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PEPT2

Molecular structure and tissue distribution
Peptide transporter 2 (SLC15A2) as a predominant high-affinity, low-capacity renal peptide transporter is located in S2- and S3-segment of proximal tubule cells, although expression has also been observed in neurons, astrocytes, choroid plexus epithelial cells, bronchial epithelial cells, Alveolar pneumocytes, mammary gland and spleen. Human PEPT2 consists of 729 amino acids..

Interaction of hPEPT2 with endogenous compounds and drugs
PEPT2 operates as H+-coupled symporter of di- and tripeptides. PEPT2 reabsorbs renally filtered drugs from tubular fluid into proximal tubules, thereby affecting the systemic pharmacokinetics of several drugs. Substrates of PEPT2 include many important drug classes, including antivirals, β-lactam antibiotics, and angiotensin-converting enzyme (ACE) inhibitors. One of the most commonly used reference substrates of the H+/peptide cotransporter is also glycylsarcosine (Gly-Sar). PEPT2 possess tenfold higher affinity for Gly-Sar than PEPT1. Uptake of Gly-Sar by PEPT2 can be inhibited with losartan, kyotorphin, carnosine and cefaclor. In choroid plexus epithelial cells PEPT2 functions as efflux transporter and probably is involved in translocation as well as in optimizing the neuropeptide level in brain. Meanwhile, is known that PEPT1 and PEPT2 interact with most but not all proteinogenic dipeptide (400) and tripeptide (8000).

 

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