Vital role of oligopeptide transporters in physiology and drug transport and their clinical relevance / 药物评价研究

ABSTRACT

The oligopeptide transporters (PEPTs),including PEPT1 and PEPT2,belong to the SLC family and are driven by H+ gradient.PEPT1,the low-affinity and high-capacity transporter,is mainly expressed in small intestine,whereas PEPT2,the high-affinity and low-capacity transporter,is mainly expressed in kidney,brain and lung and has a broader distribution in the organism.The PEPTs are responsible for the absorption and conservation of dietary protein digestion products in intestine and kidney,respectively,and in maintaining homeostasis of neuropeptides in brain.They are also responsible for the absorption and disposition of a number of pharmacologically important compounds including some aminocephalosporins,angiotensin-converting enzyme inhibitors,antiviral prodrugs and others.And PEPTs are also associated with some intestinal diseases and cancer.Therefore,this article summarizes the important role of PEPTs in physiology and drug transport and their clinical relevance.