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Cell-surface receptors and transporters (nanoparticle delivery context)

Molecular classification
Receptor, Transporter, Membrane protein
01

Overview

Cell-surface receptors and transporters represent a broad category of membrane-bound proteins utilized as docking sites for ligand-functionalized nanoparticle delivery systems. These targets, such as the transferrin receptor and folate receptor, are frequently exploited because they are overexpressed in pathological tissues like solid tumors (Sahay et al., 2010, Nature Nanotechnology). When a nanoparticle's surface ligands bind to these receptors, they typically trigger receptor-mediated endocytosis, allowing the delivery vehicle to enter the cell and release its therapeutic payload (Kou et al., 2013, African Journal of Pharmacy and Pharmacology). This targeted approach aims to increase the local concentration of drugs at the disease site while minimizing systemic exposure and associated side effects (Bareford & Swaan, 2007, Advanced Drug Delivery Reviews). Beyond simple binding, these proteins facilitate the transport of large or polar molecules that cannot otherwise cross the lipid bilayer (Zhang et al., 2012, ACS Nano). The efficiency of this process is highly dependent on the affinity of the ligand and the density of the target receptor on the cell surface. However, the success of this strategy is often limited by the heterogeneity of receptor expression across patient populations and the challenge of achieving efficient endosomal escape once the vehicle is internalized. Furthermore, off-target accumulation in organs like the liver and spleen remains a significant hurdle for clinical translation of these targeted nanomedicines.

Other names
Cell-surface markers for nanoparticle targetingEndocytic receptorsMembrane transporters for drug deliveryTargeted delivery receptors
02

Mechanism of action

Receptor-mediated endocytosis and carrier-mediated transport facilitate the cellular internalization of nanoparticle-encapsulated therapeutic agents (Sahay et al., 2010, Nature Nanotechnology).

03

Biological functions

EndocytosisTranscytosisCellular uptakeSignal transductionLigand binding
04

Disease associations

CancerInflammationInfectionGenetic disorders
05

Safety considerations

Off-target uptake by the mononuclear phagocyte systemLysosomal sequestration of the payloadImmunogenicity of the delivery vehiclePotential saturation of endogenous transport pathways
06

Interacting drugs

Liposomal doxorubicin

4 more in the full profile.

07

Biomarkers

Folate receptor alpha expressionTransferrin receptor (CD71) levelsHER2/neu expressionIntegrin alpha-v beta-3 levels

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