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. 2019 Jan 10;9(5):902–922. doi: 10.1016/j.apsb.2019.01.004

Table 3.

Representative ligand-mediated transport in oral delivery of therapeutic peptides/proteins.

Name Distribution/Function Characteristics Ref.
Bile acid transporters In the epithelium of ileum The ASBT in the small intestine transports bile acids into epithelial cells for bile acid recycling 5., 48., 52., 76., 77., 78., 79., 80., 81.
UEA-1 In M-cell M-cell selective molecular signature 20
Lectin-like protein receptors In the intestine Proteins or glycoproteins specifically recognize the carbohydrate moieties on the intestine 42
Biotin (vitamin B7) receptor In the intestine The biotin receptor distributes throughout the small intestine 55
Proton-coupled oligopeptide transporters PepT1 and PepT2 In the brush border membrane of the small intestine Driven by the presence of an inward H+ gradient and a negative membrane potential. Transports various natural di/tri-peptides and comprehensive peptide-mimetics. High capacity, low affinity 82., 83.
CSK peptide transporters In goblet cells CSK peptide specifically recognize goblet cells 84
AT-1002 peptide Open TJs A hexamer peptide derived from ZOT open the TJs transiently and reversibly 85
Monocarboxylate transporter In the intestine Cellular uptake of SCFAs efficiently, among which butyrate is in majority, a key mediator of physiological function in the intestine 86
CD44 receptor In the intestine A highly heterogeneous single-stranded transmembrane glycoprotein widely expressed on the membrane 87

ASBT, apical sodium-dependent bile acid transporter; CSK, CSKSSDYQC; ZOT, zonula occludins toxin; TJs, tight junctions; UEA-1, ulex europaeus agglutinin-1; SCFAs, short chain fatty acids.