acivicin

Acivicin is a modified amino acid and structural analog of glutamine, originally isolated as a fermentation product from Streptomyces sviceus. It functions primarily as an antimetabolite and glutamine antagonist, inhibiting several glutamate-dependent synthetic enzymes. Its main mechanism of action is the inhibition of gamma-glutamyl transferase (GGT) and other glutamine amidotransferases involved in purine and pyrimidine biosynthesis, thereby disrupting nucleotide synthesis essential for tumor cell proliferation. Acivicin also inhibits aldehyde dehydrogenase 4 family member A1 (ALDH4A1) by binding to its catalytic site, contributing to its cytotoxic effects in cancer cells. Although it demonstrated antitumor activity in preclinical studies and early clinical trials, further development was halted due to dose-limiting central nervous system toxicity observed in patients. Acivicin has also been studied for antiparasitic activity, including potential use against visceral leishmaniasis[1][2][3][5][6].

Other names

acivicine