Cell-surface uptake receptors

Cell-surface uptake receptors represent a broad functional class of membrane proteins responsible for the internalization of extracellular substances, including nutrients, signaling molecules, and pathogens (Source: PubMed, PMID: 35564321). These receptors, such as the asialoglycoprotein receptor (ASGPR), transferrin receptor (TfR), and Niemann-Pick C1-like 1 (NPC1L1), typically operate through receptor-mediated endocytosis to maintain cellular homeostasis (Source: UniProt; NIH). In drug development, they are extensively utilized as gateways for targeted delivery; for instance, GalNAc-conjugated oligonucleotides exploit ASGPR for liver-specific uptake, while antibody-drug conjugates (ADCs) target overexpressed receptors in cancer cells (Source: Alnylam Pharmaceuticals; Nature Reviews Drug Discovery). Furthermore, these receptors can serve as entry points for viruses, such as ACE2 for SARS-CoV-2 (Source: AHA Journals). Therapeutic strategies involving these receptors must account for endosomal escape, receptor recycling kinetics, and potential off-target effects in tissues where the receptor is constitutively expressed (Source: PubMed).

Other names

Endocytic receptorsInternalization receptorsCell-surface transport receptorsUptake receptors

Drugs targeting these receptors typically utilize them for cellular entry via receptor-mediated endocytosis. Once bound, the drug-receptor complex is internalized into endosomes, where the drug is released to reach its intracellular target (Source: Nature Reviews Drug Discovery).