Encountering unpredicted off-target effects of pharmacological inhibitors

被引：16

作者：

Miyazawa, Keiji ^{[1
]}

机构：

[1] Univ Yamanashi, Dept Biochem, Interdisciplinary Grad Sch Med & Engn, Chuo Ku, Yamanashi 4093898, Japan

来源：

JOURNAL OF BIOCHEMISTRY | 2011年 / 150卷 / 01期

关键词：

Inhibitor; Kinase; JNK; off-target; PI3K; PROTEIN-KINASE INHIBITORS; TYROSINE KINASE; SP600125;

D O I：

10.1093/jb/mvr053

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：

With the emergence of chemical biology, the use of pharmacological inhibitors in biological research has been expanding. SP600125 is a low-molecular weight compound that has been widely used to inhibit c-Jun-N-terminal kinase (JNK). A recent publication by Tanemura et al. (J. Biochem. 145:345-354, 2009) indicated that SP600125 also inhibits phosphatidylinositol 3-kinase (PI3K) in an isoform-selective fashion: it efficiently inhibited the delta isoform of p110 catalytic subunit (p110 delta), which is primarily expressed in leucocytes, but neither of the ubiquitously expressed isoforms, p110 alpha and p110 gamma. Here, I discuss what we learn from such unpredicted off-target effects of pharmacological inhibitors.

引用

页码：1 / 3

页数：3

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