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晶体结构的一个 BRAF 激酶结构域单体解释基础的别构调节。

Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation.

机构信息

1] Lunenfeld-Tanenbaum Research Institute, Mount Sinai Hospital, Toronto, Ontario, Canada. [2] Department of Biochemistry, University of Toronto, Toronto, Ontario, Canada.

Institute for Research in Immunology and Cancer, Université de Montréal, Montréal, Québec, Canada.

出版信息

Nat Struct Mol Biol. 2015 Jan;22(1):37-43. doi: 10.1038/nsmb.2924. Epub 2014 Dec 1.

Abstract

Reported RAF kinase domain structures adopt a side-to-side dimer configuration reflective of an 'on' state that underpins an allosteric mechanism of regulation. Atomic details of the monomer 'off' state have been elusive. Reinspection of the BRAF kinase domain structures revealed that sulfonamide inhibitors induce features of an off state, primarily a laterally displaced helix αC stabilized by the activation segment helix 1 (AS-H1). These features correlated with the ability of sulfonamides to disrupt human BRAF homodimers in cells, in vitro and in crystals yielding a structure of BRAF in a monomer state. The crystal structure revealed exaggerated, nonproductive positions of helix αC and AS-H1, the latter of which is the target of potent BRAF oncogenic mutations. Together, this work provides formal proof of an allosteric link between the RAF dimer interface, the activation segment and the catalytic infrastructure.

摘要

报道的 RAF 激酶结构域采用侧对侧二聚体构象,反映了一种“开启”状态,这种状态为别构调节机制提供了基础。单体“关闭”状态的原子细节一直难以捉摸。重新检查 BRAF 激酶结构域结构表明,磺酰胺抑制剂诱导出“关闭”状态的特征,主要是由激活片段螺旋 1(AS-H1)稳定的侧向位移螺旋 αC。这些特征与磺酰胺在细胞、体外和晶体中破坏人 BRAF 同源二聚体的能力相关,从而得到 BRAF 在单体状态下的结构。晶体结构显示出螺旋 αC 和 AS-H1 的夸张、非生产性位置,后者是强效 BRAF 致癌突变的靶点。总之,这项工作为 RAF 二聚体界面、激活片段和催化基础设施之间的别构联系提供了正式证据。

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