Biochemical Pharmacology, Metabolism, and Mechanism of Action of L-Alanosine, a Novel, Natural Antitumor Agent

Publisher Summary This chapter discusses the biochemical pharmacology, metabolism, and mechanism of action of L-alanosine, a novel, natural antitumor agent. It must be admitted that the results so far obtained offer little encouragement that L-alanosine prove useful in the treatment of human cancer. Notwithstanding such presumptive inactivity, it does seem justified to capitalize on the leads offered by this unusual antibiotic in the design of second generation molecules with heightened potency, specificity, or even novel properties absent from the parent structure. Otherwise, the enormous investment of time and talent required to bring L-alanosine from culture medium to clinic might well be wasted. The most obvious such lead is chemical. Based on the studies with L-alanosine, the N-hydroxy-N-nitroso functionality is now established as a kind of surrogate carboxyl group, able to mimic its physiologic prototype with fidelity, both as to charge and geometry in space.