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Cell-surface receptors on blood-brain barrier endothelial cells" refers to a diverse set of proteins located on the luminal and abluminal surfaces of the endothelial cells lining cerebral blood vessels. They serve as molecular gatekeepers, mediating the highly selective translocation of substances between blood and brain, including nutrients, signaling molecules, and drugs. These receptors encompass multiple families — such as G protein-coupled receptors (e.g., sphingosine-1-phosphate receptors), transporter proteins (e.g., P-glycoprotein, organic anion polypeptide transporters), receptor tyrosine kinases (e.g., insulin receptor), adhesion molecules (e.g., PECAM-1, VE-cadherin), and metabolic enzymes (e.g., cytochrome P450 variants)[1][2][3][4][5]. They are essential both in maintaining CNS homeostasis and as therapeutic targets or delivery portals for central nervous system drug development, but targeting them requires careful consideration due to the risk of impairing the protective function of the BBB.
Direct modulation of receptor- or transporter-mediated signaling or transport (e.g., receptor agonism/antagonism). Efflux/influx inhibition (for transporters). Use as portals for drug delivery via receptor-mediated transcytosis. Blocking immune cell adhesion for anti-inflammatory strategies.
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