Gene and Protein Information
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

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
Alphafold	O95477 (Hs), P41233 (Mm)
ChEMBL Target	CHEMBL2362986 (Hs), CHEMBL1641361 (Mm)
DrugBank Target	O95477 (Hs)
Ensembl Gene	ENSG00000165029 (Hs), ENSMUSG00000015243 (Mm), ENSRNOG00000018126 (Rn)
Entrez Gene	19 (Hs), 11303 (Mm), 313210 (Rn)
Human Protein Atlas	ENSG00000165029 (Hs)
KEGG Gene	hsa:19 (Hs), mmu:11303 (Mm), rno:313210 (Rn)
Pharos	O95477 (Hs)
UniProtKB	O95477 (Hs), P41233 (Mm)
Wikipedia	ABCA1 (Hs)

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 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]

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].