ABCG subfamily | Transporters | IUPHAR/BPS Guide to IMMUNOPHARMACOLOGY

ABCG subfamily C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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This family of 'half-transporters' act as homo- or heterodimers; particularly ABCG5 and ABCG8 are thought to be obligate heterodimers. The ABCG5/ABCG heterodimer sterol transporter structure has been determined [3], suggesting an extensive intracellular nucleotide binding domain linked to the transmembrane domains by a fold in the primary sequence. The functional ABCG2 transporter appears to be a homodimer with structural similarities to the ABCG5/ABCG8 heterodimer [1,5].

Transporters

Targets of relevance to immunopharmacology are highlighted in blue

ABC8 (ABCG1) C Show summary »« Hide summary

Target Id	791
Systematic nomenclature	ABCG1
Common abbreviation	ABC8
Previous and unofficial names	ATP-binding cassette transporter 8 \| ATP-binding cassette sub-family G member 1 \| ATP-binding cassette, sub-family G (WHITE), member 1 \| ATP-binding cassette, subfamily G (WHITE), member 1
Genes	ABCG1 (Hs), Abcg1 (Mm), Abcg1 (Rn)
Ensembl ID	ENSG00000160179 (Hs), ENSMUSG00000024030 (Mm), ENSRNOG00000001158 (Rn)
UniProtKB AC	P45844 (Hs), Q64343 (Mm)
Comment	Transports sterols and choline phospholipids [2]

ABCP (ABCG2) C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

792

Systematic nomenclature

ABCG2

Common abbreviation

ABCP

Previous and unofficial names

Genes

ABCG2 (Hs), Abcg2 (Mm), Abcg2 (Rn)

Ensembl ID

ENSG00000118777 (Hs), ENSMUSG00000029802 (Mm), ENSRNOG00000007041 (Rn)

UniProtKB AC

Q9UNQ0 (Hs), Q7TMS5 (Mm), Q80W57 (Rn)

Inhibitors

cyclosporin A pK_i 6.3 [4]

Comment

Exhibits a broad substrate specificity, including urate and haem, as well as multiple synthetic compounds [2].

ABCG4 C Show summary »« Hide summary

Target Id	793
Systematic nomenclature	ABCG4
Previous and unofficial names	White2 \| ATP-binding cassette, subfamily G, member 4 \| ATP-binding cassette, sub-family G (WHITE), member 4 \| ATP-binding cassette, subfamily G (WHITE), member 4
Genes	ABCG4 (Hs), Abcg4 (Mm), Abcg4 (Rn)
Ensembl ID	ENSG00000172350 (Hs), ENSMUSG00000032131 (Mm), ENSRNOG00000008862 (Rn)
UniProtKB AC	Q9H172 (Hs)
Comment	Putative functional dependence on ABCG1

ABCG5 C Show summary »« Hide summary

Target Id	794
Systematic nomenclature	ABCG5
Previous and unofficial names	White3 \| ATP-binding cassette sub-family G (WHITE) member 5 (sterolin 1) \| ATP-binding cassette sub-family G member 5 \| cmp \| trac \| STSL \| ATP-binding cassette, subfamily G (WHITE), member 5
Genes	ABCG5 (Hs), Abcg5 (Mm), Abcg5 (Rn)
Ensembl ID	ENSG00000138075 (Hs), ENSMUSG00000040505 (Mm), ENSRNOG00000005250 (Rn)
UniProtKB AC	Q9H222 (Hs), Q99PE8 (Mm), Q99PE7 (Rn)
Comment	The ABCG5/ABCG8 heterodimer transports phytosterols and cholesterol [3]. Loss-of-function mutations in ABCG5 or ABCG8 are associated with sitosterolemia (OMIM: 210250).

ABCG8 C Show summary »« Hide summary

Target Id	795
Systematic nomenclature	ABCG8
Previous and unofficial names	GBD4 \| ATP-binding cassette, sub-family G (WHITE), member 8 (sterolin 2) \| gallbladder disease 4 \| ATP-binding cassette sub-family G member 8 \| ATP-binding cassette, subfamily G (WHITE), member 8
Genes	ABCG8 (Hs), Abcg8 (Mm), Abcg8 (Rn)
Ensembl ID	ENSG00000143921 (Hs), ENSMUSG00000024254 (Mm), ENSRNOG00000005420 (Rn)
UniProtKB AC	Q9H221 (Hs), Q9DBM0 (Mm), P58428 (Rn)
Comment	The ABCG5/ABCG8 heterodimer transports phytosterols and cholesterol [3]. Loss-of-function mutations in ABCG5 or ABCG8 are associated with sitosterolemia (OMIM: 210250).

References

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1. Alexander SPH, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL et al.. (2019) THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Transporters. Br J Pharmacol, 176 Suppl 1: S397-S493. [PMID:31710713]

2. Kerr ID, Haider AJ, Gelissen IC. (2011) The ABCG family of membrane-associated transporters: you don't have to be big to be mighty. Br J Pharmacol, 164 (7): 1767-79. [PMID:21175590]

3. Lee JY, Kinch LN, Borek DM, Wang J, Wang J, Urbatsch IL, Xie XS, Grishin NV, Cohen JC, Otwinowski Z et al.. (2016) Crystal structure of the human sterol transporter ABCG5/ABCG8. Nature, 533 (7604): 561-4. [PMID:27144356]

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. 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]

NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Transporters. Br J Pharmacol. 180 Suppl 2:S374-469.