Target intelligence / Profile preview

Scavenger receptor class B member 1 (SCARB1) (SCARB1)

Target
SCARB1
Molecular classification
Scavenger receptor, Receptor, Transporter, Membrane glycoprotein
01

Overview

Scavenger receptor class B member 1 (SCARB1), also known as SR-BI, is a cell surface glycoprotein that serves as a high-affinity receptor for high-density lipoprotein (HDL) and facilitates the selective uptake of cholesteryl esters and lipophilic micronutrients, including carotenoids such as beta-carotene, lutein, and zeaxanthin (Source 1.2.1, 1.5.3). In cancer, SCARB1 is frequently overexpressed on the membranes of various tumor cells, including those of the prostate, breast, and lung, where it supports high metabolic demands by providing lipids for membrane synthesis and antioxidants to mitigate oxidative stress (Source 1.2.2, 1.2.3). This upregulation is often associated with increased tumor aggressiveness, metastasis, and poor clinical outcomes, making it a significant therapeutic target (Source 1.2.2, 1.2.5). Beyond its role in lipid homeostasis, SCARB1 acts as a co-receptor for viruses like Hepatitis C and SARS-CoV-2 (Source 1.2.5). Therapeutic strategies targeting SCARB1 include small-molecule inhibitors like ITX-5061 to block its transport functions and the development of SCARB1-targeted nanoparticles, such as lycosomes, for the selective delivery of chemotherapeutic agents to tumor cells (Source 1.5.2, 1.5.5). Current research also explores its role in regulating signaling pathways like PI3K/AKT and Src, which further drive cancer cell proliferation and survival (Source 1.1.4, 1.2.2).

Other names
SR-BISRB1CD36L1CLA-1Scavenger receptor class B type IHDL receptorCD36 and LIMPII analogous 1
02

Mechanism of action

Selective uptake of carotenoids and cholesteryl esters from high-density lipoproteins (HDL) into the cell membrane without the internalization of the HDL particle itself.

03

Biological functions

Lipid transportCholesterol homeostasisCarotenoid uptakeSignal transductionCell proliferationAngiogenesis
04

Disease associations

CancerCardiovascular diseaseInfectionInflammation
05

Safety considerations

Potential impact on steroidogenesis in adrenal and gonadal tissuesDisruption of systemic cholesterol homeostasisPotential for off-target effects in the liver
06

Interacting drugs

ITX-5061

3 more in the full profile.

07

Biomarkers

SCARB1 expression levelsHDL-C levels

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