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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。
Oligopeptide transporters (PEPTs) belong to the large family of solute transporters (SLCs) driven by H ~ + gradients, including PEPT1 and PEPT2. PEPT1 is a low-affinity, high-capacity transporter and is mainly expressed in the small intestine. PEPT2 is a high-affinity, low-capacity transporter mainly expressed in the kidney, brain and lung, and widely distributed in organisms. In addition to reabsorption of dipeptides and tripeptides and the maintenance of neuropeptide homeostasis in the brain, PEPTs are also capable of absorbing and treating many important compounds such as some aminocephalosporins, angiotensin converting enzyme inhibitors, antiviral prodrugs Etc., and PEPTs are also associated with some intestinal diseases and cancers. This review summarizes the important role and clinical relevance of PEPTs in physiology and drug delivery.