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Target not currently curated in GtoImmuPdb

Target id: 756

Nomenclature: ABCA1

Abbreviated Name: ABC1, CERP

Systematic Nomenclature: ABCA1

Family: ABCA subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 15 2261 9q31.1 ABCA1 ATP binding cassette subfamily A member 1
Mouse 15 2261 4 28.57 cM Abca1 ATP-binding cassette, sub-family A member 1
Rat - - Abca1 ATP binding cassette subfamily A member 1
Previous and Unofficial Names Click here for help
ABC1 | ATP-binding cassette | ATP-binding cassette, sub-family A (ABC1), member 1 | ATP-binding cassette, subfamily A (ABC1), member 1 | Cholesterol efflux regulatory protein | HDLDT1
Database Links Click here for help
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas

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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
probucol Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition - - 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 Peptide Immunopharmacology Ligand 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]
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
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].


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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]


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