Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DTI7UX6)

• DTP Name: Breast cancer resistance protein (ABCG2)
• Gene Name: ABCG2
• UniProt ID: Q9UNQ0 (ABCG2_HUMAN)
• VARIDT ID: DTD0004
• Synonyms: ABC15; ABCG2; ABCP; ATP-binding cassette sub-family G member 2; BCRP; BCRP1; BMDP; CD338; CDw338; EST157481; GOUT1; MRX; MXR; MXR-1; MXR1; Mitoxantrone resistance-associated protein; Placenta-specific ATP-binding cassette transporter; UAQTL1; Urate exporter; hABCG2
• DTP Family:
  ATP-Binding Cassette (ABC) Superfamily
  Eye Pigment Precursor Transporter (EPP) Family (ABCG)
• Tissue Specificity: Intestinal enterocyte, hepatocyte (canalicular), kidney proximal tubule, brain endothelia, placenta, stem cells, mammary gland (lactating), expressed at high levels on the apical surface of many tumor cell lines
• Sequence:
  MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
  KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
  SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
  QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
  SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
  DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
  ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
  TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
  MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
  MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
  NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
• Function: This transporter functioned in both renal and extrarenal urate excretion. 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.
• Endogenous Substrate(s): Bisbenzimide; Pheophorbide A
• TCDB ID: 3.A.1.204.2
• Gene ID: 9429
• 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 DTP

127 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Abacavir	DMMN36E	Human immunodeficiency virus infection	1C62	Approved	[2]
Aciclovir	DMYLOVR	Virus infection	1A24-1D9Z	Approved	[3]
Adefovir	DMM278X	Hepatitis B virus infection	1E51.0	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	Smoking dependence	6C4A.2	Approved	[12]
Canagliflozin	DMFRM1I	Type-2 diabetes	5A11	Approved	[13]
Cephalothin sodium	DM51Z9E	Bacterial infection	1A00-1C4Z	Approved	[14]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[15]
Chlorothiazide	DMLHESP	Congestive heart failure	BD10	Approved	[16]
Cholic acid	DM7OKQV	Peroxisomal disorder	5C57	Approved	[17]
Ciclosporin	DMT2KRV	Psoriasis vulgaris	EA90	Approved	[15]
Cimetidine	DMH61ZB	Acid-reflux disorder	DA22	Approved	[18]
Ciprofloxacin XR	DM2NLS9	Bacterial infection	1A00-1C4Z	Approved	[19]
Cisplatin	DMRHGI9	Solid tumour/cancer	2A00-2F9Z	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	Solid tumour/cancer	2A00-2F9Z	Approved	[23]
Dasatinib	DMJV2EK	Chronic myelogenous leukaemia	2A20.0	Approved	[24]
Daunorubicin	DMQUSBT	Acute myeloid leukaemia	2A60	Approved	[25]
Dehydroepiandrosterone sulfate	DM4Q80H	Dyspareunia	GA12	Approved	[26]
Delavirdine	DM3NF5G	Human immunodeficiency virus infection	1C62	Approved	[15]
Deoxycholic acid	DM3GYAL	N. A.	N. A.	Approved	[14]
Diclofenac	DMPIHLS	Osteoarthritis	FA00-FA05	Approved	[27]
Dipyridamole	DMXY30O	Hypertension	BA00-BA04	Approved	[28]
Dirithromycin	DM0D9YJ	Bacterial infection	1A00-1C4Z	Approved	[14]
Docetaxel	DMDI269	Solid tumour/cancer	2A00-2F9Z	Approved	[29]
Doxorubicin	DMVP5YE	Solid tumour/cancer	2A00-2F9Z	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	Non-small-cell lung cancer	2C25.Y	Approved	[35]
Erythromycin	DM4K7GQ	Bacterial infection	1A00-1C4Z	Approved	[28]
Estradiol	DMUNTE3	Breast cancer	2C60-2C65	Approved	[36]
Estrone sulfate	DMVBIZL	Menopausal and postmenopausal disorder	GA30	Approved	[37]
Estrone sulfate	DMVBIZL	Menopausal and postmenopausal disorder	GA30	Approved	[38]
Etoposide	DMNH3PG	Solid tumour/cancer	2A00-2F9Z	Approved	[39]
Ezetimibe	DM7A8TW	Hypercholesterolaemia	5C80.0	Approved	[40]
Fluorouracil	DMUM7HZ	Solid tumour/cancer	2A00-2F9Z	Approved	[41]
Fluvastatin	DM4MDJY	Hypercholesterolaemia	5C80.0	Approved	[42]
Folic acid	DMEMBJC	Folate-deficiency anemia	3A02.Y	Approved	[43]
Ganciclovir	DM1MBYQ	Virus infection	1A24-1D9Z	Approved	[44]
Gefitinib	DM15F0X	Solid tumour/cancer	2A00-2F9Z	Approved	[15]
Glibenclamide	DM8JXPZ	Diabetic complication	5A2Y	Approved	[45]
Glutathione	DMAHMT9	Human immunodeficiency virus infection	1C62	Approved	[46]
Grepafloxacin	DMGLX0T	Chronic bronchitis	CA20.1	Approved	[47]
Hesperetin	DMKER83	High blood cholesterol level	5C80.00	Approved	[48]
Hydroxychloroquine	DMSIVND	Malaria	1F40-1F45	Approved	[49]
Idarubicin	DMM0XGL	Acute myeloid leukaemia	2A60	Approved	[50]
Idelalisib	DM602WT	Chronic lymphocytic leukaemia	2A82.0	Approved	[51]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[52]
Irinotecan	DMP6SC2	Colorectal cancer	2B91.Z	Approved	[53]
Lamivudine	DMI347A	Chronic HBV infection	1E51.0Z	Approved	[54]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[55]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[56]
Lopinavir	DMITQS0	Human immunodeficiency virus infection	1C62	Approved	[15]
Menadione	DMSJDTY	Vitamin K deficiency	5B59	Approved	[57]
Mercaptopurine	DMTM2IK	Acute lymphoblastic leukaemia	2A85	Approved	[4]
Metformin	DM89QE1	Type-2 diabetes	5A11	Approved	[58]
Methotrexate	DM2TEOL	leukaemia	2A60-2B33	Approved	[59]
Mitoxantrone	DMM39BF	Solid tumour/cancer	2A00-2F9Z	Approved	[25]
Mycophenolate mofetil	DMPQAGE	Organ transplant rejection	NE84	Approved	[60]
Nicardipine	DMCDYW7	High blood pressure	BA00	Approved	[15]
Nifurtimox	DMSQLZJ	Chagas disease	IF53	Approved	[61]
Nilotinib	DM7HXWT	Chronic myelogenous leukaemia	2A20.0	Approved	[24]
Nitrofurantoin	DM7PQIK	Urinary tract infection	GC08	Approved	[62]
Norfloxacin	DMIZ6W2	Bacterial infection	1A00-1C4Z	Approved	[63]
Ofloxacin	DM0VQN3	Bacterial infection	1A00-1C4Z	Approved	[15]
Olmesartan medoxomil	DMWBHRY	High blood pressure	BA00	Approved	[32]
Oxaliplatin	DMQNWRD	Colorectal cancer	2B91.Z	Approved	[64]
Paclitaxel	DMLB81S	Breast cancer	2C60-2C65	Approved	[29]
Palbociclib	DMD7L94	Breast cancer	2C60-2C65	Approved	[65]
Pantoprazole	DMSVOCZ	Gastroesophageal reflux disease	DA22.Z	Approved	[66]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[67]
Pemetrexed	DMMX2E6	Malignant pleural mesothelioma	2C26.0	Approved	[68]
Pirarubicin	DMGTW1I	Breast cancer	2C60-2C65	Approved	[41]
Pitavastatin	DMJH792	Hyperlipidemia	5C80.Z	Approved	[28]
Pitavastatin calcium	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[69]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[70]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[71]
Pravastatin	DM6A0X7	Hypercholesterolaemia	5C80.0	Approved	[15]
Prazosin	DMCD9YG	Benign prostatic hyperplasia	GA90	Approved	[72]
Progesterone	DMUY35B	Premature labour	JB00	Approved	[36]
Pyrimethamine	DM5X7VY	Malaria	1F40-1F45	Approved	[73]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[15]
Rabeprazole	DMMZXIW	Bacterial infection	1A00-1C4Z	Approved	[74]
Raltitrexed	DMT9K8G	Rectal adenocarcinoma	2B92	Approved	[75]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[32]
Reserpine	DM6VM38	Hypertension	BA00-BA04	Approved	[15]
Riboflavin	DM8YMWE	Acne vulgaris	ED80	Approved	[76]
Rifampin	DMA8J1G	Tuberculosis	1B10-1B1Z	Approved	[14]
Riluzole	DMECBWN	Amyotrophic lateral sclerosis	8B60.0	Approved	[77]
Riociguat	DMXBLMP	Pulmonary arterial hypertension	BB01.0	Approved	[32]
Rivaroxaban	DMQMBZ1	Deep vein thrombosis	BD71	Approved	[78]
Rosiglitazone	DMILWZR	Type 2 diabetes	5A11	Approved	[79]
Rosuvastatin	DMMIQ7G	Hypercholesterolaemia	5C80.0	Approved	[80]
Saquinavir	DMG814N	Human immunodeficiency virus infection	1C62	Approved	[81]
Simvastatin	DM30SGU	Hypercholesterolaemia	5C80.0	Approved	[71]
Sofosbuvir	DMQI86A	Hepatitis C virus infection	1E51.1	Approved	[32]
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[82]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[83]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[82]
Talazoparib	DM2M3OC	Breast cancer	2C60-2C65	Approved	[84]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[85]
Teniposide	DMLW57T	Acute lymphoblastic leukaemia	2A85	Approved	[15]
Tenofovir	DM1IS6U	Human immunodeficiency virus infection	1C62	Approved	[32]
Teriflunomide	DMQ2FKJ	Hyperlipidaemia	5C80	Approved	[49]
Testosterone	DM7HUNW	Osteoporosis	FB83.0	Approved	[86]
Tetracycline	DMZA017	Bacterial infection	1A00-1C4Z	Approved	[14]
Thioguanine	DM7NKEV	Acute myeloid leukaemia	2A60	Approved	[4]
Topotecan	DMP6G8T	Ovarian cancer	2C73	Approved	[87]
Trimetrexate	DMDEA85	Toxoplasmosis	1F57	Approved	[73]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[88]
Verteporfin	DMIY6DB	Psoriasis vulgaris	EA90	Approved	[89]
Vinblastine	DM5TVS3	Solid tumour/cancer	2A00-2F9Z	Approved	[29]
Vincristine	DMINOX3	Acute lymphoblastic leukaemia	2A85	Approved	[73]
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]

30 Clinical Trial Drug(s) Transported by This DTP

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	[75]
Exatecan	DMCA7FN	Solid tumour/cancer	2A00-2F9Z	Phase 3	[75]
Karenitecin	DMCRGY4	Lung cancer	2C25.0	Phase 3	[75]
Nolatrexed	DMOF0CA	Solid tumour/cancer	2A00-2F9Z	Phase 3	[73]
Resveratrol	DM3RWXL	Giant cell arteritis	4A44.2	Phase 3	[43]
Synthetic hypericin	DMXU4ON	Virus infection	1A24-1D9Z	Phase 3	[92]
Tenofovir alafenamide	DMHOV7D	Hepatitis B virus infection	1E51.0	Phase 3	[93]
Genistein	DM0JETC	Menopause symptom	GA30.0	Phase 2/3	[38]
9-AMINOCAMPTOTHECIN	DMQXYRG	Acquired immune deficiency syndrome	1C62.3	Phase 2	[75]
Bisantrene	DMW76V0	Acute myelogenous leukaemia	2A41	Phase 2	[75]
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	[75]
Flavopiridol	DMKSUOI	Acute myeloid leukaemia	2A60	Phase 2	[96]
Gimatecan	DMSKMET	Breast cancer	2C60-2C65	Phase 2	[75]
HPPH	DM25PQB	Lung cancer	2C25.0	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	Trichuris trichiura infection	1F6G	Phase 2	[100]
PEITC	DMOMN31	Prostate cancer	2C82.0	Phase 2	[26]
Piritrexim	DM276N1	Bladder cancer	2C94	Phase 2	[73]
UCN-01	DMUNJZB	Non-small-cell lung cancer	2C25.Y	Phase 2	[75]
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	Solid tumour/cancer	2A00-2F9Z	Phase 1	[102]
Mycophenolic acid glucuronide	DM5O4X9	lung transplantation	PK80.20	Phase 1	[60]
Sphingosine-1-Phosphate	DMJCQKA	Acne vulgaris	ED80	Phase 1	[103]

7 Discontinued Drug(s) Transported by This DTP

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	[75]
Rhodamine-123	DMQAK6T	Prostate cancer	2C82.0	Discontinued in Phase 1	[108]

9 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Azidothymidine monophosphate	DM3FLMR	Solid tumour/cancer	2A00-2F9Z	Preclinical	[107]
Barasertib-hQPA	DMTJZIL	Solid tumour/cancer	2A00-2F9Z	Preclinical	[109]
BMS 536924	DMDJH2L	Solid tumour/cancer	2A00-2F9Z	Preclinical	[110]
Enrofloxacin	DMK6WIO	Bacterial infection	1A00-1C4Z	Preclinical	[111]
Homocamptothecin	DMBQDA3	Solid tumour/cancer	2A00-2F9Z	Preclinical	[112]
N-desethyl sunitinib	DM5ATJ0	Solid tumour/cancer	2A00-2F9Z	Preclinical	[113]
Pancratistatin	DM3YUGA	Solid tumour/cancer	2A00-2F9Z	Preclinical	[114]
Puromycin	DMDKLB5	Bacterial infection	1A00-1C4Z	Preclinical	[26]
Scutellarin	DMJT1E5	Cerebrovascular ischaemia	8B1Z	Preclinical	[115]

14 Investigative Drug(s) Transported by This DTP

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	Discovery agent	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	[75]
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]

Molecular Expression Atlas (MEA) of This DTP

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Acute myelocytic leukaemia	2B33.1	Bone marrow	1.20E-13	-1.20E+00	-1.06E+00
Adrenocortical carcinoma	2D11.Z	Kidney	9.16E-08	-1.58E+00	-2.25E+00
Alopecia	ED70	Skin from scalp	3.80E-04	2.65E-01	7.35E-01
Alzheimer's disease	8A20	Entorhinal cortex	9.45E-01	-5.34E-02	-9.01E-02
Ankylosing spondylitis	FA92.0	Pheripheral blood	5.41E-01	3.49E-02	3.92E-02
Aortic stenosis	BB70	Calcified aortic valve	8.86E-01	-1.13E-01	-1.68E-01
Apnea	7A40	Hyperplastic tonsil	6.69E-02	-4.44E-01	-1.15E+00
Arthropathy	FA00-FA5Z	Peripheral blood	1.18E-01	1.35E-01	3.22E-01
Asthma	CA23	Nasal and bronchial airway	1.98E-03	-2.85E-01	-5.81E-01
Atopic dermatitis	EA80	Skin	7.93E-01	7.12E-02	1.92E-01
Autism	6A02	Whole blood	2.17E-02	-2.80E-01	-5.98E-01
Autoimmune uveitis	9A96	Peripheral monocyte	2.27E-01	6.81E-02	5.45E-01
Autosomal dominant monocytopenia	4B04	Whole blood	3.09E-01	9.63E-02	4.35E-01
Bacterial infection of gingival	1C1H	Gingival tissue	5.61E-01	1.20E-01	2.41E-01
Batten disease	5C56.1	Whole blood	3.63E-01	-9.17E-02	-7.04E-01
Behcet's disease	4A62	Peripheral blood	6.57E-01	1.19E-01	4.49E-01
Bipolar disorder	6A60-6A6Z	Prefrontal cortex	1.33E-01	-1.08E-01	-2.92E-01
Bladder cancer	2C94	Bladder tissue	4.60E-05	-2.12E+00	-3.70E+00
Breast cancer	2C60-2C6Z	Breast tissue	1.46E-65	-1.41E+00	-1.41E+00
Cardioembolic stroke	8B11.20	Whole blood	8.30E-03	3.32E-01	4.78E-01
Cervical cancer	2C77	Cervical tissue	3.56E-01	-6.63E-02	-8.93E-02
Childhood onset rheumatic disease	FA20.Z	Peripheral blood	3.80E-01	2.72E-02	1.14E-01
Chronic hepatitis C	1E51.1	Whole blood	2.62E-01	-1.53E-02	-9.73E-02
Chronic obstructive pulmonary disease	CA22	Lung tissue	2.23E-01	-2.71E-01	-4.13E-01
Chronic obstructive pulmonary disease	CA22	Small airway epithelium	8.74E-01	6.45E-02	1.09E-01
Chronic rhinosinusitis	CA0A	Sinus mucosa tissue	9.04E-01	1.60E-01	3.29E-01
Colon cancer	2B90	Colon tissue	1.83E-95	-5.61E+00	-4.08E+00
Coronary artery disease	BA80-BA8Z	Peripheral blood	7.25E-01	4.35E-02	1.03E-01
Diffuse large B-cell lymphoma	2A81	Tonsil tissue	3.96E-01	-1.08E-01	-4.64E-01
Endometriosis	GA10	Endometrium tissue	3.20E-01	-2.44E-01	-2.70E-01
Familial hypercholesterolemia	5C80.00	Peripheral blood	5.10E-01	1.12E-01	5.67E-01
Familial hypercholesterolemia	5C80.00	Whole blood	2.28E-08	-3.66E-01	-8.07E-01
Gastric cancer	2B72	Gastric tissue	2.57E-03	1.18E+00	6.01E+00
Glioblastopma	2A00.00	Nervous tissue	7.63E-03	-2.10E-01	-2.66E-01
Glioma	2A00.0Y-2A00.0Z	White matter tissue	9.24E-02	-8.49E-01	-5.22E-01
Head and neck cancer	2D42	Head and neck tissue	1.07E-06	-3.94E-01	-6.94E-01
HIV-associated neurocognitive impairment	8A2Y-8A2Z	White matter tissue	9.04E-01	-5.67E-02	-1.17E-01
Huntington's disease	8A01.10	Whole blood	7.81E-01	-5.28E-03	-4.32E-02
Idiopathic pulmonary fibrosis	CB03.4	Lung tissue	7.08E-02	4.57E-01	7.88E-01
Immunodeficiency	4A00-4A20	Peripheral blood	1.23E-01	9.01E-02	3.32E-01
Influenza	1.00E+30	Whole blood	7.89E-01	2.48E-02	2.72E-01
Interstitial cystitis	GC00.3	Bladder tissue	1.87E-04	-9.47E-01	-4.76E+00
Intracranial aneurysm	8B01.0	Intracranial artery	4.08E-03	1.26E+00	1.95E+00
Irritable bowel syndrome	DD91.0	Rectal colon tissue	6.27E-01	3.30E-02	4.87E-02
Ischemic stroke	8B11	Peripheral blood	3.49E-01	1.41E-01	8.40E-01
Juvenile idiopathic arthritis	FA24	Peripheral blood	9.69E-07	1.39E-01	3.45E-01
Lateral sclerosis	8B60.4	Cervical spinal cord	2.86E-02	-9.76E-01	-8.53E-01
Lateral sclerosis	8B60.4	Skin	1.12E-01	7.91E-02	1.09E+00
Liver cancer	2C12.0	Liver tissue	9.85E-09	-1.57E+00	-1.47E+00
Liver failure	DB99.7-DB99.8	Liver tissue	1.12E-01	-7.55E-01	-1.72E+00
Lung cancer	2C25	Lung tissue	3.87E-47	-1.28E+00	-1.63E+00
Lupus erythematosus	4A40	Whole blood	8.72E-01	-1.28E-01	-2.19E-01
Major depressive disorder	6A70-6A7Z	Whole blood	1.78E-02	2.76E-01	4.58E-01
Major depressive disorder	6A70-6A7Z	Hippocampus	3.72E-02	-1.56E-01	-4.33E-01
Melanoma	2C30	Skin	2.23E-01	-1.00E-01	-1.30E-01
Multiple myeloma	2A83.1	Bone marrow	3.08E-02	-4.06E-01	-8.83E-01
Multiple myeloma	2A83.1	Peripheral blood	7.10E-01	5.87E-03	1.61E-02
Multiple sclerosis	8A40	Plasmacytoid dendritic cells	9.93E-01	-1.09E-01	-5.77E-01
Myelodysplastic syndrome	2A36-2A3Z	Bone marrow	3.18E-03	-3.40E-01	-9.58E-01
Myelofibrosis	2A20.2	Whole blood	8.22E-03	1.38E+00	4.26E+00
Myocardial infarction	BA41-BA50	Peripheral blood	7.72E-01	-8.41E-02	-1.02E-01
Myopathy	8C70.6	Muscle tissue	3.75E-04	4.90E-01	2.14E+00
Neonatal sepsis	KA60	Whole blood	1.57E-03	4.02E-02	6.01E-02
Neuroectodermal tumour	2A00.11	Brain stem tissue	1.01E-01	-2.88E-01	-6.33E-01
Non-alcoholic fatty liver disease	DB92	Liver tissue	7.81E-01	-2.27E-01	-3.64E-01
Obesity related type 2 diabetes	5A11	Omental adipose tissue	2.83E-01	2.41E-01	7.57E-01
Olive pollen allergy	CA08.00	Peripheral blood	1.17E-01	7.74E-01	1.26E+00
Oral cancer	2B6E	Oral tissue	1.32E-01	3.44E-01	4.51E-01
Osteoarthritis	FA00-FA0Z	Synovial tissue	6.74E-01	3.97E-02	5.80E-02
Osteoporosis	FB83.1	Bone marrow	4.09E-01	1.59E-01	8.09E-02
Ovarian cancer	2C73	Ovarian tissue	1.76E-03	-1.19E+00	-1.71E+00
Pancreatic cancer	2C10	Pancreas	8.05E-01	-5.92E-02	-8.17E-02
Parkinson's disease	8A00.0	Substantia nigra tissue	9.26E-01	-9.37E-02	-1.15E-01
Pediatric respiratory syncytial virus infection	CA40.11	Peripheral blood	1.93E-03	2.91E-01	2.28E+00
Pituitary cancer	2D12	Pituitary tissue	7.04E-03	-1.33E+00	-1.69E+00
Pituitary gonadotrope tumour	2D12	Pituitary tissue	3.60E-02	-1.07E+00	-1.14E+00
Polycystic ovary syndrome	5A80.1	Vastus lateralis muscle	8.25E-01	-4.10E-02	-3.44E-01
Polycythemia vera	2A20.4	Whole blood	6.04E-15	5.83E-01	1.90E+00
Pompe disease	5C51.3	Biceps muscle	9.32E-01	-4.76E-02	-1.05E-01
Preterm birth	KA21.4Z	Myometrium	1.56E-01	5.36E-01	8.59E-01
Prostate cancer	2C82	Prostate	7.49E-01	5.58E-01	4.90E-01
Psoriasis	EA90	Skin	6.07E-04	1.66E-01	4.54E-01
Rectal cancer	2B92	Rectal colon tissue	3.39E-04	-4.15E+00	-3.65E+00
Renal cancer	2C90-2C91	Kidney	2.10E-01	3.71E-01	7.59E-01
Retinoblastoma	2D02.2	Uvea	1.43E-02	-3.15E-01	-6.12E-01
Rheumatoid arthritis	FA20	Synovial tissue	4.63E-01	-1.31E-01	-2.30E-01
Rhinovirus infection	CA42.1	Nasal epithelium tissue	3.09E-01	-1.41E-02	-1.00E-01
Schizophrenia	6A20	Prefrontal cortex	7.71E-03	-9.31E-01	-5.46E-01
Schizophrenia	6A20	Superior temporal cortex	5.82E-02	-3.72E-01	-7.51E-01
Scleroderma	4A42.Z	Whole blood	9.37E-01	9.35E-02	1.33E-01
Seizure	8A60-8A6Z	Whole blood	9.20E-02	-2.90E-01	-2.32E-01
Sensitive skin	EK0Z	Skin	8.12E-01	-1.51E-01	-5.67E-01
Sepsis with septic shock	1G41	Whole blood	2.13E-15	4.37E-02	9.56E-02
Shwachman-Diamond syndrome	3A70.0	Bone marrow	1.93E-02	7.63E-01	1.07E+00
Sickle cell disease	3A51.0-3A51.3	Peripheral blood	3.15E-02	2.04E-01	7.07E-01
Simpson golabi behmel syndrome	LD2C	Adipose tissue	2.79E-01	-2.47E-02	-1.94E-01
Sjogren's syndrome	4A43.2	Salivary gland tissue	5.47E-01	8.34E-02	4.15E-01
Skin cancer	2C30-2C3Z	Skin	5.18E-17	3.16E-01	7.14E-01
Thrombocythemia	3B63	Whole blood	7.74E-03	2.60E-01	8.17E-01
Thrombocytopenia	3B64	Whole blood	3.02E-01	-3.34E-02	-6.08E-02
Thyroid cancer	2D10	Thyroid	5.25E-11	6.24E-01	9.23E-01
Tibial muscular dystrophy	8C75	Muscle tissue	1.91E-02	2.50E-01	1.01E+00
Tuberous sclerosis complex	LD2D.2	Perituberal tissue	6.64E-01	-5.89E-01	-7.99E-01
Type 2 diabetes	5A11	Liver tissue	1.85E-01	-1.34E-01	-4.20E-01
Ureter cancer	2C92	Urothelium	6.15E-01	-1.07E-01	-6.10E-01
Uterine cancer	2C78	Endometrium tissue	3.03E-24	-1.50E+00	-1.59E+00
Vitiligo	ED63.0	Skin	1.37E-01	-1.98E-01	-7.61E-01

Drug Affinity of This DTP Assessed by Cell Line

Approved Drug(s)

Drug Name	Highest Status	Cell Line	Affinity	REF
Daunorubicin	Approved	Spodoptera frugiperda (Sf9) cells-BCRP	Km = 2.5 microM	[25]
Doxorubicin	Approved	Spodoptera frugiperda (Sf9) cells-BCRP	Km = 5 microM	[25]
Methotrexate	Approved	Breast carcinoma cell line (MCF7)-BCRP	Km = 681 microM	[59]
Methotrexate	Approved	Human embryonic kidney cells (HEK293)-BCRP	Km = 1340 microM	[123]
Methotrexate	Approved	Human embryonic kidney cells (HEK293)-BCRP	Km = 1410 microM	[124]
Mitoxantrone	Approved	Spodoptera frugiperda (Sf9) cells-BCRP	Km = 7 microM	[25]
Pitavastatin calcium	Approved	Human embryonic kidney cells (HEK293)-BCRP	Km = 5.73 microM	[69]
Rosuvastatin	Approved	Human embryonic kidney cells (HEK293)-BCRP	Km = 2.02 microM	[80]
Rosuvastatin	Approved	Madin-Darby canine kidney cells (MDCKII)-BCRP	Km = 10.1 microM	[125]
Sulfasalazine	Approved	Spodoptera frugiperda (Sf9) cells-BCRP	Km = 0.7 microM	[126]
Topotecan	Approved	Madin-Darby canine kidney cells (MDCKII)-BCRP	Km = 213 microM	[94]

Clinical Trial Drug(s)

Drug Name	Highest Status	Cell Line	Affinity	REF
LE-SN38	Phase 2	Human lung carcinoma cells (PC-6/SN2-5H)-BCRP	Km = 4 microM	[98]

Investigative Drug(s)

Drug Name	Highest Status	Cell Line	Affinity	REF
[3H]estradiol-17beta-glucuronide	Investigative	Human embryonic kidney cells (HEK293)-BCRP	Km = 44.2 microM	[123]

The Drug Therapeutic Target (DTT) Role of This DTP

• DTP DTT Name: ATP-binding cassette transporter G2 (ABCG2) DTT Info
• DTP DTT Type: Successful
• Related Disease:
  Irritable bowel syndrome [ICD-11: DD91]
  Rheumatoid arthritis [ICD-11: FA20]

1 Approved Drug(s) Targeting This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[1]

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