EFFECTS OF HERBIMYCIN-A AND VARIOUS SH-REAGENTS ON P60V-SRC KINASE-ACTIVITY INVITRO

被引:49
作者
FUKAZAWA, H
MIZUNO, S
UEHARA, Y
机构
[1] Department of Antibiotics, National Institute of Health, Shinagawa-ku, Tokyo, 141
关键词
D O I
10.1016/S0006-291X(05)81053-8
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Herbimycin A is an antibiotic which reverses transformation caused by src family oncogenes. It inactivates p60v-src in vitro, possibly by binding to reactive SH-group(s) of the kinase. We examined effects of various SH-reagents on p60v-src and observed that N-[p-(2-benzimidazolyl)phenyl]maleimide (BIPM) or N-(9-acridinyl)maleimide (NAM) were potent inactivators of the kinase, whereas N-ethylmaleimide (NEM) required high concentrations, and iodoacetamide was totally ineffective in reducing the kinase activity. Pretreatment of p60v-src immune-complex with NEM and iodoacetamide, however, protected the kinase from inactivation by herbimycin A, BIPM, and NAM. The results suggest that SH-group(s) to which herbimycin A binds is not essential for the kinase activity, but is positioned in the vicinity of the active center. © 1990 Academic Press, Inc.
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页码:276 / 282
页数:7
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