寡肽轉(zhuǎn)運體（PEPTs）屬于溶質(zhì)轉(zhuǎn)運體（SLC）大家族，以H⁺梯度為驅(qū)動力，包括PEPT1和PEPT2。PEPT1是低親和力、高容量轉(zhuǎn)運蛋白，主要表達(dá)于小腸；而PEPT2是高親和力、低容量的轉(zhuǎn)運蛋白，主要在腎臟、腦和肺中表達(dá)，在生物體中分布較廣。PEPTs除重吸收二肽和三肽以及維持腦中神經(jīng)肽的穩(wěn)態(tài)作用外，還能夠吸收和處置許多重要的化合物，如一些氨基頭孢菌素、血管緊張素轉(zhuǎn)化酶抑制劑、抗病毒前藥等，而且PEPTs也與一些腸道疾病和癌癥相關(guān)。因此綜述了PEPTs在生理、藥物轉(zhuǎn)運中的重要作用及臨床相關(guān)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.

國家自然科學(xué)基金項目（81473280）