蛋白激酶C三角酶的cys2激活剂结合域的晶体结构与醇 Ester 复合在一起
G Zhang1, M G Kazanietz, P M Blumberg
1Laboratory of Molecular Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0580, USA.
蛋白激酶Cs (PKCs) 是由醇激活的酶. 结构分析显示,醇结合会产生一种疏水的表面,促进PKC delta的膜插入.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 结构生物学 结构生物学
背景情况:
- 蛋白激酶Cs (PKCs) 是关键的调节酶,参与细胞信号传递.
- PKCs与细胞膜结合,并由二甲糖醇或促进瘤的化合物,如博 Ester 激活.
研究的目的:
- 为了阐明PKC三角激活由醇的结构基础.
- 了解激活剂结合如何影响膜协会.
主要方法:
- 使用X射线结晶学来确定PKC三角激活剂结合域的结构.
- 结构在复合中与博酸13-乙酸确定.
主要成果:
- 博13-乙酸结合在一个由两个β链在域的尖端形成的槽内.
- 特定的醇氧基因与保留的主链组形成键.
- 激活剂结合导致连续的疏水表面,覆盖域的很大一部分.
结论:
- 结构数据解释了博 Ester 结合如何促进 PKC delta 插入细胞膜.
- 了解这种机制可以了解PKC调节和信号通路.
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