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ABCG2

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Target not currently curated in GtoImmuPdb

Target id: 792

Nomenclature: ABCG2

Abbreviated Name: ABCP

Systematic Nomenclature: ABCG2

Family: ABCG subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 655 4q22.1 ABCG2 ATP binding cassette subfamily G member 2 (JR blood group)
Mouse 6 657 6 27.82 cM Abcg2 ATP binding cassette subfamily G member 2 (Junior blood group)
Rat 6 657 4q24 Abcg2 ATP binding cassette subfamily G member 2
Previous and Unofficial Names Click here for help
BCRP | breast cancer resistance protein | mitoxantrone resistance-associated protein | MXR | Placenta-specific ATP- binding cassette transporter | ABCP | CD338 | ATP-binding cassette protein G2 | ATP-binding cassette sub-family G member 2 | ATP-binding cassette, sub-family G (WHITE), member 2 | BCRP1 | breast cancer resistance protein 1 homolog | ATP-binding cassette, sub-family G (WHITE), member 2 (Junior blood group) | ATP-binding cassette, subfamily G (WHITE), member 2 | ATP-binding cassette | ATP binding cassette subfamily G member 2 (Junior blood group)
Database Links Click here for help
Alphafold Q9UNQ0 (Hs), Q7TMS5 (Mm), Q80W57 (Rn)
ChEMBL Target CHEMBL5393 (Hs), CHEMBL2073705 (Mm), CHEMBL3509585 (Rn)
Ensembl Gene ENSG00000118777 (Hs), ENSMUSG00000029802 (Mm), ENSRNOG00000007041 (Rn)
Entrez Gene 9429 (Hs), 26357 (Mm), 312382 (Rn)
Human Protein Atlas ENSG00000118777 (Hs)
KEGG Gene hsa:9429 (Hs), mmu:26357 (Mm), rno:312382 (Rn)
OMIM 603756 (Hs)
Pharos Q9UNQ0 (Hs)
UniProtKB Q9UNQ0 (Hs), Q7TMS5 (Mm), Q80W57 (Rn)
Wikipedia ABCG2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of wild-type, human ABCG2 in complex with two antigen-binding fragments of 5D3 (5D3-Fab)
PDB Id:  5NJ3
Resolution:  3.8Å
Species:  Human
References:  6

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
cyclosporin A Peptide Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.3 pKi 4
⤷ pKi 6.3 (Ki 5x10-7 M) [4]
Description: Inhibition of ABCG2-ATPase activity induced by substrate binding.
KS 176 Small molecule or natural product N/A Inhibition 6.2 pIC50
⤷ pIC50 6.2 (IC50 5.9x10-7 M)
Description: Pheo A assay
compound 14 [PMID: 30925062] Small molecule or natural product Click here for species-specific activity table Hs Non-competitive 5.6 pIC50 5
⤷ pIC50 5.6 (IC50 2.38x10-6 M) [5]
Description: Measuring inhibition in MDCK II BCRP cells expressing hABCG2 by pheophorbide A assay.
Ko 143 Small molecule or natural product N/A Inhibition - -
⤷
Fumitremorgin C Small molecule or natural product N/A Inhibition - -
⤷
View species-specific inhibitor tables
General Comments
ABCG2 causes multidrug resistance in cancer [1-3].

References

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1. Allikmets R, Schriml LM, Hutchinson A, Romano-Spica V, Dean M. (1998) A human placenta-specific ATP-binding cassette gene (ABCP) on chromosome 4q22 that is involved in multidrug resistance. Cancer Res, 58 (23): 5337-9. [PMID:9850061]

2. Doyle LA, Yang W, Abruzzo LV, Krogmann T, Gao Y, Rishi AK, Ross DD. (1998) A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci USA, 95 (26): 15665-70. [PMID:9861027]

3. Miyake K, Mickley L, Litman T, Zhan Z, Robey R, Cristensen B, Brangi M, Greenberger L, Dean M, Fojo T et al.. (1999) Molecular cloning of cDNAs which are highly overexpressed in mitoxantrone-resistant cells: demonstration of homology to ABC transport genes. Cancer Res, 59 (1): 8-13. [PMID:9892175]

4. Ozvegy C, Litman T, Szakács G, Nagy Z, Bates S, Váradi A, Sarkadi B. (2001) Functional characterization of the human multidrug transporter, ABCG2, expressed in insect cells. Biochem Biophys Res Commun, 285 (1): 111-7. [PMID:11437380]

5. Silbermann K, Stefan SM, Elshawadfy R, Namasivayam V, Wiese M. (2019) Identification of Thienopyrimidine Scaffold as an Inhibitor of the ABC Transport Protein ABCC1 (MRP1) and Related Transporters Using a Combined Virtual Screening Approach. J Med Chem, 62 (9): 4383-4400. [PMID:30925062]

6. Taylor NMI, Manolaridis I, Jackson SM, Kowal J, Stahlberg H, Locher KP. (2017) Structure of the human multidrug transporter ABCG2. Nature, 546 (7659): 504-509. [PMID:28554189]

Contributors

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