Bioactivatable pseudo-tripeptidization of cyclic dipeptides to increase the affinity toward oligopeptide transporter 1 for enhanced oral absorption: an application to cyclo(L-Hyp-L-Ser) (JBP485).
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DOI: 10.1021/acs.jmedchem.9b00358
Abstract: The cyclic dipeptides generally present lower affinity toward intestinal oligopeptide transporter 1 (PEPT1) than the linear dipeptides. JBP485 (cyclo(L-Hyp-L-Ser)) is a low-affinity substrate of PEPT1 with poor oral bioavailability. However, JBP923 (L-Hyp-L-Ser) is a high-affinity… read more here.
Keywords: cyclic dipeptides; affinity; hyp ser; pseudo tripeptidization ... See more keywords