A systematic search has been made for inhibitors of L asparagine synthetase (L glutamine hydrolyzing, EC 126.96.36.199) from leukemia 5178Y/AR, a rodent neoplasm resistant to the oncolytic enzyme L asparaginase (EC 188.8.131.52). The classes of chemicals examined in this search included substrate and product analogs, agents capable of reacting with sulfhydryl functions, and a variety of modifiers whose mechanism of interaction with proteins is known. In general, antagonists of L glutamine and thiol reagents proved to be the most effective inhibitors of L asparagine synthetase from this tumor source. Within these groups, certain structural prerequisites to inhibition are reported. Attempts to correlate oncolytic potency with enzyme inhibitory potency were unsuccessful.
|Original language||English (US)|
|Number of pages||65|
|Journal||Cancer Treatment Reports|
|State||Published - Dec 1 1976|
ASJC Scopus subject areas
- Cancer Research