ABCA1 | ABCA subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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ABCA1

Target not currently curated in GtoImmuPdb

Target id: 756

Nomenclature: ABCA1

Abbreviated Name: ABC1, CERP

Systematic Nomenclature: ABCA1

Family: ABCA subfamily

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - ABCA1 ATP binding cassette subfamily A member 1
Mouse - - Abca1 ATP-binding cassette, sub-family A (ABC1), member 1
Rat - - Abca1 ATP binding cassette subfamily A member 1
Previous and Unofficial Names
ABC1 | HDLDT1 | ATP-binding cassette, sub-family A (ABC1), member 1 | Cholesterol efflux regulatory protein | ATP-binding cassette, subfamily A (ABC1), member 1 | ATP-binding cassette
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
UniProtKB
Wikipedia

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
probucol Hs Inhibition - - 1,4
[1,4]
Description: Inhibition of cholesterol efflux from normal human skin fibroblasts, but not from fibroblasts negative in ABCA1.
Inhibitor Comments
Favari et al. (2005) report that probucol inhibits ABCA1-mediated cholesterol efflux from in vitro cultured mouse J774 cells by 80%, and from human fibroblasts by >50% [1].
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
bihelical apoA-I mimetic peptide 5A Hs Binding - - 3
The 5A sequence was able to solubilize phospholipid vesicles and stimulated cholesterol and phospholipid efflux by the ABCA1 transporter with high specificity but no specific binding data was reported [3]
General Comments
Loss-of-function mutations in ABCA1 are associated with Tangier disease, in which plasma HDL cholesterol levels are greatly reduced. ABCA1 is a key player in cholesterol efflux from macrophages to lipid-free apo-A1 in a process known as reverse cholesterol transport, a role that is important in atherosclerosis. ABCA1 also controls apoE lipidation, and has a role in Alzheimer's disease, including an impact on deposition and clearance. ABCA1 is transcriptionally regulated by Liver X receptors (LXR) and retinoic X receptor (RXR), which are being explored as therapeutic targets for development of agonists for treatment of metabolic and neurodegenerative disorders [2].

References

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1. Favari E, Zanotti I, Zimetti F, Ronda N, Bernini F, Rothblat GH. (2004) Probucol inhibits ABCA1-mediated cellular lipid efflux. Arterioscler. Thromb. Vasc. Biol., 24 (12): 2345-50. [PMID:15514211]

2. Koldamova R, Fitz NF, Lefterov I. (2014) ATP-binding cassette transporter A1: from metabolism to neurodegeneration. Neurobiol. Dis., 72 Pt A: 13-21. [PMID:24844148]

3. Sethi AA, Stonik JA, Thomas F, Demosky SJ, Amar M, Neufeld E, Brewer HB, Davidson WS, D'Souza W, Sviridov D et al.. (2008) Asymmetry in the lipid affinity of bihelical amphipathic peptides. A structural determinant for the specificity of ABCA1-dependent cholesterol efflux by peptides. J. Biol. Chem., 283 (47): 32273-82. [PMID:18805791]

4. Wu CA, Tsujita M, Hayashi M, Yokoyama S. (2004) Probucol inactivates ABCA1 in the plasma membrane with respect to its mediation of apolipoprotein binding and high density lipoprotein assembly and to its proteolytic degradation. J. Biol. Chem., 279 (29): 30168-74. [PMID:15140889]

Contributors

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