5-重氮-4-氧代-L-正缬氨酸：具有生物学特异性的反应性天冬酰胺类似物。

5-Diazo-4-oxo-L-norvaline: reactive asparagine analog with biological specificity.

作者信息

Handschumacher R E, Bates C J, Chang P K, Andrews A T, Fischer G A

出版信息

Science. 1968 Jul 5;161(3836):62-3. doi: 10.1126/science.161.3836.62.

DOI:10.1126/science.161.3836.62

Abstract

The L-asparagine analog, 5-diazo-4-oxo-L-norvaline, specifically inactivates L-asparaginase and inhibits the growth of L-asparagine-dependent or L-asparaginase-sensitive tumor cells in culture. With 5-(14)C-labeled compound, a biphasic incorporation into sensitive cells occurs, but the inhibition of cell multiplication is manifest much later than the rapid phase of incorporation of the analog.

摘要

L-天冬酰胺类似物5-重氮-4-氧代-L-正缬氨酸能特异性地使天冬酰胺酶失活，并在培养中抑制依赖L-天冬酰胺或对天冬酰胺酶敏感的肿瘤细胞的生长。对于5-(14)C标记的化合物，会出现一个双相性地掺入敏感细胞的过程，但是细胞增殖的抑制比该类似物掺入的快速阶段要晚得多才表现出来。