Journal
CURRENT DRUG METABOLISM
Volume 16, Issue 1, Pages 71-83Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389200216666150401110754
Keywords
PepT1; ASBT; prodrug; oral bioavailability; tissue targeting
Funding
- National Nature Science Foundation of China [81173009, 30973655]
- Project for Excellent Talents of Liaoning Province [LR20110028]
- Program for New Century Excellent Talents in University [NCET-12-1015]
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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.
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