With the rapid development of molecular biology, various of drug transporters have
been discovered in several important organs of the body, which determine intracellular exposure
and pharmacokinetic performances of drugs by modulating cellular entry and exit. This article
focuses on the design of transporter-linked prodrug to enhance oral bioavailability and to acquire
tissue-specific distribution pattern, especially paying attention to peptide transporter 1 (PepT1)
and apical sodium dependent bile acid transporter (ASBT). Conjugation of the native promotety
to active drug was one of the effective methods to improve membrane permeability and distribution
profiles of drugs. In this review, we highlight the transporter-linked prodrug design modality based on PepT1 and ASBT. The biology
of transporters, structure-transport relationship, key features of natural substrates and successful examples of transporter-linked prodrugs
are overviewed in detail.
Keywords: PepT1, ASBT, prodrug, oral bioavailability, tissue targeting.
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