Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTIMJ02)

DTT Name	ATP-binding cassette transporter G2 (ABCG2)
Synonyms	Urate exporter; Placenta-specific ATP-binding cassette transporter; Mitoxantrone resistance-associated protein; MXR; CDw338; CD338; Breast cancer resistance protein; BCRP1; BCRP; ABCP
Gene Name	ABCG2
DTT Type	Successful target	[1]
BioChemical Class	ABC transporter
UniProt ID	ABCG2_HUMAN
TTD ID	T56556
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
Sequence	MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
Function	Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. Implicated in the efflux of numerous drugs and xenobiotics: mitoxantrone, the photosensitizer pheophorbide, camptothecin, methotrexate, azidothymidine (AZT), and the anthracyclines daunorubicin and doxorubicin. High-capacity urate exporter functioning in both renal and extrarenal urate excretion.
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 ) Heme biosynthesis (R-HSA-189451 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[1]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Rheumatoid arthritis	FA20	Synovial tissue	5.91E-02	0.39	0.65
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The Drug Transporter (DTP) Role of This DTT

DTT DTP Name

Breast cancer resistance protein (ABCG2) DTP Info

Gene Name

ABCG2

127 Approved Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Abacavir	DMMN36E	Human immunodeficiency virus infection	1C62	Approved	[2]
Aciclovir	DMYLOVR	Genital herpes	1A94	Approved	[3]
Adefovir	DMM278X	N. A.	N. A.	Approved	[4]
Alfuzosin	DMZVMKF	Benign prostatic hyperplasia	GA90	Approved	[5]
Apixaban	DM89JLN	Thrombosis	DB61-GB90	Approved	[6]
ARRY-162	DM1P6FR	Melanoma	2C30	Approved	[7]
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[8]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[9]
Bicalutamide	DMZMSPF	Prostate cancer	2C82.0	Approved	[10]
Brigatinib	DM7W94S	Anaplastic large cell lymphoma	2A90.A	Approved	[11]
Bupropion	DM5PCS7	Depression	6A70-6A7Z	Approved	[12]
Canagliflozin	DMFRM1I	Non-insulin dependent diabetes	5A11	Approved	[13]
Cephalothin Sodium	DM51Z9E	Bacterial infection	1A00-1C4Z	Approved	[14]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[15]
Chlorothiazide	DMLHESP	Chronic heart failure	BD1Z	Approved	[16]
Cholic Acid	DM7OKQV	Cholelithiasis	DC11	Approved	[17]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Cimetidine	DMH61ZB	Acid-reflux disorder	DA22	Approved	[18]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[19]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[20]
Cladribine	DM3JDRP	Hairy cell leukaemia	2A82.2	Approved	[21]
Clofarabine	DMCVJ86	Acute lymphoblastic leukaemia	2A85	Approved	[21]
Dabrafenib	DMX6OE3	Melanoma	2C30	Approved	[22]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[23]
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[24]
Daunorubicin	DMQUSBT	Acute monocytic leukemia		Approved	[25]
Dehydroepiandrosterone sulfate	DM4Q80H	N. A.	N. A.	Approved	[26]
Delavirdine	DM3NF5G	Human immunodeficiency virus infection	1C62	Approved	[15]
Deoxycholic acid	DM3GYAL	Subcutaneous fat disorder	EF02	Approved	[14]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[27]
Dipyridamole	DMXY30O	Atrial fibrillation	BC81.3	Approved	[28]
Dirithromycin	DM0D9YJ	Bacterial infection	1A00-1C4Z	Approved	[14]
Docetaxel	DMDI269	Advanced cancer	2A00-2F9Z	Approved	[29]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[30]
Eltrombopag	DMOGFIX	Thrombocytopenia	3B64	Approved	[31]
Empagliflozin	DMRF9YK	Type-1 diabetes	5A10	Approved	[32]
Entacapone	DMLBVKQ	Parkinson disease	8A00.0	Approved	[33]
Entecavir	DM7VTQO	Hepatitis B virus infection	1E51.0	Approved	[34]
Epirubicin	DMPDW6T	Solid tumour/cancer	2A00-2F9Z	Approved	[15]
Erlotinib	DMCMBHA	Adrenal gland neoplasm		Approved	[35]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[28]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[36]
Estrone sulfate	DMVBIZL	Atrophic vaginitis	GA30.2	Approved	[37]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[38]
Ezetimibe	DM7A8TW	Atherosclerosis	BD40	Approved	[39]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[40]
Fluvastatin	DM4MDJY	Arteriosclerosis	BD40	Approved	[41]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[42]
Ganciclovir	DM1MBYQ	Cytomegalovirus infection	1D82	Approved	[43]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[15]
Glibenclamide	DM8JXPZ	Diabetic complication	5A2Y	Approved	[44]
Glutathione	DMAHMT9	Human immunodeficiency virus infection	1C62	Approved	[45]
Grepafloxacin	DMGLX0T	Chronic bronchitis	CA20.1	Approved	[46]
Hesperetin	DMKER83	High blood cholesterol level	5C80.00	Approved	[47]
Hydroxychloroquine	DMSIVND	Chronic renal failure	GB61.Z	Approved	[48]
Idarubicin	DMM0XGL	Acute myelogenous leukaemia	2A41	Approved	[49]
Idelalisib	DM602WT	Chronic lymphocytic leukaemia	2A82.0	Approved	[50]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[51]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[52]
Lamivudine	DMI347A	Chronic HBV infection	1E51.0Z	Approved	[53]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[54]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[55]
Lopinavir	DMITQS0	Human immunodeficiency virus infection	1C62	Approved	[15]
Menadione	DMSJDTY	Vitamin K deficiency	5B59	Approved	[56]
Mercaptopurine	DMTM2IK	Acute lymphoblastic leukaemia	2A85	Approved	[4]
Metformin	DM89QE1	Colorectal carcinoma		Approved	[57]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[58]
Mitoxantrone	DMM39BF	Acute myelogenous leukaemia	2A41	Approved	[25]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[59]
Nicardipine	DMCDYW7	High blood pressure	BA00	Approved	[15]
Nifurtimox	DMSQLZJ	Chagas disease	IF53	Approved	[60]
Nilotinib	DM7HXWT	Chronic myelogenous leukaemia	2A20.0	Approved	[24]
Nitrofurantoin	DM7PQIK	Urinary tract infection	GC08	Approved	[61]
Norfloxacin	DMIZ6W2	Acute gonococcal cervicitis		Approved	[62]
Ofloxacin	DM0VQN3	Acute gonococcal cervicitis		Approved	[15]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[32]
Oxaliplatin	DMQNWRD	Adenocarcinoma	2D40	Approved	[63]
Paclitaxel	DMLB81S	Breast carcinoma		Approved	[29]
Palbociclib	DMD7L94	Breast cancer	2C60-2C65	Approved	[64]
Pantoprazole	DMSVOCZ	Gastrinoma	2C10.1	Approved	[65]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[66]
Pemetrexed	DMMX2E6	Central nervous system lymphoma	2B33.5	Approved	[67]
Pirarubicin	DMGTW1I	Breast cancer	2C60-2C65	Approved	[40]
Pitavastatin	DMJH792	Hypercholesterolaemia	5C80.0	Approved	[28]
PITAVASTATIN CALCIUM	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[68]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[69]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[70]
Pravastatin	DM6A0X7	Adult acute monocytic leukemia		Approved	[15]
Prazosin	DMCD9YG	Benign prostatic hyperplasia	GA90	Approved	[71]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[36]
Pyrimethamine	DM5X7VY	Malaria	1F40-1F45	Approved	[72]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[15]
Rabeprazole	DMMZXIW	Bacterial infection	1A00-1C4Z	Approved	[73]
Raltitrexed	DMT9K8G	Rectal adenocarcinoma	2B92	Approved	[74]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[32]
Reserpine	DM6VM38	Hypertension	BA00-BA04	Approved	[15]
Riboflavin	DM8YMWE	Acne vulgaris	ED80	Approved	[75]
Rifampin	DMA8J1G	Tuberculosis	1B10-1B1Z	Approved	[14]
Riluzole	DMECBWN	Amyotrophic lateral sclerosis	8B60.0	Approved	[76]
Riociguat	DMXBLMP	Chronic thromboembolic pulmonary hypertension		Approved	[32]
Rivaroxaban	DMQMBZ1	Deep vein thrombosis	BD71	Approved	[77]
Rosiglitazone	DMILWZR	Chronic kidney disease	GB61	Approved	[78]
Rosuvastatin	DMMIQ7G	Arteriosclerosis	BD40	Approved	[79]
Saquinavir	DMG814N	Human immunodeficiency virus infection	1C62	Approved	[80]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[70]
Sofosbuvir	DMQI86A	Hepatitis C	1E51	Approved	[32]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[81]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[82]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[81]
Talazoparib	DM1KS78	Breast cancer	2C60-2C65	Approved	[83]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[84]
Teniposide	DMLW57T	Acute lymphoblastic leukaemia	2A85	Approved	[15]
Tenofovir	DM1IS6U	Chronic hepatitis B virus infection		Approved	[32]
Tenofovir alafenamide	DMTQF4A	Hiv infectious disease		Approved	[85]
Teriflunomide	DMQ2FKJ	Hyperlipidaemia	5C80	Approved	[48]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[86]
Tetracycline	DMZA017	Acne vulgaris	ED80	Approved	[14]
Thioguanine	DM7NKEV	Acute lymphocytic leukaemia	2B33.3	Approved	[4]
Topotecan	DMP6G8T	Central nervous system neoplasm		Approved	[87]
Trimetrexate	DMDEA85	Toxoplasmosis	1F57	Approved	[72]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[88]
Verteporfin	DMIY6DB	Choroidal neovascularization	9B76	Approved	[89]
Vinblastine	DM5TVS3	Advanced cancer	2A00-2F9Z	Approved	[29]
Vincristine	DMINOX3	Acute lymphoblastic leukaemia	2A85	Approved	[72]
VRX496	DMIO4V5	Acquired immune deficiency syndrome	1C62.3	Approved	[15]
YN-968D1	DMMP3Y2	Breast cancer	2C60-2C65	Approved	[90]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[15]
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⏷ Show the Full List of 127 Approved Drug(s)

29 Clinical Trial Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Camptothecin	DM6CHNJ	Solid tumour/cancer	2A00-2F9Z	Phase 3	[91]
Edotecarin	DM3ZL7D	Gastric adenocarcinoma	2B72	Phase 3	[74]
Exatecan	DMCA7FN	Solid tumour/cancer	2A00-2F9Z	Phase 3	[74]
Karenitecin	DMCRGY4	Lung cancer	2C25.0	Phase 3	[74]
Nolatrexed	DMOF0CA	Solid tumour/cancer	2A00-2F9Z	Phase 3	[72]
Resveratrol	DM3RWXL	Giant cell arteritis	4A44.2	Phase 3	[42]
Synthetic hypericin	DMXU4ON	Virus infection	1A24-1D9Z	Phase 3	[92]
Genistein	DM0JETC	Menopause symptom	GA30.0	Phase 2/3	[93]
9-AMINOCAMPTOTHECIN	DMQXYRG	Acquired immune deficiency syndrome	1C62.3	Phase 2	[74]
Bisantrene	DMW76V0	N. A.	N. A.	Phase 2	[74]
CKD602	DMW9F1G	Solid tumour/cancer	2A00-2F9Z	Phase 2	[94]
CP-724714	DMUJ0W7	Lymphoma	2A80-2A86	Phase 2	[95]
DIFLOMOTECAN	DM20ATW	Solid tumour/cancer	2A00-2F9Z	Phase 2	[74]
Flavopiridol	DMKSUOI	Acute myeloid leukaemia	2A60	Phase 2	[96]
Gimatecan	DMSKMET	Breast cancer	2C60-2C65	Phase 2	[74]
HPPH	DM25PQB	N. A.	N. A.	Phase 2	[97]
LE-SN38	DMW50NF	Colorectal cancer	2B91.Z	Phase 2	[98]
NSC-645809	DMPJQZG	Breast cancer	2C60-2C65	Phase 2	[99]
Ortataxel	DM1EK5D	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]
Oxfendazole	DMSNL51	N. A.	N. A.	Phase 2	[100]
PEITC	DMOMN31	Prostate cancer	2C82.0	Phase 2	[26]
PIRITREXIM	DM276N1	Bladder cancer	2C94	Phase 2	[72]
UCN-01	DMUNJZB	Non-small-cell lung cancer	2C25.Y	Phase 2	[74]
BN-2629	DMA9MP5	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[101]
Taurocholic Acid	DM2LZ8F	Type-2 diabetes	5A11	Phase 1/2	[17]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[26]
Benzoylphenylurea	DMMW4HV	N. A.	N. A.	Phase 1	[102]
Mycophenolic acid glucuronide	DM5O4X9	N. A.	N. A.	Phase 1	[59]
Sphingosine-1-phosphate	DMJCQKA	Acne vulgaris	ED80	Phase 1	[103]
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⏷ Show the Full List of 29 Clinical Trial Drug(s)

7 Discontinued Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Parabis	DMDKXYC	N. A.	N. A.	Withdrawn from market	[104]
BECATECARIN	DMRQV8I	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 3	[105]
Befloxatone	DMZIV6D	Major depressive disorder	6A70.3	Discontinued in Phase 3	[106]
E-3040	DM35KZG	Thrombosis	DB61-GB90	Discontinued in Phase 2	[107]
Lurtotecan	DMF1RTW	Ovarian cancer	2C73	Discontinued in Phase 2	[26]
NB-506	DMGVYXB	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[74]
Rhodamine-123	DMQAK6T	Prostate cancer	2C82.0	Discontinued in Phase 1	[108]
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9 Preclinical Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Azidothymidine monophosphate	DM3FLMR	N. A.	N. A.	Preclinical	[107]
Barasertib-hQPA	DMTJZIL	N. A.	N. A.	Preclinical	[109]
BMS 536924	DMDJH2L	N. A.	N. A.	Preclinical	[110]
Enrofloxacin	DMK6WIO	N. A.	N. A.	Preclinical	[111]
Homocamptothecin	DMBQDA3	N. A.	N. A.	Preclinical	[112]
N-desethyl sunitinib	DM5ATJ0	N. A.	N. A.	Preclinical	[113]
Pancratistatin	DM3YUGA	N. A.	N. A.	Preclinical	[114]
Puromycin	DMDKLB5	N. A.	N. A.	Preclinical	[26]
Scutellarin	DMJT1E5	N. A.	N. A.	Preclinical	[115]
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⏷ Show the Full List of 9 Preclinical Drug(s)

14 Investigative Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Butanoic Acid	DMTAJP7	Discovery agent	N.A.	Investigative	[116]
Cholesterol	DMR3J6S	Discovery agent	N.A.	Investigative	[36]
Chrysin	DM7V2LG	Discovery agent	N.A.	Investigative	[15]
COUMESTROL	DM40TBU	Discovery agent	N.A.	Investigative	[117]
daidzein	DMRFTJX	Discovery agent	N.A.	Investigative	[117]
glycocholic acid	DM0SXNM	Discovery agent	N.A.	Investigative	[17]
Hematoporphyrin	DMVK36Q	N. A.	N. A.	Investigative	[118]
JNJ-7706621	DMHTYBS	Discovery agent	N.A.	Investigative	[119]
Mepacrine	DMU8L7C	Discovery agent	N.A.	Investigative	[14]
phosphatidylserine	DM76TSG	Discovery agent	N.A.	Investigative	[120]
Protoporphyrin IX	DMWYE7A	Discovery agent	N.A.	Investigative	[74]
Tyrphostin ag-1478	DM87ZIH	Discovery agent	N.A.	Investigative	[20]
uric acid	DMA1MKT	Discovery agent	N.A.	Investigative	[121]
[3H]estradiol-17beta-glucuronide	DM3KJ45	Discovery agent	N.A.	Investigative	[122]
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⏷ Show the Full List of 14 Investigative Drug(s)

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27	Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone. Drug Metab Dispos. 2009 Jan;37(1):129-36.
28	ABCG2: a perspective. Adv Drug Deliv Rev. 2009 Jan 31;61(1):3-13.
29	Ixabepilone, a novel microtubule-targeting agent for breast cancer, is a substrate for P-glycoprotein (P-gp/MDR1/ABCB1) but not breast cancer resistance protein (BCRP/ABCG2). J Pharmacol Exp Ther. 2011 May;337(2):423-32.
30	Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
31	Assessment of the pharmacokinetic interaction between eltrombopag and lopinavir-ritonavir in healthy adult subjects. Antimicrob Agents Chemother. 2012 Jun;56(6):2846-51.
32	KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
33	Elucidation of the Impact of P-glycoprotein and Breast Cancer Resistance Protein on the Brain Distribution of Catechol-O-Methyltransferase Inhibitors. Drug Metab Dispos. 2017 Dec;45(12):1282-1291.
34	Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
35	Functions of the breast cancer resistance protein (BCRP/ABCG2) in chemotherapy. Adv Drug Deliv Rev. 2009 Jan 31;61(1):26-33.
36	Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
37	ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem. 2003 Jun 20;278(25):22644-9.
38	Characterization of 3-methoxy flavones for their interaction with ABCG2 as suggested by ATPase activity. Biochim Biophys Acta. 2014 Nov;1838(11):2929-38.
39	Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab Dispos. 2009 Aug;37(8):1698-702.
40	Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
41	Evaluation of the usefulness of breast cancer resistance protein (BCRP) knockout mice and BCRP inhibitor-treated monkeys to estimate the clinical impact of BCRP modulation on the pharmacokinetics of BCRP substrates. Pharm Res. 2015 May;32(5):1634-47.
42	The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
43	Side populations of glioblastoma cells are less sensitive to HSV-TK/GCV suicide gene therapy system than the non-side population. In Vitro Cell Dev Biol Anim. 2010 Jun;46(6):497-501.
44	Glyburide transport across the human placenta. Obstet Gynecol. 2015 Mar;125(3):583-8.
45	Glutathione transport is a unique function of the ATP-binding cassette protein ABCG2. J Biol Chem. 2010 May 28;285(22):16582-7.
46	Involvement of breast cancer resistance protein (ABCG2) in the biliary excretion mechanism of fluoroquinolones. Drug Metab Dispos. 2007 Oct;35(10):1873-9.
47	Interaction of the breast cancer resistance protein with plant polyphenols. Biochem Biophys Res Commun. 2004 Apr 23;317(1):269-75.
48	MDR-ABC transporters: biomarkers in rheumatoid arthritis. Clin Exp Rheumatol. 2013 Sep-Oct;31(5):779-87.
49	Amonafide L-malate is not a substrate for multidrug resistance proteins in secondary acute myeloid leukemia. Leukemia. 2008 Nov;22(11):2110-5.
50	DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB09054)
51	Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
52	Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Cancer Chemother Pharmacol. 2006 Sep;58(3):374-83.
53	The effect of ABCG2 V12M, Q141K and Q126X, known functional variants in vitro, on the disposition of lamivudine. Br J Clin Pharmacol. 2007 Nov;64(5):645-54.
54	The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Drug Metab Dispos. 2008 Apr;36(4):695-701.
55	Leflunomide and its metabolite A771726 are high affinity substrates of BCRP: implications for drug resistance. Ann Rheum Dis. 2009 Jul;68(7):1201-7.
56	The naphthoquinones, vitamin K3 and its structural analogue plumbagin, are substrates of the multidrug resistance linked ATP binding cassette drug transporter ABCG2. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3279-86.
57	Role of human placental apical membrane transporters in the efflux of glyburide, rosiglitazone, and metformin. Am J Obstet Gynecol. 2010 Apr;202(4):383.e1-7.
58	Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
59	Influence of drug transporters and UGT polymorphisms on pharmacokinetics of phenolic glucuronide metabolite of mycophenolic acid in Japanese renal transplant recipients. Ther Drug Monit. 2008 Oct;30(5):559-64.
60	The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Brain Res. 2012 Feb 3;1436:111-21.
61	The breast cancer resistance protein (BCRP/ABCG2) affects pharmacokinetics, hepatobiliary excretion, and milk secretion of the antibiotic nitrofurantoin. Mol Pharmacol. 2005 May;67(5):1758-64.
62	Breast cancer resistance protein (BCRP/ABCG2) transports fluoroquinolone antibiotics and affects their oral availability, pharmacokinetics, and milk secretion. Drug Metab Dispos. 2006 Apr;34(4):690-5.
63	Effect of ABCG2 on cytotoxicity of platinum drugs: interference of EGFP. Toxicol In Vitro. 2008 Dec;22(8):1846-52.
64	Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model. J Pharmacol Exp Ther. 2015 Nov;355(2):264-71.
65	Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions. Cancer Res. 2004 Aug 15;64(16):5804-11.
66	Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53.
67	pH-Dependent transport of pemetrexed by breast cancer resistance protein. Drug Metab Dispos. 2011 Sep;39(9):1478-85.
68	Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol. 2005 Sep;68(3):800-7.
69	DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB08901)
70	Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
71	P-glycoprotein and breast cancer resistance protein expression and function at the blood-brain barrier and blood-cerebrospinal fluid barrier (choroid plexus) in streptozotocin-induced diabetes in rats. Brain Res. 2011 Jan 25;1370:238-45.
72	Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates. Cancer Chemother Pharmacol. 2006 Dec;58(6):826-34.
73	Co-administration of proton pump inhibitors delays elimination of plasma methotrexate in high-dose methotrexate therapy. Br J Clin Pharmacol. 2009 Jan;67(1):44-9.
74	Pharmacogenomic importance of ABCG2. Pharmacogenomics. 2008 Aug;9(8):1005-9.
75	Multidrug transporter ABCG2/breast cancer resistance protein secretes riboflavin (vitamin B2) into milk. Mol Cell Biol. 2007 Feb;27(4):1247-53.
76	Interactions between riluzole and ABCG2/BCRP transporter. Neurosci Lett. 2009 Mar 6;452(1):12-6.
77	Absence of both MDR1 (ABCB1) and breast cancer resistance protein (ABCG2) transporters significantly alters rivaroxaban disposition and central nervous system entry. Basic Clin Pharmacol Toxicol. 2013 Mar;112(3):164-70.
78	ATP-binding cassette transporters in human heart failure. Naunyn Schmiedebergs Arch Pharmacol. 2008 May;377(3):231-43.
79	Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
80	Nicotine and cotinine increases the brain penetration of saquinavir in rat. J Neurochem. 2010 Dec;115(6):1495-507.
81	Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier. Mol Pharm. 2011 Apr 4;8(2):571-82.
82	Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
83	DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB11760)
84	The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
85	Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals. J Acquir Immune Defic Syndr. 2018 Aug 1;78(4):465-472.
86	Association of the ABCG2 C421A polymorphism with prostate cancer risk and survival. BJU Int. 2008 Dec;102(11):1694-9.
87	Differential inhibition of murine Bcrp1/Abcg2 and human BCRP/ABCG2 by the mycotoxin fumitremorgin C. Eur J Pharmacol. 2010 Oct 10;644(1-3):41-8.
88	Tyrosine kinase inhibitors and multidrug resistance proteins: interactions and biological consequences. Cancer Chemother Pharmacol. 2010 Jan;65(2):335-46.
89	The tyrosine kinase inhibitor imatinib mesylate enhances the efficacy of photodynamic therapy by inhibiting ABCG2. Clin Cancer Res. 2007 Apr 15;13(8):2463-70.
90	Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters. Cancer Res. 2010 Oct 15;70(20):7981-91.
91	The beta-carboline alkaloid harmine inhibits BCRP and can reverse resistance to the anticancer drugs mitoxantrone and camptothecin in breast cancer cells. Phytother Res. 2010 Jan;24(1):146-9.
92	Drug efflux transporters, MRP1 and BCRP, affect the outcome of hypericin-mediated photodynamic therapy in HT-29 adenocarcinoma cells. Photochem Photobiol Sci. 2009 Dec;8(12):1716-23.
93	Differential selectivity of efflux transporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: a strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2. J Pharm Sci. 2012 May;101(5):1888-97.
94	Involvement of P-glycoprotein, multidrug resistance protein 2 and breast cancer resistance protein in the transport of belotecan and topotecan in Caco-2 and MDCKII cells. Pharm Res. 2008 Nov;25(11):2601-12.
95	Multi-drug-resistance-reverting agents: 2-aryloxazole and 2-arylthiazole derivatives as potent BCRP or MRP1 inhibitors. ChemMedChem. 2009 Feb;4(2):188-95.
96	The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2. Mol Cancer Ther. 2012 Sep;11(9):2033-44.
97	Substrate affinity of photosensitizers derived from chlorophyll-a: the ABCG2 transporter affects the phototoxic response of side population stem cell-like cancer cells to photodynamic therapy. Mol Pharm. 2010 Oct 4;7(5):1789-804.
98	Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells. Biochem Biophys Res Commun. 2001 Nov 9;288(4):827-32.
99	C421 allele-specific ABCG2 gene amplification confers resistance to the antitumor triazoloacridone C-1305 in human lung cancer cells. Biochem Pharmacol. 2007 Jun 30;74(1):41-53.
100	Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2). Drug Metab Dispos. 2005 May;33(5):614-8.
101	Optimization of the antitumor activity of sequence-specific pyrrolobenzodiazepine derivatives based on their affinity for ABC transporters. AAPS J. 2010 Dec;12(4):617-27.
102	American Association for Cancer Research.
103	Estradiol induces export of sphingosine 1-phosphate from breast cancer cells via ABCC1 and ABCG2. J Biol Chem. 2010 Apr 2;285(14):10477-86.
104	Human and rat ABC transporter efflux of bisphenol a and bisphenol a glucuronide: interspecies comparison and implications for pharmacokinetic assessment. Toxicol Sci. 2012 Aug;128(2):317-25.
105	Becatecarin (rebeccamycin analog, NSC 655649) is a transport substrate and induces expression of the ATP-binding cassette transporter, ABCG2, in lung carcinoma cells. Cancer Chemother Pharmacol. 2009 Aug;64(3):575-83.
106	Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening. J Nucl Med. 2011 Mar;52(3):415-23.
107	Role of the breast cancer resistance protein (ABCG2) in drug transport. AAPS J. 2005 May 11;7(1):E118-33.
108	Alectinib (CH5424802) antagonizes ABCB1- and ABCG2-mediated multidrug resistance in vitro, in vivo and ex vivo. Exp Mol Med. 2017 Mar 17;49(3):e303.
109	P-glycoprotein and breast cancer resistance protein in acute myeloid leukaemia cells treated with the aurora-B kinase inhibitor barasertib-hQPA. BMC Cancer. 2011 Jun 16;11:254.
110	Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924. Mol Cancer Ther. 2011 Jan;10(1):117-25.
111	Interaction of enrofloxacin with breast cancer resistance protein (BCRP/ABCG2): influence of flavonoids and role in milk secretion in sheep. J Vet Pharmacol Ther. 2006 Aug;29(4):279-87.
112	ABCG2: determining its relevance in clinical drug resistance. Cancer Metastasis Rev. 2007 Mar;26(1):39-57.
113	P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. J Pharmacol Exp Ther. 2012 Apr;341(1):164-73.
114	Identification of compounds that correlate with ABCG2 transporter function in the National Cancer Institute Anticancer Drug Screen. Mol Pharmacol. 2009 Nov;76(5):946-56.
115	Mechanistic studies on the absorption and disposition of scutellarin in humans: selective OATP2B1-mediated hepatic uptake is a likely key determinant for its unique pharmacokinetic characteristics. Drug Metab Dispos. 2012 Oct;40(10):2009-20.
116	The short-chain fatty acid butyrate is a substrate of breast cancer resistance protein. Am J Physiol Cell Physiol. 2011 Nov;301(5):C984-94.
117	Effect of breast cancer resistance protein (Bcrp/Abcg2) on the disposition of phytoestrogens. Mol Pharmacol. 2007 Oct;72(4):967-75.
118	Cellular phototoxicity evoked through the inhibition of human ABC transporter ABCG2 by cyclin-dependent kinase inhibitors in vitro. Pharm Res. 2009 Feb;26(2):449-58.
119	Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor. Mol Cancer Ther. 2006 Oct;5(10):2459-67.
120	ABCG2: a potential marker of stem cells and novel target in stem cell and cancer therapy. Life Sci. 2010 Apr 24;86(17-18):631-7.
121	Extra-renal elimination of uric acid via intestinal efflux transporter BCRP/ABCG2. PLoS One. 2012;7(2):e30456.
122	Regulation of the function of the human ABCG2 multidrug transporter by cholesterol and bile acids: effects of mutations in potential substrate and steroid binding sites. Drug Metab Dispos. 2014 Apr;42(4):575-85.