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We showed [Biochem. J. (1981) 194, 99-102] that inhibition of gamma-glutamyl transpeptidase in vivo with serine-borate decreases amino acid uptake by mammary gland. However, doubts arose about the validity of this inhibitor in metabolic studies because it must be used in very large amounts. New inhibitors have been isolated, like anthglutin and acivicin, which are effective at low concentrations in vivo. Here, we show that treatment of lactating rats with these substances decreases the transpeptidase activity and the amino acid uptake by the gland. These results support the hypothesis that the gamma-glutamyl cycle functions as an amino acid transport system in mammary gland.