Inhibition of L asparagine synthetase by a new amino acid antibiotic with antitumor activity: L (αS,5S) α amino 3 chloro 4,5 dihydro 5 isoxazoleacetic acid (NSC-163501)

D. A. Cooney, H. N. Jayaram, J. A. Ryan, V. H. Bono

Research output: Chapter in Book/Report/Conference proceedingChapter

27 Citations (Scopus)

Abstract

NSC 163501 and its hydroxy analog (αS,4S,5R) α amino 3 chloro 4 hydroxy 4,5 dihydro 5 isoxazoleacetic acid (NSC 176324) are powerful inhibitors of the utilization of L glutamine by L asparagine synthetase both in vitro and in vivo. The type of inhibition produced in vitro is concluded to be apparently competitive on the basis of graphic analysis. L glutamine in large molar excess effectively antagonizes inhibition produced by these agents; however, established inhibition is concluded to be irreversible on the basis of dialysis experiments. Attempts to demonstrate alteration of the inhibitor molecule in the act of catalysis were unsuccessful.

Original languageEnglish (US)
Title of host publicationCANCER CHEMOTHER.REP.
Pages793-802
Number of pages10
Volume58
Edition6
StatePublished - 1974
Externally publishedYes

Fingerprint

acivicin
Aspartate-Ammonia Ligase
U 43795
Asparagine
Glutamine
Anti-Bacterial Agents
Amino Acids
Acids
Catalysis
Dialysis
In Vitro Techniques

ASJC Scopus subject areas

  • Medicine(all)

Cite this

Cooney, D. A., Jayaram, H. N., Ryan, J. A., & Bono, V. H. (1974). Inhibition of L asparagine synthetase by a new amino acid antibiotic with antitumor activity: L (αS,5S) α amino 3 chloro 4,5 dihydro 5 isoxazoleacetic acid (NSC-163501). In CANCER CHEMOTHER.REP. (6 ed., Vol. 58, pp. 793-802)

Inhibition of L asparagine synthetase by a new amino acid antibiotic with antitumor activity : L (αS,5S) α amino 3 chloro 4,5 dihydro 5 isoxazoleacetic acid (NSC-163501). / Cooney, D. A.; Jayaram, H. N.; Ryan, J. A.; Bono, V. H.

CANCER CHEMOTHER.REP.. Vol. 58 6. ed. 1974. p. 793-802.

Research output: Chapter in Book/Report/Conference proceedingChapter

Cooney, D. A. ; Jayaram, H. N. ; Ryan, J. A. ; Bono, V. H. / Inhibition of L asparagine synthetase by a new amino acid antibiotic with antitumor activity : L (αS,5S) α amino 3 chloro 4,5 dihydro 5 isoxazoleacetic acid (NSC-163501). CANCER CHEMOTHER.REP.. Vol. 58 6. ed. 1974. pp. 793-802
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