ABCG2 | ABCG subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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ABCG2

Target not currently curated in GtoImmuPdb

Target id: 792

Nomenclature: ABCG2

Abbreviated Name: ABCP

Systematic Nomenclature: ABCG2

Family: ABCG subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - ABCG2 ATP binding cassette subfamily G member 2 (Junior blood group)
Mouse - - Abcg2 ATP binding cassette subfamily G member 2 (Junior blood group)
Rat - - Abcg2 ATP binding cassette subfamily G member 2
Previous and Unofficial Names
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
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Selected 3D Structures
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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
cyclosporin A 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 N/A Inhibition 6.2 pIC50
pIC50 6.2 (IC50 5.9x10-7 M)
Description: Pheo A assay
compound 14 [PMID: 30925062] 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 N/A Inhibition - -
Fumitremorgin C 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. U.S.A., 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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