Target intelligence / Profile preview

Scavenger receptor class B member 1 (SR-BI) (SR-BI)

Target
SR-BI
Molecular classification
Scavenger receptor, Lipoprotein receptor, Transporter, Receptor
01

Overview

Scavenger receptor class B member 1 (SR-BI) is a multi-ligand cell surface glycoprotein that serves as the primary receptor for high-density lipoprotein (HDL). It is highly expressed in the liver and steroidogenic tissues, where it mediates the selective uptake of cholesteryl esters from HDL without the internalization and degradation of the HDL particle itself (PMID: 8598915). In the context of the foam cell formation pathway, SR-BI plays a pivotal role in reverse cholesterol transport, facilitating the removal of excess cholesterol from peripheral tissues, including macrophages, for transport back to the liver (PMID: 10676942). While its hepatic function is generally considered cardioprotective, its role in macrophages and other peripheral cells is more complex and can influence the development of atherosclerosis and foam cell accumulation. Beyond lipid metabolism, SR-BI is a known co-receptor for the Hepatitis C virus (HCV) entry into hepatocytes, making it a target for antiviral drug development, such as the antagonist ITX-5061 (PMID: 20603045). Therapeutic modulation of SR-BI remains challenging due to its essential role in producing steroid hormones and the potential for off-target effects on lipid homeostasis.

Other names
SCARB1CD36L1CLA-1SRB1Scavenger receptor class B type I
02

Mechanism of action

SR-BI facilitates the selective uptake of cholesteryl esters from high-density lipoprotein (HDL) into cells and mediates the bidirectional flux of free cholesterol between the cell membrane and lipoproteins (PMID: 8598915, 10676942).

03

Biological functions

Reverse cholesterol transportSelective lipid uptakeLipid metabolismSteroidogenesisViral entry
04

Disease associations

Cardiovascular diseaseAtherosclerosisHepatitis CHypercholesterolemiaCancer
05

Safety considerations

Potential impairment of adrenal and gonadal steroidogenesisRisk of altered biliary cholesterol secretion and gallstone formationComplex tissue-specific effects on atherosclerosis riskSusceptibility to viral infections (e.g., HCV)
06

Interacting drugs

ITX-5061

3 more in the full profile.

07

Biomarkers

HDL-cholesterol levelsSCARB1 genetic variants (e.g., P297S mutation) (PMID: 26965621)Hepatic SR-BI protein expression levelsCholesteryl ester transfer rates

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