TITLE

Advances in research of PepT1-targeted prodrug

AUTHOR(S)
Feng Cao; Yahan Gao; Qineng Ping
PUB. DATE
February 2012
SOURCE
Asian Journal of Pharmaceutical Sciences;2012, Vol. 7 Issue 1, p110
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
The mammalian proton-coupled peptide transporter 1 (PepT1), which is predominantly located principally on the luminal cell membrane of the intestine, plays an important role in the absorption of di- and tripeptides from the digestion of ingested protein. A lot of poorly absorbed drugs have been modified into peptidomimetic prodrugs with affinity for PepT1 to improve permeability across intestinal membrane, and eventually enhance oral bioavailability of the drugs. Due to the broad substrate specificity of the transporter this strategy has become a hot topic of research on targeted prodrug. This review addressed progress of functional properties of PepT1, expression and transporter structure of PepT1 and structural features of PepT1 substrates. In addition, PepT1-targeted prodrugs with various structures (amide, ester and other types) and different functions, such as improvement of oral bioavailability, circumvention of drug efflux transporter, increase of ocular bioavailability, improvement of tumor targetability and efficiency, have also been summarized. With the recognition of crystal structural model of PepT1 just provided in 2011, rational design of peptidomimetic drugs/prodrugs utilizing the transport activity of PepT1 is expected.
ACCESSION #
76385095

 

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