Inhibitors of L asparagine synthetase, in vitro

D. A. Cooney, J. S. Driscoll, H. A. Milman, H. N. Jayaram, R. D. Davis

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

A systematic search has been made for inhibitors of L asparagine synthetase (L glutamine hydrolyzing, EC 6.3.5.4) from leukemia 5178Y/AR, a rodent neoplasm resistant to the oncolytic enzyme L asparaginase (EC 3.5.1.1). 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 languageEnglish (US)
Pages (from-to)1493-1557
Number of pages65
JournalCancer Treatment Reports
Volume60
Issue number10
StatePublished - Dec 1 1976

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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    Cooney, D. A., Driscoll, J. S., Milman, H. A., Jayaram, H. N., & Davis, R. D. (1976). Inhibitors of L asparagine synthetase, in vitro. Cancer Treatment Reports, 60(10), 1493-1557.