寡肽转运体在生理、药物转运的重要作用及临床相关性

Vital role of oligopeptide transporters in physiology and drug transport and their clinical relevance

寡肽转运体(PEPTs)属于溶质转运体(SLC)大家族,以H^+梯度为驱动力,包括PEPT1和PEPT2。PEPT1是低亲和力、高容量转运蛋白,主要表达于小肠;而PEPT2是高亲和力、低容量的转运蛋白,主要在肾脏、脑和肺中表达,在生物体中分布较广。PEPTs除重吸收二肽和三肽以及维持脑中神经肽的稳态作用外,还能够吸收和处置许多重要的化合物,如一些氨基头孢菌素、血管紧张素转化酶抑制剂、抗病毒前药等,而且PEPTs也与一些肠道疾病和癌症相关。因此综述了PEPTs在生理、药物转运中的重要作用及临床相关性。

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.