Broad substrate specificity ATP-binding cassette transporter ABCG2

Details

Name
Broad substrate specificity ATP-binding cassette transporter ABCG2
Kind
protein
Synonyms
  • 7.6.2.2
  • ABCP
  • ATP-binding cassette sub-family G member 2
  • BCRP
  • BCRP1
  • Breast cancer resistance protein
  • CDw338
  • Mitoxantrone resistance-associated protein
  • MXR
  • Placenta-specific ATP-binding cassette transporter
  • Urate exporter
Gene Name
ABCG2
UniProtKB Entry
Q9UNQ0Swiss-Prot
Organism
Humans
NCBI Taxonomy ID
9606
Amino acid sequence
>lcl|BSEQ0002125|Broad substrate specificity ATP-binding cassette transporter ABCG2
MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
Number of residues
655
Molecular Weight
72313.47
Theoretical pI
8.9
GO Classification
Functions
ATP binding / protein homodimerization activity
Processes
transmembrane transport / urate metabolic process
Components
mitochondrial membrane / plasma membrane
General Function
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells (PubMed:11306452, PubMed:12958161, PubMed:19506252, PubMed:20705604, PubMed:28554189, PubMed:30405239, PubMed:31003562). Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme (PubMed:20705604, PubMed:23189181). Also mediates the efflux of sphingosine-1-P from cells (PubMed:20110355). Acts as a urate exporter functioning in both renal and extrarenal urate excretion (PubMed:19506252, PubMed:20368174, PubMed:22132962, PubMed:31003562, PubMed:36749388). In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates (PubMed:12682043, PubMed:28554189, PubMed:30405239). Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux (PubMed:11306452, PubMed:12477054, PubMed:15670731, PubMed:18056989, PubMed:31254042). In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity)
Specific Function
Abc-type xenobiotic transporter activity
Pfam Domain Function
Signal Regions
Not Available
Transmembrane Regions
396-416 429-449 478-498 507-527 536-556 631-651
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0016303|ATP-binding cassette sub-family G member 2 (ABCG2)
ATGTCTTCCAGTAATGTCGAAGTTTTTATCCCAGTGTCACAAGGAAACACCAATGGCTTC
CCCGCGACAGCTTCCAATGACCTGAAGGCATTTACTGAAGGAGCTGTGTTAAGTTTTCAT
AACATCTGCTATCGAGTAAAACTGAAGAGTGGCTTTCTACCTTGTCGAAAACCAGTTGAG
AAAGAAATATTATCGAATATCAATGGGATCATGAAACCTGGTCTCAACGCCATCCTGGGA
CCCACAGGTGGAGGCAAATCTTCGTTATTAGATGTCTTAGCTGCAAGGAAAGATCCAAGT
GGATTATCTGGAGATGTTCTGATAAATGGAGCACCGCGACCTGCCAATTTCAAATGTAAT
TCAGGTTACGTGGTACAAGATGATGTTGTGATGGGCACTCTGACGGTGAGAGAAAACTTA
CAGTTCTCAGCAGCTCTTCGGCTTGCAACAACTATGACGAATCATGAAAAAAACGAACGG
ATTAACAGGGTCATTCAAGAGTTAGGTCTGGATAAAGTGGCAGACTCCAAGGTTGGAACT
CAGTTTATCCGTGGTGTGTCTGGAGGAGAAAGAAAAAGGACTAGTATAGGAATGGAGCTT
ATCACTGATCCTTCCATCTTGTTCTTGGATGAGCCTACAACTGGCTTAGACTCAAGCACA
GCAAATGCTGTCCTTTTGCTCCTGAAAAGGATGTCTAAGCAGGGACGAACAATCATCTTC
TCCATTCATCAGCCTCGATATTCCATCTTCAAGTTGTTTGATAGCCTCACCTTATTGGCC
TCAGGAAGACTTATGTTCCACGGGCCTGCTCAGGAGGCCTTGGGATACTTTGAATCAGCT
GGTTATCACTGTGAGGCCTATAATAACCCTGCAGACTTCTTCTTGGACATCATTAATGGA
GATTCCACTGCTGTGGCATTAAACAGAGAAGAAGACTTTAAAGCCACAGAGATCATAGAG
CCTTCCAAGCAGGATAAGCCACTCATAGAAAAATTAGCGGAGATTTATGTCAACTCCTCC
TTCTACAAAGAGACAAAAGCTGAATTACATCAACTTTCCGGGGGTGAGAAGAAGAAGAAG
ATCACAGTCTTCAAGGAGATCAGCTACACCACCTCCTTCTGTCATCAACTCAGATGGGTT
TCCAAGCGTTCATTCAAAAACTTGCTGGGTAATCCCCAGGCCTCTATAGCTCAGATCATT
GTCACAGTCGTACTGGGACTGGTTATAGGTGCCATTTACTTTGGGCTAAAAAATGATTCT
ACTGGAATCCAGAACAGAGCTGGGGTTCTCTTCTTCCTGACGACCAACCAGTGTTTCAGC
AGTGTTTCAGCCGTGGAACTCTTTGTGGTAGAGAAGAAGCTCTTCATACATGAATACATC
AGCGGATACTACAGAGTGTCATCTTATTTCCTTGGAAAACTGTTATCTGATTTATTACCC
ATGAGGATGTTACCAAGTATTATATTTACCTGTATAGTGTACTTCATGTTAGGATTGAAG
CCAAAGGCAGATGCCTTCTTCGTTATGATGTTTACCCTTATGATGGTGGCTTATTCAGCC
AGTTCCATGGCACTGGCCATAGCAGCAGGTCAGAGTGTGGTTTCTGTAGCAACACTTCTC
ATGACCATCTGTTTTGTGTTTATGATGGTCTGTTGGTCAATCTCACAACCATTGCATCTT
GGCTGTCATGGCTTCAGTACTTCAGCATTCCACGATATGGATTTACGGCTTTGCAGCATA
ATGAATTTTTGGGACAAAACTTCTGCCCAGGACTCAATGCAACAGGAAACAATCCTTGTA
ACTATGCAACATGTACTGGCGAAGAATATTTGGTAA
Chromosome Location
4
Locus
4q22.1
External Identifiers
ResourceLink
UniProtKB IDQ9UNQ0
UniProtKB Entry NameABCG2_HUMAN
GenBank Protein ID4185796
GenBank Gene IDAF103796
GeneCard IDABCG2
GenAtlas IDABCG2
HGNC IDHGNC:74
PDB ID(s)5NJ3, 5NJG, 6ETI, 6FEQ, 6FFC, 6HBU, 6HCO, 6HIJ, 6HZM, 6VXF, 6VXH, 6VXI, 6VXJ, 7NEQ, 7NEZ, 7NFD, 7OJ8, 7OJH, 7OJI, 8BHT, 8BI0, 8P7W, 8P8A, 8P8J, 8U2C
KEGG IDhsa:9429
IUPHAR/Guide To Pharmacology ID792
NCBI Gene ID9429
General References
  1. Allikmets R, Schriml LM, Hutchinson A, Romano-Spica V, Dean M: A human placenta-specific ATP-binding cassette gene (ABCP) on chromosome 4q22 that is involved in multidrug resistance. Cancer Res. 1998 Dec 1;58(23):5337-9. [Article]
  2. Doyle LA, Yang W, Abruzzo LV, Krogmann T, Gao Y, Rishi AK, Ross DD: A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci U S A. 1998 Dec 22;95(26):15665-70. [Article]
  3. Komatani H, Kotani H, Hara Y, Nakagawa R, Matsumoto M, Arakawa H, Nishimura S: Identification of breast cancer resistant protein/mitoxantrone resistance/placenta-specific, ATP-binding cassette transporter as a transporter of NB-506 and J-107088, topoisomerase I inhibitors with an indolocarbazole structure. Cancer Res. 2001 Apr 1;61(7):2827-32. [Article]
  4. Zhou S, Schuetz JD, Bunting KD, Colapietro AM, Sampath J, Morris JJ, Lagutina I, Grosveld GC, Osawa M, Nakauchi H, Sorrentino BP: The ABC transporter Bcrp1/ABCG2 is expressed in a wide variety of stem cells and is a molecular determinant of the side-population phenotype. Nat Med. 2001 Sep;7(9):1028-34. [Article]
  5. Zhang W, Mojsilovic-Petrovic J, Andrade MF, Zhang H, Ball M, Stanimirovic DB: The expression and functional characterization of ABCG2 in brain endothelial cells and vessels. FASEB J. 2003 Nov;17(14):2085-7. Epub 2003 Sep 4. [Article]
  6. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [Article]
  7. Hillier LW, Graves TA, Fulton RS, Fulton LA, Pepin KH, Minx P, Wagner-McPherson C, Layman D, Wylie K, Sekhon M, Becker MC, Fewell GA, Delehaunty KD, Miner TL, Nash WE, Kremitzki C, Oddy L, Du H, Sun H, Bradshaw-Cordum H, Ali J, Carter J, Cordes M, Harris A, Isak A, van Brunt A, Nguyen C, Du F, Courtney L, Kalicki J, Ozersky P, Abbott S, Armstrong J, Belter EA, Caruso L, Cedroni M, Cotton M, Davidson T, Desai A, Elliott G, Erb T, Fronick C, Gaige T, Haakenson W, Haglund K, Holmes A, Harkins R, Kim K, Kruchowski SS, Strong CM, Grewal N, Goyea E, Hou S, Levy A, Martinka S, Mead K, McLellan MD, Meyer R, Randall-Maher J, Tomlinson C, Dauphin-Kohlberg S, Kozlowicz-Reilly A, Shah N, Swearengen-Shahid S, Snider J, Strong JT, Thompson J, Yoakum M, Leonard S, Pearman C, Trani L, Radionenko M, Waligorski JE, Wang C, Rock SM, Tin-Wollam AM, Maupin R, Latreille P, Wendl MC, Yang SP, Pohl C, Wallis JW, Spieth J, Bieri TA, Berkowicz N, Nelson JO, Osborne J, Ding L, Meyer R, Sabo A, Shotland Y, Sinha P, Wohldmann PE, Cook LL, Hickenbotham MT, Eldred J, Williams D, Jones TA, She X, Ciccarelli FD, Izaurralde E, Taylor J, Schmutz J, Myers RM, Cox DR, Huang X, McPherson JD, Mardis ER, Clifton SW, Warren WC, Chinwalla AT, Eddy SR, Marra MA, Ovcharenko I, Furey TS, Miller W, Eichler EE, Bork P, Suyama M, Torrents D, Waterston RH, Wilson RK: Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature. 2005 Apr 7;434(7034):724-31. [Article]
  8. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  9. Miyake K, Mickley L, Litman T, Zhan Z, Robey R, Cristensen B, Brangi M, Greenberger L, Dean M, Fojo T, Bates SE: Molecular cloning of cDNAs which are highly overexpressed in mitoxantrone-resistant cells: demonstration of homology to ABC transport genes. Cancer Res. 1999 Jan 1;59(1):8-13. [Article]
  10. Schmitz G, Langmann T, Heimerl S: Role of ABCG1 and other ABCG family members in lipid metabolism. J Lipid Res. 2001 Oct;42(10):1513-20. [Article]
  11. Xu J, Liu Y, Yang Y, Bates S, Zhang JT: Characterization of oligomeric human half-ABC transporter ATP-binding cassette G2. J Biol Chem. 2004 May 7;279(19):19781-9. Epub 2004 Mar 4. [Article]
  12. Diop NK, Hrycyna CA: N-Linked glycosylation of the human ABC transporter ABCG2 on asparagine 596 is not essential for expression, transport activity, or trafficking to the plasma membrane. Biochemistry. 2005 Apr 12;44(14):5420-9. [Article]
  13. Ozvegy-Laczka C, Koblos G, Sarkadi B, Varadi A: Single amino acid (482) variants of the ABCG2 multidrug transporter: major differences in transport capacity and substrate recognition. Biochim Biophys Acta. 2005 Feb 1;1668(1):53-63. [Article]
  14. Henriksen U, Gether U, Litman T: Effect of Walker A mutation (K86M) on oligomerization and surface targeting of the multidrug resistance transporter ABCG2. J Cell Sci. 2005 Apr 1;118(Pt 7):1417-26. Epub 2005 Mar 15. [Article]
  15. Wakabayashi K, Nakagawa H, Tamura A, Koshiba S, Hoshijima K, Komada M, Ishikawa T: Intramolecular disulfide bond is a critical check point determining degradative fates of ATP-binding cassette (ABC) transporter ABCG2 protein. J Biol Chem. 2007 Sep 21;282(38):27841-6. Epub 2007 Aug 8. [Article]
  16. Dehghan A, Kottgen A, Yang Q, Hwang SJ, Kao WL, Rivadeneira F, Boerwinkle E, Levy D, Hofman A, Astor BC, Benjamin EJ, van Duijn CM, Witteman JC, Coresh J, Fox CS: Association of three genetic loci with uric acid concentration and risk of gout: a genome-wide association study. Lancet. 2008 Dec 6;372(9654):1953-61. doi: 10.1016/S0140-6736(08)61343-4. Epub 2008 Oct 1. [Article]
  17. Woodward OM, Kottgen A, Coresh J, Boerwinkle E, Guggino WB, Kottgen M: Identification of a urate transporter, ABCG2, with a common functional polymorphism causing gout. Proc Natl Acad Sci U S A. 2009 Jun 23;106(25):10338-42. doi: 10.1073/pnas.0901249106. Epub 2009 Jun 8. [Article]
  18. Matsuo H, Takada T, Ichida K, Nakamura T, Nakayama A, Ikebuchi Y, Ito K, Kusanagi Y, Chiba T, Tadokoro S, Takada Y, Oikawa Y, Inoue H, Suzuki K, Okada R, Nishiyama J, Domoto H, Watanabe S, Fujita M, Morimoto Y, Naito M, Nishio K, Hishida A, Wakai K, Asai Y, Niwa K, Kamakura K, Nonoyama S, Sakurai Y, Hosoya T, Kanai Y, Suzuki H, Hamajima N, Shinomiya N: Common defects of ABCG2, a high-capacity urate exporter, cause gout: a function-based genetic analysis in a Japanese population. Sci Transl Med. 2009 Nov 4;1(5):5ra11. doi: 10.1126/scitranslmed.3000237. [Article]
  19. Desuzinges-Mandon E, Arnaud O, Martinez L, Huche F, Di Pietro A, Falson P: ABCG2 transports and transfers heme to albumin through its large extracellular loop. J Biol Chem. 2010 Oct 22;285(43):33123-33. doi: 10.1074/jbc.M110.139170. Epub 2010 Aug 12. [Article]
  20. Nakayama A, Matsuo H, Takada T, Ichida K, Nakamura T, Ikebuchi Y, Ito K, Hosoya T, Kanai Y, Suzuki H, Shinomiya N: ABCG2 is a high-capacity urate transporter and its genetic impairment increases serum uric acid levels in humans. Nucleosides Nucleotides Nucleic Acids. 2011 Dec;30(12):1091-7. doi: 10.1080/15257770.2011.633953. [Article]
  21. Mo W, Zhang JT: Human ABCG2: structure, function, and its role in multidrug resistance. Int J Biochem Mol Biol. 2012;3(1):1-27. Epub 2011 Mar 30. [Article]
  22. Zelinski T, Coghlan G, Liu XQ, Reid ME: ABCG2 null alleles define the Jr(a-) blood group phenotype. Nat Genet. 2012 Jan 15;44(2):131-2. doi: 10.1038/ng.1075. [Article]
  23. Saison C, Helias V, Ballif BA, Peyrard T, Puy H, Miyazaki T, Perrot S, Vayssier-Taussat M, Waldner M, Le Pennec PY, Cartron JP, Arnaud L: Null alleles of ABCG2 encoding the breast cancer resistance protein define the new blood group system Junior. Nat Genet. 2012 Jan 15;44(2):174-7. doi: 10.1038/ng.1070. [Article]
  24. Kobuchi H, Moriya K, Ogino T, Fujita H, Inoue K, Shuin T, Yasuda T, Utsumi K, Utsumi T: Mitochondrial localization of ABC transporter ABCG2 and its function in 5-aminolevulinic acid-mediated protoporphyrin IX accumulation. PLoS One. 2012;7(11):e50082. doi: 10.1371/journal.pone.0050082. Epub 2012 Nov 26. [Article]
  25. Iida A, Saito S, Sekine A, Mishima C, Kitamura Y, Kondo K, Harigae S, Osawa S, Nakamura Y: Catalog of 605 single-nucleotide polymorphisms (SNPs) among 13 genes encoding human ATP-binding cassette transporters: ABCA4, ABCA7, ABCA8, ABCD1, ABCD3, ABCD4, ABCE1, ABCF1, ABCG1, ABCG2, ABCG4, ABCG5, and ABCG8. J Hum Genet. 2002;47(6):285-310. [Article]
  26. Itoda M, Saito Y, Shirao K, Minami H, Ohtsu A, Yoshida T, Saijo N, Suzuki H, Sugiyama Y, Ozawa S, Sawada J: Eight novel single nucleotide polymorphisms in ABCG2/BCRP in Japanese cancer patients administered irinotacan. Drug Metab Pharmacokinet. 2003;18(3):212-7. [Article]
  27. Zamber CP, Lamba JK, Yasuda K, Farnum J, Thummel K, Schuetz JD, Schuetz EG: Natural allelic variants of breast cancer resistance protein (BCRP) and their relationship to BCRP expression in human intestine. Pharmacogenetics. 2003 Jan;13(1):19-28. [Article]
  28. Morisaki K, Robey RW, Ozvegy-Laczka C, Honjo Y, Polgar O, Steadman K, Sarkadi B, Bates SE: Single nucleotide polymorphisms modify the transporter activity of ABCG2. Cancer Chemother Pharmacol. 2005 Aug;56(2):161-72. Epub 2005 Apr 19. [Article]
  29. Maekawa K, Itoda M, Sai K, Saito Y, Kaniwa N, Shirao K, Hamaguchi T, Kunitoh H, Yamamoto N, Tamura T, Minami H, Kubota K, Ohtsu A, Yoshida T, Saijo N, Kamatani N, Ozawa S, Sawada J: Genetic variation and haplotype structure of the ABC transporter gene ABCG2 in a Japanese population. Drug Metab Pharmacokinet. 2006 Apr;21(2):109-21. [Article]

Associated Data

Drug Relations
DrugDrug groupPharmacological action?TypeActionsDetails
BiricodarinvestigationalunknowntargetDetails
Gefitinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Quercetinexperimental, investigationalunknowntransporterinhibitorDetails
NaringeninexperimentalunknowntransporterinhibitorDetails
Topotecanapproved, investigationalunknowntransportersubstrateDetails
Novobiocinapproved, investigational, vet_approved, withdrawnunknowntransporterinhibitorDetails
EstroneapprovedunknowntransporterinhibitorDetails
Saquinavirapproved, investigationalunknowntransporterinhibitorDetails
Omeprazoleapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
HesperetinexperimentalunknowntransporterinhibitorDetails
GenisteininvestigationalunknowntransporterinhibitorDetails
NelfinavirapprovednotransporterinhibitorDetails
GlyburideapprovedunknowntransportersubstrateDetails
Diethylstilbestrolapproved, investigational, withdrawnunknowntransporterinhibitorDetails
Ritonavirapproved, investigationalunknowntransporterinhibitorDetails
PravastatinapprovednotransportersubstrateDetails
Doxorubicinapproved, investigationalunknowntransportersubstrateDetails
PantoprazoleapprovedunknowntransportersubstrateinhibitorDetails
Cyclosporineapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Taurocholic acidapproved, experimentalunknowntransporterinhibitorDetails
ImatinibapprovednotransportersubstrateinhibitorDetails
Estradiolapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Mitoxantroneapproved, investigationalunknowntransportersubstrateDetails
DaidzinexperimentalunknowntransporterinhibitorDetails
Sorafenibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Sunitinibapproved, investigationalunknowntransporterinhibitorDetails
Dronabinolapproved, illicitnotransporterinhibitorDetails
Buprenorphineapproved, illicit, investigational, vet_approvedunknowntransporterinhibitorDetails
SulfasalazineapprovednotransportersubstrateinhibitorDetails
Telmisartanapproved, investigationalunknowntransporterinhibitorDetails
Dexamethasoneapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Dasatinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
PrazosinapprovedunknowntransportersubstrateDetails
Lansoprazoleapproved, investigationalunknowntransporterinhibitorDetails
Rabeprazoleapproved, investigationalunknowntransporterinhibitorDetails
ElacridarinvestigationalunknowntransporterinhibitorDetails
Nilotinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Erlotinibapproved, investigationalunknowntransporterinhibitorDetails
VandetanibapprovedunknowntransporterinhibitorDetails
Lamivudineapproved, investigationalunknowntransportersubstrateDetails
Irinotecanapproved, investigationalunknowntransportersubstrateDetails
EtoposideapprovedunknowntransportersubstrateDetails
Dactinomycinapproved, investigationalunknowntransportersubstrateDetails
Conjugated estrogensapprovedunknowntransportersubstrateDetails
Cerivastatinapproved, withdrawnunknowntransportersubstrateDetails
Testosteroneapproved, investigationalunknowntransportersubstrateDetails
TamoxifenapprovedunknowntransportersubstrateDetails
Sumatriptanapproved, investigationalunknowntransportersubstrateDetails
DaunorubicinapprovedunknowntransportersubstrateDetails
Cholesterolapproved, investigationalunknowntransporterinducerDetails
MethotrexateapprovedunknowntransportersubstrateDetails
Folic acidapproved, nutraceutical, vet_approvedunknowntransportersubstrateDetails
Alvocidibexperimental, investigationalunknowntransportersubstrateDetails
Vincristineapproved, investigationalunknowntransportersubstrateDetails
TeniposideapprovedunknowntransportersubstrateDetails
Nitrofurantoinapproved, vet_approvedunknowntransportersubstrateDetails
Ivermectinapproved, investigational, vet_approvedunknowntransportersubstrateDetails
CamptothecinexperimentalunknowntransportersubstrateDetails
Riluzoleapproved, investigationalunknowntransportersubstrateDetails
Cladribineapproved, investigationalunknowntransportersubstrateDetails
Clofarabineapproved, investigationalunknowntransportersubstrateDetails
Oxaliplatinapproved, investigationalnotransportersubstrateDetails
CabazitaxelapprovedunknowntransporterinhibitorDetails
PitavastatinapprovedunknowntransportersubstrateDetails
PazopanibapprovedunknowntransportersubstrateDetails
RilpivirineapprovedunknowntransporterinhibitorDetails
TeriflunomideapprovedunknowntransportersubstrateinhibitorDetails
Leflunomideapproved, investigationalunknowntransportersubstrateDetails
VemurafenibapprovedunknowntransportersubstrateinhibitorDetails
ApixabanapprovedunknowntransportersubstrateDetails
Vismodegibapproved, investigationalunknowntransporterinhibitorDetails
RegorafenibapprovedunknowntransporterinhibitorDetails
Ponatinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
EzetimibeapprovedunknowntransportersubstrateDetails
Dabrafenibapproved, investigationalnotransportersubstrateinhibitorDetails
Zafirlukastapproved, investigationalunknowntransporterantagonistDetails
VenlafaxineapprovedunknowntransporterinducerDetails
ZidovudineapprovedunknowntransportersubstrateDetails
AfatinibapprovedunknowntransportersubstrateinhibitorDetails
FluorouracilapprovedunknowntransportersubstrateDetails
Mycophenolate mofetilapproved, investigationalunknowntransportersubstrateDetails
CisplatinapprovedunknowntransportersubstrateDetails
CarboplatinapprovedunknowntransportersubstrateDetails
RosuvastatinapprovedunknowntransportersubstrateDetails
Docetaxelapproved, investigationalunknowntransportersubstrateDetails
SofosbuvirapprovednotransportersubstrateDetails
Lenvatinibapproved, investigationalnotransportersubstrateDetails
IdelalisibapprovednotransportersubstrateDetails
CobicistatapprovedunknowntransporterinhibitorDetails
Rolapitantapproved, investigationalnotransporterinhibitorDetails
Daclatasvirapproved, investigationalunknowntransporterinhibitorDetails
Cobimetinibapproved, investigationalnotransporterweak inhibitorDetails
OsimertinibapprovednotransportersubstrateDetails
Alectinibapproved, investigationalnotransporterinhibitorDetails
RiociguatapprovednotransportersubstrateDetails
DasabuvirapprovedunknowntransporterinhibitorDetails
Safinamideapproved, investigationalunknowntransporterinhibitorDetails
Velpatasvirapproved, investigationalnotransportersubstrateinhibitorDetails
SimeprevirapprovedunknowntransportersubstrateinhibitorDetails
LedipasvirapprovednotransportertransporterDetails
Ombitasvirapproved, investigationalnotransportersubstrateDetails
Delafloxacinapproved, investigationalnotransportersubstrateDetails
TopiroxostatexperimentalunknowntransporterinhibitorDetails
Voxilaprevirapproved, investigationalnotransportersubstrateinhibitorDetails
Enasidenibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Pibrentasvirapproved, investigationalunknowntransportersubstrateinhibitorDetails
Glecaprevirapproved, investigationalunknowntransportersubstrateinhibitorDetails
Copanlisibapproved, investigationalunknowntransportersubstrateDetails
Abemaciclibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Letermovirapproved, investigationalnotransporterinhibitorDetails
Brigatinibapproved, investigationalnotransportersubstrateinhibitorDetails
DolutegravirapprovednotransportersubstrateDetails
Rucaparibapproved, investigationalnotransportersubstrateinhibitorDetails
Baricitinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Cannabidiolapproved, investigationalunknowntransporterinhibitorDetails
Ertugliflozinapproved, investigationalunknowntransportersubstrateDetails
Testosterone cypionateapprovedunknowntransportersubstrateDetails
Testosterone enanthateapprovedunknowntransportersubstrateDetails
Testosterone undecanoateapproved, investigationalunknowntransportersubstrateDetails
Estradiol acetateapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Estradiol benzoateapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Estradiol cypionateapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Estradiol dienanthateapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Estradiol valerateapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Apalutamideapproved, investigationalunknowntransporterinducerDetails
Isavuconazoleapproved, investigationalunknowntransporterinhibitorDetails
NabiximolsinvestigationalunknowntransporterinhibitorDetails
Medical Cannabisexperimental, investigationalunknowntransporterinhibitorDetails
Fostamatinibapproved, investigationalnotransporterinhibitorDetails
Paritaprevirapproved, investigationalunknowntransporterinhibitorDetails
Hydrocortisone aceponateexperimental, vet_approvedunknowntransporterDetails
Hydrocortisone acetateapproved, vet_approvedunknowntransporterDetails
Hydrocortisone butyrateapproved, vet_approvedunknowntransporterDetails
Hydrocortisone cypionateapproved, investigational, vet_approvedunknowntransporterDetails
Hydrocortisone phosphateapproved, vet_approvedunknowntransporterDetails
Hydrocortisone probutateapproved, vet_approvedunknowntransporterDetails
Hydrocortisone valerateapproved, vet_approvedunknowntransporterDetails
DovitinibinvestigationalunknowntransporterinhibitorinducerDetails
Lusutrombopagapproved, investigationalunknowntransportersubstrateDetails
EltrombopagapprovedunknowntransporterinhibitorDetails
Progesteroneapproved, vet_approvedunknowntransporterinhibitorinducerDetails
Fusidic acidapproved, investigationalunknowntransporterinhibitorDetails
Duvelisibapproved, investigationalnotransportersubstrateDetails
Talazoparibapproved, investigationalunknowntransportersubstrateDetails
Dacomitinibapproved, investigationalnotransportersubstrateinhibitorDetails
Venetoclaxapproved, investigationalunknowntransporterinhibitorDetails
Revefenacinapproved, investigationalnotransportersubstrateDetails
Gilteritinibapproved, investigationalnotransporterinhibitorDetails
RivaroxabanapprovedunknowntransportersubstrateDetails
FimasartaninvestigationalunknowntransportersubstrateDetails
Glasdegibapproved, investigationalnotransportersubstrateinhibitorDetails
OlaparibapprovednotransporterinhibitorDetails
AllopurinolapprovedunknowntransportersubstrateDetails
Palbociclibapproved, investigationalnotransportersubstrateinhibitorDetails
CanagliflozinapprovedunknowntransporterDetails
Tegaserodapproved, investigational, withdrawnunknowntransportersubstrateDetails
Tenofovir alafenamideapprovednotransportersubstrateDetails
Raloxifeneapproved, investigationalunknowntransportersubstrateDetails
Alpelisibapproved, investigationalunknowntransportersubstrateDetails
Beclomethasone dipropionateapproved, investigationalunknowntransporterinhibitorDetails
Celecoxibapproved, investigationalunknowntransportersubstrateDetails
DonepezilapprovedunknowntransportersubstrateDetails
Fedratinibapproved, investigationalunknowntransporterinhibitorDetails
Istradefyllineapproved, investigationalunknowntransporterinhibitorDetails
NintedanibapprovedunknowntransporterDetails
CaffeineapprovedunknowntransporterinhibitorDetails
Lasmiditanapproved, investigationalunknowntransporterinhibitorDetails
Trastuzumab deruxtecanapproved, investigationalunknowntransportersubstrateDetails
Darolutamideapproved, investigationalunknowntransportersubstrateinhibitorDetails
Upadacitinibapproved, investigationalnotransportersubstrateinhibitorDetails
Ubrogepantapproved, investigationalunknowntransportersubstrateDetails
Avapritinibapproved, investigationalunknowntransporterinhibitormodulatorDetails
Tafamidisapproved, investigationalunknowntransporterinhibitorDetails
Tazemetostatapproved, investigationalunknowntransportersubstrateDetails
Larotrectinibapproved, investigationalnotransportersubstrateDetails
Tezacaftorapproved, investigationalnotransportersubstrateinhibitorDetails
Rimegepantapproved, investigationalunknowntransportersubstrateDetails
Ozanimodapproved, investigationalunknowntransportersubstrateDetails
Prasteroneapproved, investigational, nutraceuticalunknowntransportersubstrateDetails
Selumetinibapproved, investigationalunknowntransportersubstrateDetails
Tucatinibapproved, investigationalunknowntransportersubstrateDetails
Pemigatinibapproved, investigationalnotransportersubstrateDetails
Capmatinibapproved, investigationalunknowntransporterinhibitorDetails
Pralatrexateapproved, investigationalnotransportersubstrateDetails
Selpercatinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
RipretinibapprovedunknowntransportersubstrateinhibitorDetails
Clofazimineapproved, investigationalunknowntransporterinhibitorDetails
EmpagliflozinapprovedunknowntransportersubstrateDetails
Artesunateapproved, investigationalunknowntransportersubstrateDetails
Dexamethasone acetateapproved, investigational, vet_approvedunknowntransporterinhibitorDetails
Fostemsavirapproved, investigationalunknowntransportersubstrateinhibitorDetails
Risdiplamapproved, investigationalunknowntransportersubstrateDetails
Nifurtimoxapproved, investigationalunknowntransportersubstrateDetails
Pralsetinibapproved, investigationalnotransportersubstrateinhibitorDetails
Lonafarnibapproved, investigationalnotransporterinhibitorDetails
BerotralstatapprovedunknowntransportersubstrateDetails
Relugolixapproved, investigationalunknowntransporterinhibitorDetails
Opicaponeapproved, investigationalnotransportersubstrateDetails
Vericiguatapproved, investigationalunknowntransportersubstrateDetails
Cabotegravirapproved, investigationalunknowntransportersubstrateDetails
Tepotinibapproved, investigationalnotransporterinhibitorDetails
Trilaciclibapproved, investigationalunknowntransportersubstrateDetails
Sulpirideapproved, investigationalunknowntransportersubstrateDetails
Temozolomideapproved, investigationalnotransportersubstrateDetails
AvanafilapprovedunknowntransporterinhibitorDetails
FebuxostatapprovednotransporterinhibitorDetails
Tivozanibapproved, investigationalnotransporterinhibitorDetails
Amisulprideapproved, investigationalnotransportersubstrateDetails
Sotorasibapproved, investigationalunknowntransporterinhibitorDetails
Infigratinibapproved, investigationalnotransportersubstrateinhibitorDetails
Brincidofovirapproved, investigationalnotransporterinhibitorDetails
Belumosudilapproved, investigationalnotransporterinhibitorDetails
Mobocertinibapproved, investigationalunknowntransporterinhibitorDetails
Atogepantapproved, investigationalnotransportersubstrateDetails
Asciminibapproved, investigationalnotransportersubstrateinhibitorDetails
Maribavirapproved, investigationalnotransporterinhibitorDetails
Sotagliflozinapproved, investigationalnotransporterinhibitorDetails
Roxadustatapproved, investigationalunknowntransporterinhibitorDetails
Cannabinolexperimental, investigationalunknowntransporterinhibitorDetails
Pacritinibapproved, investigationalnotransporterinhibitorDetails
Oteseconazoleapproved, investigationalnotransporterinhibitorDetails
AzvudineinvestigationalunknowntargetregulatorDetails
Tecovirimatapproved, investigationalunknowntransporterinhibitorDetails
StiripentolapprovedunknowntransporterinhibitorDetails
Baloxavir marboxilapproved, investigationalunknowntransporterinhibitorDetails
Deucravacitinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Telotristat ethylapproved, investigationalnocarrierbinderDetails
Futibatinibapproved, investigationalnotransportersubstrateDetails
LinzagolixapprovednotransportersubstrateDetails
Niraparibapproved, investigationalnotransportersubstrateinhibitorDetails
Pemetrexedapproved, investigationalnotransporterDetails
Olutasidenibapproved, investigationalnotransporterinhibitorDetails
Pirtobrutinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Elacestrantapproved, investigationalunknowntransporterinhibitorDetails
Daprodustatapproved, investigationalnotransportersubstrateDetails
Sparsentanapproved, investigationalunknowntransportersubstrateinhibitorDetails
Leniolisibapproved, investigationalnotransportersubstrateinhibitorDetails
Aripiprazoleapproved, investigationalunknowntransporterDetails
Vadadustatapproved, investigationalunknowntransporterinhibitorDetails
Quizartinibapproved, investigationalnotransporterinhibitorDetails
Palovaroteneapproved, investigationalnotransporterinhibitorDetails
Momelotinibapproved, investigationalunknowntransportersubstrateinhibitorDetails
Encorafenibapproved, investigationalnotransporterinhibitorDetails
Gefapixantapproved, investigationalnotransportersubstrateDetails
Binimetinibapproved, investigationalnotransportersubstrateDetails
Capivasertibapproved, investigationalnotransporterinhibitorDetails
Repotrectinibapproved, investigationalnotransporterinhibitorDetails
Isavuconazoniumapproved, investigationalunknowntransporterinhibitorDetails
Avatrombopagapproved, investigationalnotransporterinhibitorDetails
Itraconazoleapproved, investigationalunknowntransporterinhibitorDetails
Aprocitentanapproved, investigationalnotransportersubstrateinhibitorDetails
Resmetiromapproved, investigationalunknowntransportersubstrateinhibitorDetails
Danicopanapproved, investigationalnotransporterinhibitorDetails
Tovorafenibapproved, investigationalunknowntransporterinhibitorDetails
Elafibranorapproved, investigationalunknowntransportersubstrateinhibitorDetails
Ensifentrineapproved, investigationalunknowntransportersubstrateDetails
DeuruxolitinibinvestigationalunknowntransportersubstrateinhibitorDetails
Vorasidenibapproved, investigationalunknowntransporterinhibitorDetails
Seladelparapproved, investigationalunknowntransportersubstrateDetails
SulfasalazineapprovedyestargetinhibitorDetails
Lazertinibapproved, investigationalunknowntransporterinhibitorDetails