MSSSNDHVLVPMSQRNNNGLPRTNSRAVRTLAEGDVLSFHHITYRVKVKSGFLVRKTVEK EILSDINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPKGLSGDVLINGAPQPAHFKCCS GYVVQDDVVMGTLTVRENLQFSAALRLPTTMKNHEKNERINTIIKELGLEKVADSKVGTQ FIRGISGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIFS IHQPRYSIFKLFDSLTLLASGKLVFHGPAQKALEYFASAGYHCEPYNNPADFFLDVINGD SSAVMLNREEQDNEANKTEEPSKGEKPVIENLSEFYINSAIYGETKAELDQLPGAQEKKG TSAFKEPVYVTSFCHQLRWIARRSFKNLLGNPQASVAQLIVTVILGLIIGAIYFDLKYDA AGMQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFFGKVMSDLLP MRFLPSVIFTCVLYFMLGLKKTVDAFFIMMFTLIMVAYTASSMALAIATGQSVVSVATLL MTIAFVFMMLFSGLLVNLRTIGPWLSWLQYFSIPRYGFTALQYNEFLGQEFCPGFNVTDN STCVNSYAICTGNEYLINQGIELSPWGLWKNHVALACMIIIFLTIAYLKLLFLKKYS
Note: The complete
sequence may include tag sequence, target protein sequence, linker sequence and extra sequence that is
translated with the protein sequence for the purpose(s) of secretion, stability, solubility, etc.
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Protein Length
full length protein
Tag Info
N-terminal 10xHis-tagged
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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. 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. Also mediates the efflux of sphingosine-1-P from cells. Acts as a urate exporter functioning in both renal and extrarenal urate excretion. In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate. Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates. Mediates the secretion of the riboflavin and biotin vitamins into milk. Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability. Plays an important role in the exclusion of xenobiotics from the brain. 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. In placenta, it limits the penetration of drugs from the maternal plasma into the fetus. May play a role in early stem cell self-renewal by blocking differentiation (Probable).
Gene References into Functions
It is located in the blood-brain barrier limits the entry of endogenous compounds and xenobiotics into the brain, and its expression and activity are regulated by estrogen.PMID:29574357
The hypothesis that ABCG2 plays a fundamental role during mESC differentiation or that regulation of the receptor by xenobiotics may be associated with altered mESC differentiation could not be supported.PMID:28990372
Ultrasound reverses chemoresistance in breast cancer stem cell like cells by reducing ABCG2 expression.PMID:28935760
Which raises the possibility that EGFR-inhibiting drugs may cause ABCG2-mediated DDIs.PMID:28790147
We conclude that mdr1b and bcrp are essential to ovarian protection from chemotoxicity and may have an important physiological role in the ovary.PMID:28216407
deficiency in skin impairs re-epithelialization in cutaneous wound healingPMID:26739701
conclusion, MDR1 and BCRP are expressed on apical membranes of the rodent placental SynT-II layer.PMID:27616577
Bcrp1 (Abcg2), the murine orthologue of the ABC transporter Breast Cancer Resistance Protein (BCRP, ABCG2), has at least four alternative promoters that are designated by the corresponding four alternative first exons produced: E1U, E1A, E1B, and E1C. In-silico protocols are presented to predict alternative promoter usage for Bcrp1.PMID:27286290
Report novel pyrimido[1'',2'':1,5]pyrazolo[3,4-b]quinolones that reverse ABCG2-mediated resistance in cancer cells.PMID:27012188
[(18)F]Mefway is modulated by P-gp, and not by Bcrp in rodents.PMID:26250653
P-gp, Bcrp, Mrp1 and Mrp4 are differentially expressed at the outer and inner blood retinal barrier, resulting in an altered ability to limit substrate distribution at the retina as compared with the blood brain barrierPMID:26507673
Coadministration of ceritinib with a dual ABCB1 and ABCG2 inhibitor may improve treatment of brain (micro) metastases.PMID:26361725
Pparalpha complex translocates from the cytoplasm into the nucleus and further recruits coactivators and transcription machinery which induce the transcription of Abcg2 gene and ultimately results in upregulation of Bcrp protein expression and functionPMID:26465636
Among the ABC drug transporters, only ABCG2 was expressed at highly increased levels in a mouse G3 medulloblastoma model.PMID:26199091
The studies using Bcrp KO mice serve as an estimation of the clinical plasma concentration-time curve changes in ABCG2 421C>A variants for BCRP substrate drugs with the F ratio correcting the systemic clearance change by Bcrp knockout in Bcrp KO mice.PMID:25380981
the renal urate excretion was increased in Abcg2-knockout micePMID:24940679
Data indicate that the brain penetration of ABT-888 in both Abcb1a/1b-/- and Abcb1a/1b-/-;Abcg2-/- mice was significantly higher than in wild-type mice.PMID:24647572
Expression profiling of mRNA isoforms revealed that E1b is predominantly expressed and induced in the lactating mammary gland. E1b promoter sequences in the virgin gland are already hypomethylated and marked with the open chromatin histone mark H3K4me2.PMID:25117410
Abcg2 plays a cytoprotective role in response to in vivo oxidative stress.PMID:24727496
CYT387 was efficiently transported by both human MDR1 and BCRP, and very efficiently by mouse Bcrp1 and its transport could be inhibited by specific MDR1 inhibitor, zosuquidar and/or specific BCRP inhibitor, Ko143.PMID:23827160
Inhibitors also demonstrated similar effects on human and mouse ABCG2.PMID:23868912
This hypoxia-induced ERK 1/2-dependent ABCG2 expression results in resistance to H/R injury, which partially explains the mechanism by which ABCG2 contributes to cellular protection in kidney SP cells.PMID:23032069
In Bcrp1;Mrp2;Mrp3(-/-), but not Bcrp1;Mdr1a/b;Mrp(-/-) mice.PMID:24334255
Bioluminescent imaging of drug efflux at the blood-brain barrier mediated by the transporter ABCG2.PMID:24297888
In conclusion, nuclear transcription factor SF-1 is involved with the regulation of a novel promoter of Bcrp1 that governs transcription of the E1U mRNA isoform in mice.PMID:24189494
Both p-glycoprotein and breast cancer resistance protein restrict brain access for several atiepileptic drugs, information which may be useful in development of treatments for refractory epilepsy.PMID:23588114
Data indicate that Abcc4 limits the brain penetration of camptothecin analogues and teams up with Abcb1a/b and Abcg2 to form a robust cooperative drug efflux system.PMID:23461902
finding that ABCG2 deficiency can generate dysfunctional mitochondria in hepatocytes raises concerns regarding the systematic use of ABCG2 inhibitor in cancer patientsPMID:23954234
characterization of BCRP drug transporter expression and function in AB cellsPMID:23298861
Abcg2 deficiency increases oxidative stress and alters inflammatory response in the brain and exacerbates cognitive/memory deficit in double-tg mice at different developmental stagesPMID:22578166
P-glycoprotein (Mdr1a/1b) and breast cancer resistance protein (Bcrp) decrease the uptake of hydrophobic alkyl triphenylphosphonium cations by the brain.PMID:23454352
Results indicate that the potency and specificity of sildenafil as an inhibitor of ABCB1 and ABCG2 is not sufficient to warrant further clinical testing of this agent in combination with anticancer drugs.PMID:23422148
Bcrp plays a significant role in the efflux of (11)C-SC-62807 in liver and kidneyPMID:23287578
It may be concluded that BCRP plays an important role in the intestinal efflux of MED-5 and limits the bioavailability after oral administration of MED-15.PMID:23333829
Abcg2 modulates cardiac side population cell cycle progression and asymmetric cell division, establishing a mechanistic link between this surface transporter and cardiac progenitor cell function.PMID:23136123
ABCG2 determines the distribution of genistein phase II metabolites and bioavailability.PMID:22736306
we developed a positron emission tomography (PET) protocol to visualize Bcrp function at the murine blood-brain barrierPMID:22828996
Results show that ABCG2 limits the systemic exposure to many different phytoestrogens, by directing their sulfate conjugates for excretion via the feces.PMID:22707564
Lack of ABCG2 shortens latency of BRCA1-deficient mammary tumors.PMID:22767648
Localization of BCRP in endocrine organs together with the efficient allosteric inhibition of the efflux pump by steroid hormones are suggestive for a role for BCRP in steroid hormone regulation.PMID:22581381
The intracellular accumulation of vemurafenib is significantly restricted because of active efflux by P-gp(ABCB1)and BCRP(ABCG2).PMID:22454535
Assessment of activity, exploratory behavior, and anxiety levels revealed behavioral alterations in Abcb1(0/0) and Abcc1 (0/0) mice, whereas Abcg2(0/0) mice were mostly unaffected.PMID:22545122
protein abundance and its efflux pump function. The circadian clock-ATF4 pathway appears to enhance the function of BCRP during a specific time window and to modulate intestinal drug absorptionPMID:22396548
Both P-gp and Bcrp1 reduce the brain penetration of erlotinib.PMID:20963470
PDZK1 plays a pivotal role in the apical localization of BCRP.PMID:21816982
A direct and conclusive Bcrp1 efflux action on phase II metabolites of these isoflavones in vivo and suggest a possible novel concept for ABCG2/BCRP as part of metabolism-driven efflux transport of these conjugates.PMID:21828252
the expression levels of ABCG2 transcripts were also significantly decreased in denervated eyes.PMID:22232434
ATP-binding cassette, G2 subfamily (ABCG2) and BMI-1, predict the transformation of oral leukoplakia to cancer.PMID:22009787
ABCG2 protects against pressure overload-induced cardiac hypertrophy and heart failure by promoting angiogenesis and antioxidant response.PMID:22116099
the capacity and regulation of the breast cancer resistance protein (BCRP)-mediated transport in intact human intestinal epithelial monolayersPMID:22004608
Highly expressed in kidney. Lower expression in liver, colon, heart, spleen, and placenta. Expressed in mammary gland. Expressed in intestinal villi and renal proximal tubules, hepatic bile canalicular membranes, and placental labyrinth cells (at protein