Target intelligence / Profile preview

ATP-binding cassette transporter A1 (ABCA1)

Target
ABCA1
Molecular classification
Transporter, ABC transporter (ATP-binding cassette transporter), Primary active transporter
01

Overview

ATP-binding cassette transporter A1 (ABCA1) is a membrane protein that regulates cholesterol homeostasis by facilitating the transfer of cholesterol and phospholipids from cells to lipid-poor apolipoproteins, initiating high-density lipoprotein (HDL) formation. ABCA1's activity is essential for removing excess cholesterol from macrophages, thereby reducing inflammation and slowing atherosclerosis progression; it is regulated by cholesterol flux and genetic/epigenetic factors including miRNAs. Although "ssuACB cluster" is known as a bacterial ABC-type transporter involved in sulfate or metal import, it is not implicated in mammalian cholesterol metabolism—thus, the target as named is not correct for therapeutic or research purposes in this context.

Other names
ABCA1ATP-binding cassette subfamily A member 1
02

Mechanism of action

Promotion of cholesterol efflux and HDL formation; Antagonism of foam cell (macrophage) formation in vascular walls; Regulation of inflammatory signaling

03

Biological functions

Cholesterol effluxHDL (high-density lipoprotein) formationLipid transportAnti-inflammatory activity
04

Disease associations

AtherosclerosisCardiovascular diseaseMetabolic syndromeRare genetic disorders (e.g., Tangier disease)
05

Safety considerations

Dysregulation can lead to abnormal cholesterol levels, contributing to atherosclerosisGenetic loss-of-function leads to Tangier disease
06

Interacting drugs

statins

1 more in the full profile.

07

Biomarkers

Plasma HDL levels (for ABCA1 activity)Monocyte/macrophage ABCA1 expression

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