ISSN:
1432-0584
Keywords:
PTT-119
;
Alkylating agents
;
Melphalan
;
Drug resistance
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary PTT-119 is an antineoplastic agent in which an alkylating moiety, m-sarcolysine, is linked to two amino acid analogs. Previous studies showed a higher “in vitro” cytotoxicity of PTT-119 when compared to free m-sarcolysine; the mechanisms of this enhanced activity are not completely understood. In this study we incubated peripheral blood cells from 8 chronic lymphocytic leukemia patients with both m-sarcolysine and equimolar concentrations of PTT-119, measuring the intracellular concentration of the alkylating moiety. We observed a significantly higher intracellular concentration of m-sarcolysine in cells incubated with the peptide-bound drug than with the free drug (58.3 ± 39.6 versus 4.4 ± 1.9 ng/106 cells;P = 0.013). This observation could explain the higher cytotoxic activity of PTT-119 and the lack of cross-resistance with melphalan.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01732884
Permalink