Institute for Biomedical Sciences, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, Georgia, USA.
Veterans Affairs Medical Center, Decatur, Georgia, USA.
Compr Physiol. 2018 Mar 25;8(2):731-760. doi: 10.1002/cphy.c170032.
Mammalian members of the proton-coupled oligopeptide transporter family are integral membrane proteins that mediate the cellular uptake of di/tripeptides and peptide-like drugs and couple substrate translocation to the movement of H , with the transmembrane electrochemical proton gradient providing the driving force. Peptide transporters are responsible for the (re)absorption of dietary and/or bacterial di- and tripeptides in the intestine and kidney and maintaining homeostasis of neuropeptides in the brain. These proteins additionally contribute to absorption of a number of pharmacologically important compounds. In this overview article, we have provided updated information on the structure, function, expression, localization, and activities of PepT1 (SLC15A1), PepT2 (SLC15A2), PhT1 (SLC15A4), and PhT2 (SLC15A3). Peptide transporters, in particular, PepT1 are discussed as drug-delivery systems in addition to their implications in health and disease. Particular emphasis has been placed on the involvement of PepT1 in the physiopathology of the gastrointestinal tract, specifically, its role in inflammatory bowel diseases. © 2018 American Physiological Society. Compr Physiol 8:731-760, 2018.
哺乳动物质子偶联寡肽转运蛋白家族成员是整合膜蛋白，可介导二肽/三肽和肽类药物的细胞摄取，并将底物转运与 H 的运动偶联，跨膜电化学质子梯度提供驱动力。肽转运蛋白负责肠道和肾脏中膳食和/或细菌二肽和三肽的（再）吸收，并维持大脑中神经肽的体内平衡。这些蛋白还促进了许多具有重要药理学意义的化合物的吸收。在这篇综述文章中，我们提供了关于 PepT1（SLC15A1）、PepT2（SLC15A2）、PhT1（SLC15A4）和 PhT2（SLC15A3）的结构、功能、表达、定位和活性的最新信息。除了在健康和疾病中的意义外，还将肽转运蛋白，特别是 PepT1 作为药物传递系统进行了讨论。特别强调了 PepT1 在胃肠道生理学病理中的作用，特别是在炎症性肠病中的作用。美国生理学会 2018 年综合生理学 8:731-760。
