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在2.3A分辨率下,MAP激酶ERK2的原子结构为2.3A

F Zhang¹, A Strand, D Robbins

¹Department of Biochemistry, University of Texas Southwestern Medical Center at Dallas.

|February 24, 1994

概括

确定了米托基激活蛋白 (MAP) 激酶ERK2在非活性状态下的结构. 这揭示了全球和地方的结构变化对ERK2激活至关重要.

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:

线素激活蛋白 (MAP) 激酶ERK2是细胞信号通路中的关键酶.
ERK2由Ras和Raf等上游激酶调节,是各种疾病的目标.
了解ERK2的结构对于理解其激活机制和药物开发至关重要.

研究的目的:

阐明ERK2低活性构造的结构基础.
为ERK2激活所需的结构变化提供见解.
确定ERK2活动调节的潜在目标.

主要方法:

使用X射线晶体学来确定ERK2.2的三维结构.
该结构的分辨率为2.3安格斯特罗姆.
进行了与活性激酶构成的比较结构分析.

主要成果:

解决了ERK2的非酸化,低活性构造.
与活跃的cAMP依赖蛋白激酶相比,非活跃的ERK2的两个域更加分离.
不活跃的ERK2中的结位被氨酸185.5阻塞.

结论:

ERK2激活可能涉及重大全球和本地形状重组.
铁素185在维持ERK2.2的非活性状态方面发挥着至关重要的作用.
解决的结构为理解ERK2调节和设计抑制剂提供了基础.

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