Jul 23.
33 From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells. Toxicol Sci. 2017 Jun 1;157(2):451-464. doi: 10.1093/toxsci/kfx062.
34 Bezafibrate stimulates canalicular localization of NBD-labeled PC in HepG2 cells by PPARalpha-mediated redistribution of ABCB4. J Lipid Res. 2004 Oct;45(10):1813-25. doi: 10.1194/jlr.M400132-JLR200. Epub 2004 Jul 16.
35 Pharmacological inhibition of Rho-kinase (ROCK) signaling enhances cisplatin resistance in neuroblastoma cells. Int J Oncol. 2010 Nov;37(5):1297-305. doi: 10.3892/ijo_00000781.
36 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.
37 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
38 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.
39 Antidepressant induced cholestasis: hepatocellular redistribution of multidrug resistant protein (MRP2). Gut. 2003 Feb;52(2):300-3. doi: 10.1136/gut.52.2.300.
40 ABC-transporter blockage mediated by xanthotoxin and bergapten is the major pathway for chemosensitization of multidrug-resistant cancer cells. Toxicol Appl Pharmacol. 2017 Dec 15;337:22-29. doi: 10.1016/j.taap.2017.10.018. Epub 2017 Oct 25.
41 MRP2 (ABCC2) transports taxanes and confers paclitaxel resistance and both processes are stimulated by probenecid. Int J Cancer. 2005 Sep 20;116(5):824-9. doi: 10.1002/ijc.21013.
42 Role of multidrug resistance protein 2 (MRP2, ABCC2) in alkylating agent detoxification: MRP2 potentiates glutathione S-transferase A1-1-mediated resistance to chlorambucil cytotoxicity. J Pharmacol Exp Ther. 2004 Jan;308(1):260-7. doi: 10.1124/jpet.103.057729. Epub 2003 Oct 20.
43 Inhibition of Human Hepatic Bile Acid Transporters by Tolvaptan and Metabolites: Contributing Factors to Drug-Induced Liver Injury?. Toxicol Sci. 2016 Jan;149(1):237-50. doi: 10.1093/toxsci/kfv231. Epub 2015 Oct 26.
44 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
45 Enhancement effect of resveratrol on the intestinal absorption of bestatin by regulating PEPT1, MDR1 and MRP2 in vivo and in vitro. Int J Pharm. 2015 Nov 10;495(1):588-598. doi: 10.1016/j.ijpharm.2015.09.042. Epub 2015 Sep 21.
46 Inhibition of multidrug resistance proteins MRP1 and MRP2 by a series of alpha,beta-unsaturated carbonyl compounds. Biochem Pharmacol. 2005 Jun 15;69(12):1879-90. doi: 10.1016/j.bcp.2005.04.001.
47 Autophagy inhibition upregulates CD4(+) tumor infiltrating lymphocyte expression via miR-155 regulation and TRAIL activation. Mol Oncol. 2016 Dec;10(10):1516-1531. doi: 10.1016/j.molonc.2016.08.005. Epub 2016 Sep 16.
48 Variable p53/Nrf2 crosstalk contributes to triptolide-induced hepatotoxic process. Toxicol Lett. 2023 Apr 15;379:67-75. doi: 10.1016/j.toxlet.2023.03.011. Epub 2023 Mar 28.
49 Analysis of ATP-binding cassette transporter expression in drug-selected cell lines by a microarray dedicated to multidrug resistance. Mol Pharmacol. 2004 Dec;66(6):1397-405. doi: 10.1124/mol.104.005009. Epub 2004 Sep 1.
50 Fasiglifam (TAK-875) Alters Bile Acid Homeostasis in Rats and Dogs: A Potential Cause of Drug Induced Liver Injury. Toxicol Sci. 2017 May 1;157(1):50-61. doi: 10.1093/toxsci/kfx018.
51 Resveratrol inhibits genistein-induced multi-drug resistance protein 2 (MRP2) expression in HepG2 cells. Arch Biochem Biophys. 2011 Aug 15;512(2):160-6. doi: 10.1016/j.abb.2011.06.004. Epub 2011 Jun 12.
52 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.
53 CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.
54 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.
55 The effects of aflatoxin B1 on transporters and steroid metabolizing enzymes in JEG-3 cells. Toxicol Lett. 2013 Apr 26;218(3):200-6.
56 Effects of endocrine disruptors on genes associated with 17beta-estradiol metabolism and excretion. Steroids. 2008 Nov;73(12):1242-51.
57 Characterization of the 5'-flanking region of the human multidrug resistance protein 2 (MRP2) gene and its regulation in comparison withthe multidrug resistance protein 3 (MRP3) gene. Eur J Biochem. 2000 Mar;267(5):1347-58. doi: 10.1046/j.1432-1327.2000.01106.x.
58 Reactive oxygen species-related induction of multidrug resistance-associated protein 2 expression in primary hepatocytes exposed to sulforaphane. Biochem Biophys Res Commun. 2001 Mar 23;282(1):257-63. doi: 10.1006/bbrc.2001.4531.
59 Modulation of the xenobiotic transformation system and inflammatory response by ochratoxin A exposure using a co-culture system of Caco-2 and HepG2 cells. Food Chem Toxicol. 2015 Dec;86:245-52.
60 ABCG2/BCRP decreases the transfer of a food-born chemical carcinogen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in perfused term human placenta. Toxicol Appl Pharmacol. 2008 Oct 15;232(2):210-7. doi: 10.1016/j.taap.2008.07.006. Epub 2008 Jul 18.
61 Quantitative structure activity relationship studies on the flavonoid mediated inhibition of multidrug resistance proteins 1 and 2. Biochem Pharmacol. 2005 Feb 15;69(4):699-708. doi: 10.1016/j.bcp.2004.11.002. Epub 2004 Dec 23.
62 Baohuoside I inhibits FXR signaling pathway to interfere with bile acid homeostasis via targeting ER degradation. Cell Biol Toxicol. 2023 Aug;39(4):1215-1235. doi: 10.1007/s10565-022-09737-x. Epub 2022 Jul 8.
63 Formononetin potentiates epirubicin-induced apoptosis via ROS production in HeLa cells in vitro. Chem Biol Interact. 2013 Oct 5;205(3):188-97. doi: 10.1016/j.cbi.2013.07.003. Epub 2013 Jul 16.
64 Regulation of hepatic drug transporter activity and expression by organochlorine pesticides. J Biochem Mol Toxicol. 2014 Mar;28(3):119-28.
65 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.
66 7,3',4'-Trihydroxyisoflavone modulates multidrug resistance transporters and induces apoptosis via production of reactive oxygen species. Toxicology. 2012 Dec 16;302(2-3):221-32. doi: 10.1016/j.tox.2012.08.003. Epub 2012 Aug 15.
67 Bioactive terpenoids and flavonoids from Ginkgo biloba extract induce the expression of hepatic drug-metabolizing enzymes through pregnane X receptor, constitutive androstane receptor, and aryl hydrocarbon receptor-mediated pathways. Pharm Res. 2009 Apr;26(4):872-82.
68 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.
69 Tumor necrosis factor-alpha-induced protein 3 as a putative regulator of nuclear factor-kappaB-mediated resistance to O6-alkylating agents in human glioblastomas. J Clin Oncol. 2006 Jan 10;24(2):274-87. doi: 10.1200/JCO.2005.02.9405. Epub 2005 Dec 19.
70 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.
71 Resistance to topoisomerase II inhibitors in human glioma cell lines overexpressing multidrug resistant associated protein (MRP) 2. J Med Invest. 2005 Feb;52(1-2):41-8. doi: 10.2152/jmi.52.41.
72 A mechanistic study on reduced toxicity of irinotecan by coadministered thalidomide, a tumor necrosis factor-alpha inhibitor. J Pharmacol Exp Ther. 2006 Oct;319(1):82-104. doi: 10.1124/jpet.106.103606. Epub 2006 Jun 30.
73 Genetic variants contributing to daunorubicin-induced cytotoxicity. Cancer Res. 2008 May 1;68(9):3161-8. doi: 10.1158/0008-5472.CAN-07-6381.
74 Intestinal expression of cytochrome P450 enzymes and ABC transporters and carbamazepine and phenytoin disposition. Acta Neurol Scand. 2007 Apr;115(4):232-42. doi: 10.1111/j.1600-0404.2006.00761.x.
75 The Enhanced metastatic potential of hepatocellular carcinoma (HCC) cells with sorafenib resistance. PLoS One. 2013 Nov 11;8(11):e78675. doi: 10.1371/journal.pone.0078675. eCollection 2013.
76 Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci. 2008 May;99(5):967-72.
77 Functional defect caused by the 4544G>A SNP in ABCC2: potential impact for drug cellular disposition. Pharmacogenet Genomics. 2011 Dec;21(12):884-93. doi: 10.1097/FPC.0b013e32834d672b.
78 Selenium-dependent and -independent transport of arsenic by the human multidrug resistance protein 2 (MRP2/ABCC2): implications for the mutual detoxification of arsenic and selenium. Carcinogenesis. 2010 Aug;31(8):1450-5. doi: 10.1093/carcin/bgq125. Epub 2010 Jun 27.
79 Influence of ABCB1, ABCC1, ABCC2, and ABCG2 haplotypes on the cellular exposure of nelfinavir in vivo. Pharmacogenet Genomics. 2005 Sep;15(9):599-608. doi: 10.1097/01.fpc.0000172241.42546.d3.
80 Effects of fibrates on human organic anion-transporting polypeptide 1B1-, multidrug resistance protein 2- and P-glycoprotein-mediated transport. Xenobiotica. 2005 Jul;35(7):737-53.
81 Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol. 2005 Sep;68(3):800-7.
82 Mrp2 is involved in the efflux and disposition of fosinopril. J Appl Toxicol. 2013 Jun;33(6):458-65. doi: 10.1002/jat.1767. Epub 2011 Nov 17.
83 MRP2 involvement in renal proximal tubular elimination of methylmercury mediated by DMPS or DMSA. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):10-7.
84 Coordinated induction of GST and MRP2 by cAMP in Caco-2 cells: role of protein kinase A signaling pathway and toxicological relevance. Toxicol Appl Pharmacol. 2015 Sep 1;287(2):178-190.
85 Transport of the investigational anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid and its acyl glucuronide by human intestinal Caco-2 cells. Eur J Pharm Sci. 2005 Apr;24(5):513-24. doi: 10.1016/j.ejps.2005.01.006.
86 Hepatic transport of PKI166, an epidermal growth factor receptor kinase inhibitor of the pyrrolo-pyrimidine class, and its main metabolite, ACU154. Drug Metab Dispos. 2004 Nov;32(11):1272-8. doi: 10.1124/dmd.104.000497. Epub 2004 Jul 27.
87 Human MRP2 exports MC-LR but not the glutathione conjugate. Chem Biol Interact. 2019 Sep 25;311:108761. doi: 10.1016/j.cbi.2019.108761. Epub 2019 Jul 23.
88 Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2. Biochem Pharmacol. 2005 Feb 1;69(3):415-23.
89 Molecular mechanisms governing different pharmacokinetics of ginsenosides and potential for ginsenoside-perpetrated herb-drug interactions on OATP1B3. Br J Pharmacol. 2015 Feb;172(4):1059-73. doi: 10.1111/bph.12971. Epub 2015 Jan 20.
90 ATP-binding cassette transporters as pitfalls in selection of transgenic cells. Anal Biochem. 2010 Apr 15;399(2):246-50. doi: 10.1016/j.ab.2009.12.014. Epub 2009 Dec 14.
91 Mutation of Trp1254 in the multispecific organic anion transporter, multidrug resistance protein 2 (MRP2) (ABCC2), alters substrate specificity and results in loss of methotrexate transport activity. J Biol Chem. 2001 Oct 12;276(41):38108-14. doi: 10.1074/jbc.M105160200. Epub 2001 Aug 10.
92 Identification and functional analysis of two novel mutations in the multidrug resistance protein 2 gene in Israeli patients with Dubin-Johnson syndrome. J Biol Chem. 2001 Oct 5;276(40):36923-30. doi: 10.1074/jbc.M105047200. Epub 2001 Jul 26.