Carrier mechanism and specificity accounting for the increase in intracellular melphalan by the basic amino acids
Vistica, D.T.; Schuette, B.P.
Molecular Pharmacology 19(1): 92-96
1981
ISSN/ISBN: 0026-895X PMID: 7207465 Document Number: 180660
The basic amino acids arginine and its lower homologue, .alpha.-amino-.gamma.-guanidinobutyric acid, increased [mouse leukemia L1210] intracellular melphalan levels only in the presence of leucine and Na+. This increase occurred solely through the monovalent cation-dependent, high-affinity, leucine-preferring transport system, 1 of the 2 amino acid transport systems responsible for melphalan uptake. Acceleration of melphalan exodus by leucine is antagonized by .alpha.-amino-.gamma.-guanidinobutyric acid, resulting in increased cellular retention of melphalan.