ABCG2 Membrane Protein Introduction

Introduction of ABCG2

ABCG2, ATP-binding cassette sub-family G member 2 is a protein that in humans is encoded by the ABCG2 gene. ABCG2 is a constitutively expressed ATP-binding cassette (ABC) transporter that protects many tissues against xenobiotic molecules. Its activity affects the pharmacokinetics of commonly used drugs and limits the delivery of therapeutics into tumor cells, thus contributing to multidrug resistance.

Basic Information of ABCG2
Protein Name	ATP-binding cassette sub-family G member 2
Gene Name	ABCG2
Aliases	Breast cancer resistance protein, CDw338, Mitoxantrone resistance-associated protein, Placenta-specific ATP-binding cassette transporter, Urate exporter, CD antigen: CD338, ABCP, BCRP, BCRP1, MXR
Organism	Homo sapiens (Human)
UniProt ID	Q9UNQ0
Transmembrane Times	6
Length (aa)	655
Sequence	MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVEKEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCNSGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGTQFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIFSIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIINGDSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKKITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDSTGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLPMRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLLMTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGNNPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS

Function of ABCG2 Membrane Protein

ATP binding cassette superfamily, subfamily G (WHITE), member 2, is a multidrug resistance transporter, which is expressed in the placenta and is involved in the transport of specific molecules into or out the placenta, homolog to Drosophila white and yeast ADP1 gene ABCG2. It has high-capacity urate exporter function in both renal and extrarenal urate excretion. And it plays a role in porphyrin homeostasis as it is able to mediate the export of protoporphyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter may play an important role in the exclusion of xenobiotics from the brain. It also appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. ABCG2 is also implicated in the efflux of numerous drugs and xenobiotics: mitoxantrone, the photosensitizer pheophorbide, camptothecin, methotrexate, azidothymidine (AZT), and the anthracyclines daunorubicin and doxorubicin.

Fig.1 ABCG2 structure. (Taylor, 2017)

Application of ABCG2 Membrane Protein in Literature

Robey R.W., et al. Revisiting the role of ABC transporters in multidrug-resistant cancer. Nat Rev Cancer. 2018, 18(7): 452-464. PubMed ID: 29643473

This article presents recent evidence indicating that it is time to revisit the investigation into the role of ABC transporters including ABCG2 in the efficient drug delivery in various cancer types and at the blood-brain barrier. This is to evaluate whether these transporters play a clinical role in multidrug resistance.
Taylor N.M.I., et al. Structure of the human multidrug transporter ABCG2. Nature. 2017, 546(7659): 504-509. PubMed ID: 28554189

This article presents the structure of human ABCG2 determined by cryo-electron microscopy, providing the first high-resolution insight into a human multidrug transporter.
Li Y., et al. Genetic Lineage Tracing of Non-Myocyte Population by Dual Recombinases. Circulation. 2018, 138(8): 793-805. PubMed ID: 29700121

This study provides in vivo genetic evidence for non-myocyte to myocyte conversion in embryonic but not adult heart, arguing again the myogenic potential of putative stem cell populations for cardiac regeneration in the adult stage. This study also provides a new genetic strategy to identify endogenous stem cells, if any, in other organ systems for tissue repair and regeneration.
Jackson S.M., et al. Structural basis of small-molecule inhibition of human multidrug transporter ABCG2. Nat Struct Mol Biol. 2018, 25(4): 333-340. PubMed ID: 29610494

This article presents cryo-EM structures of human ABCG2 bound to synthetic derivatives of the fumitremorgin C-related inhibitor Ko143 or the multidrug resistance modulator tariquidar.
Kawabata K.C., et al. High expression of ABCG2 induced by EZH2 disruption has pivotal roles in MDS pathogenesis. Leukemia. 2018, 32(2): 419-428. PubMed ID: 28720764

This report indicates that ABCG2 de-repression induced by EZH2 mutations has crucial roles in MDS pathogenesis.

ABCG2 Preparation Options

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Reference

Taylor N M I, et al. (2017). Structure of the human multidrug transporter ABCG2. Nature. 546(7659): 504-509.

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