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Scavenger receptor class B type I, ATP-binding cassette transporter A1, ATP-binding cassette transporter G1 (SR-BI, ABCA1, ABCG1)

Target
SR-BI, ABCA1, ABCG1
Molecular classification
Receptor (SR-BI), Transporter (ABCA1, ABCG1)
01

Overview

The major macrophage membrane-associated HDL receptors are Scavenger receptor class B type I (SR-BI), ATP-binding cassette transporter A1 (ABCA1), and ATP-binding cassette transporter G1 (ABCG1). These proteins localize to the plasma membrane of macrophages and facilitate the efflux and transfer of cholesterol and phospholipids to HDL particles in the extracellular space, thereby regulating cholesterol homeostasis and contributing to reverse cholesterol transport. Dysfunction of these receptors in macrophages leads to lipid accumulation, foam cell formation, and increased risk of atherosclerosis. These proteins are considered important therapeutic targets for modulating cardiovascular and metabolic disease risk[3][4]. Note: The queried name is not a single molecule but refers collectively to several functionally related surface proteins on macrophages, with SR-BI, ABCA1, and ABCG1 being the principal and best-validated HDL-interacting molecules in this context[3]. If you are seeking structured information for a singular, canonical target, it is best to specify one of these (for example, "Scavenger receptor class B type I" (SR-BI)), as each has distinct properties and clinical significance[2][3][4].

Other names
HDL receptorHDL binding receptorcholesterol efflux transporter
02

Mechanism of action

Facilitation or inhibition of cholesterol and phospholipid transfer between macrophage membranes and HDL, modulating cholesterol balance

03

Biological functions

Cholesterol effluxLipid transportReverse cholesterol transportRegulation of cellular cholesterol homeostasis
04

Disease associations

Cardiovascular disease (e.g., atherosclerosis)Metabolic disease (e.g., diabetes, under some circumstances)Inflammation (e.g., macrophage foam cell formation in inflammatory lesions)
05

Safety considerations

Targeting these proteins can potentially disturb lipid metabolism, leading to abnormal lipid profiles or increased risk of atherosclerosis if cholesterol export is impairedNo major on-target, drug-specific adverse effects widely characterized, as few direct therapeutics exist; theoretical concerns include impact on other tissues (e.g., hepatic SR-BI and steroidogenic tissues)
06

Interacting drugs

Probucol (inhibits ABCA1)

1 more in the full profile.

07

Biomarkers

SR-BI, ABCA1, and ABCG1 expression levels in macrophages (may inform cardiovascular risk or response to therapy)Cholesterol efflux capacity of patient serum (used in research and clinical studies as a potential marker)

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