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PEPT1 and PEPT2 are H+-coupled peptide transporters expressed preferentially in the intestine and kidney, respectively, which mediate uphill transport of oligopeptides and peptide-like drugs such as ƒÀ-lactam antibiotics. In the present study, we have compared the recognition of ƒÀ-lactam antibiotics by LLC-PK, cells stably transfected with rat PEPT1 or PEPT2 cDNA. Among the examined drugs, cyclacillin (aminopenicillin) and cefadroxil (aminocephalosporin) showed the most potent inhibitory effects on glycylsarcosine uptake in PEPT1and PEPT2-expressing cells, respectively. Comparison of the Ki values of ƒÀ-lactam antibiotics between PEPT1 and PEPT2-expressing cells suggested that PEPT2 had a much higher affinity for ƒÀ-lactam antibiotics with an ƒ¿-amino group. We have examined interactions of ƒÀ-lactam antibiotics with rat renal brush-border membrane vesicles, in which PEPT1 and PEPT2 appeared to be coexpressed. The apparent Ki values of the antibiotics for glycylsarcosine transport were closely correlated with those in the PEPT2-expressing cells, suggesting that ƒÀ-lactam antibiotics interact predominantly with PEPT2 rather than PEPT1 in renal brush-border membranes. In conclusion, 1) PEPTI and PEPT2 show different recognitions of ƒÀ-lactam antibiotics, and 2) ƒÀ-lactam antibiotics predominantly interact with renal PEPT2 at pharmacological concentrations. REFERENCES (1) T. Okano et al., J. Biol. Chem., 261, 14130 (1986)(2) K. Inui et al., J. Pharmacol. Exp. Ther., 261,195 (1992)(3) S. Matsumoto et al., J. Pharmacol. Exp. Ther., 270,498 (1994)(4) H. Saito et al., J. Pharmacol. Exp. Ther., 275, 1631 (1995)(5) H. Saito et al., Biochim. Biophys. Acta, 1280, 173 (1996)(6) H. Ogihara et al., Biochem. Biophys. Res. Commun., 220, 848 (1996)(7) T. Terada et al., J. Pharmacol. Exp. Ther., 281, 1415 (1997)(8) T. Terada et al., Am. J. Physiol., in press (9) T. Terada et al., FEBS Lett., 394,196 (1996)

OLECULAR AND CELL BIOLOGICAL ANALYSES OF DRUG RECOGNITION BY RAT PEPTIDE TRANSPORTERS