Peptide transporter, renal

Lisinopril 20-40 mg p.o. qid Oral uptake likely via peptide transport, renal excretion... 

V Ganapathy, FH Leibach. (1990). Peptide transport in intestinal and renal brush border membrane vesicles. Life Sci 30 2137-2146. 

Leibach, F. H., Differential recognition of fl-lactam antibiotics by intestinal and renal peptide transporters, PEPT1 and PEPT2,... 

Doring, F., et al. Delta-aminolevulinic acid transport by intestinal and renal peptide transporters and its physiological and clinical implications. J. Clin. Invest. 1998, 101, 2761-2767. 

Ganapathy, M. E., et al. Valacyclovir a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2. Biochem. Biophys. Res. 

Daniel, H., and M. Herget. 1997. Cellular and molecular mechanisms of renal peptide transport. Am. J. Physiol. 273 Fl-8. 

Ganapathy ME, Prasad PD, Mackenzie B, Ganapathy V, Leibach FH. Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Biochim Biophys Acta 1997 1324(2) 296-308. 

Ganapathy, M.E., Brandsch, M., Prasad, P.D., Ganapathy, V. and Leibach, F.H. (1995) Differential recognition of b-lactam antibiotics by intestinal and renal peptide transporters, PEPT1 and PEPT2. Journal of Biological Chemistry, 270, 25672-25677. 

Doring, F., Walter, J., Will, J., Focking, M., Boll, M., Amasheh, S., Clauss, W. and Daniel, H. (1998) Delta-aminolevulinic add transport by intestinal and renal peptide transporters and its physiological and dinical implications. The Journal of Clinical Investigation, 101 (12), 2761-2767. 

Other important renal transport systems include the peptide transporters, which are involved in the uptake of peptide-like drugs including /3 -lactam antibiotics and angiotensin-converting enzyme inhibitors, and nucleoside transporter proteins, which are involved in uptake of nucleosides and nucleoside analogs (e.g., zidovudine and dideoxyinosine). ... 

Oral bioavailability of acyclovir (-10-30%) decreases with increasing dose. Valacyclovir is converted rapidly and virtually completely to acyclovir after oral administration. This conversion reflects first-pass intestinal and hepatic metabolism by enzymatic hydrolysis. Unlike acyclovir, valacyclovir is a substrate for intestinal and renal peptide transporters. The oral bioavailability of acyclovir increases to -70% following valacyclovir administration. Peak acyclovir concentrations occur -2 hours after dosing. Peak plasma concentrations of valacyclovir are only 4% of acyclovir levels. Less than 1% of an administered dose of valacyclovir is recovered in the urine, and most is eliminated as acyclovir. 

The availability of ALA at the cellular level has been improved by addition of, for example, DMSO (dimethyl sulfoxide) to topical formulations for increased tissue penetration [214,215] and by application of iontopheresis to induce reproducible levels of PpIX in normal skin [216]. It has been shown that ALA uses renal and intestinal peptide transporters for intracellular uptake [217]. High ALA-induced PpIX levels in intestinal epithelia suggest clinical relevance for this transport mechanism. 

Terada T, Saito H, Mukai M, Inui K-I (1997) Recognition of f3-lactam antibiotics by rat peptide transporter PEPTl and PEPT2, in LLC-PKl cells. Am J Physiol Renal Physiol 273 F706-F711. 

Chem., 270,2S 72 (1995). Differential Recognition of beta-Lactam Antibiotics by Intestinal and Renal Peptide Transporters, PEPT 1 and PEPT 2. 

Res. Commun., 246, 470 (1998). Valacyclovir A Substrate for the Intestinal and Renal Peptide Transporters PEPTl and PEPT2. 

Amino add reabsorption in the renal tubules Amino acids are small, easily filtered molecules. Efficient reabsorption mechanisms are vital to conserve amino acids which are metabolically valuable resources. Transport of individual amino acids and small peptides is symport carrier mediated mechanisms in which sodium is co-transported. The process is indirectly ATP dependent because Na is returned to the lumen of the nephron by the sodium pump , Na+/K+ dependent ATPase. 

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