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非必需半胱氨酸的突变表明,NF-κB 必需调节剂形成组成型非共价二聚体,与 IκB 激酶-β 高亲和力结合。

Mutation of nonessential cysteines shows that the NF-κB essential modulator forms a constitutive noncovalent dimer that binds IκB kinase-β with high affinity.

机构信息

Department of Chemistry and ‡Department of Biology, Boston University , Boston, Massachusetts 02215, United States.

出版信息

Biochemistry. 2013 Dec 23;52(51):9141-54. doi: 10.1021/bi401368r. Epub 2013 Dec 10.

Abstract

NEMO (NF-κB essential modulator) associates with catalytic subunits IKKα and IKKβ to form the IκB kinase (IKK) complex and is a key regulator of NF-κB pathway signaling. Biochemical and structural characterization of NEMO has been challenging, however, leading to conflicting data about basic biochemical properties such as the oligomeric state of active NEMO and its binding affinity for IKKβ. We show that up to seven of NEMO's 11 cysteine residues can be mutated to generate recombinant full-length NEMO that is highly soluble and active. Using a fluorescence anisotropy binding assay, we show that full-length NEMO binds a 44-mer peptide encompassing residues 701-745 of IKKβ with a K(D) of 2.2 ± 0.8 nM. The IKKβ binding affinities of mutants with five and seven Cys-to-Ala substitutions are indistinguishable from that of wild-type NEMO. Moreover, when expressed in NEMO -/- fibroblasts, the five-Ala and seven-Ala NEMO mutants can interact with cellular IKKβ and restore NF-κB signaling to provide protection against tumor necrosis factor α-induced cell death. Treatment of the NEMO-reconstituted cells with H₂O₂ led to the formation of covalent dimers for wild-type NEMO and the five-Ala mutant, but not for the seven-Ala mutant, confirming that Cys54 and/or Cys347 can mediate interchain disulfide bonding. However, the IKKβ binding affinity of NEMO is unaffected by the presence or absence of interchain disulfide bonding at Cys54, which lies within the IKKβ binding domain of NEMO, or at Cys347, indicating that NEMO exists as a noncovalent dimer independent of the redox state of its cysteines. This conclusion was corroborated by the observation that the secondary structure content of NEMO and its thermal stability were independent of the presence or absence of interchain disulfide bonds.

摘要

NEMO(NF-κB 必需调节剂)与催化亚基 IKKα 和 IKKβ 结合形成 IκB 激酶(IKK)复合物,是 NF-κB 途径信号转导的关键调节剂。然而,NEMO 的生化和结构特征分析具有挑战性,导致关于其基本生化特性的相互矛盾的数据,例如活性 NEMO 的寡聚状态及其与 IKKβ 的结合亲和力。我们表明,多达 NEMO 的 11 个半胱氨酸残基中的 7 个可以突变以产生高可溶性和活性的重组全长 NEMO。使用荧光各向异性结合测定法,我们表明全长 NEMO 以 2.2±0.8 nM 的 K(D)结合包含 IKKβ 残基 701-745 的 44 个残基肽。具有五个和七个 Cys-to-Ala 取代的 IKKβ 结合亲和力与野生型 NEMO 无法区分。此外,当在 NEMO -/-成纤维细胞中表达时,五个-Ala 和七个-Ala NEMO 突变体可以与细胞 IKKβ 相互作用并恢复 NF-κB 信号转导以提供对肿瘤坏死因子 α 诱导的细胞死亡的保护。用 H₂O₂处理 NEMO 重建的细胞导致野生型 NEMO 和五个-Ala 突变体形成共价二聚体,但七个-Ala 突变体没有,这证实了 Cys54 和/或 Cys347 可以介导链间二硫键形成。然而,IKKβ 结合亲和力不受 NEMO 中 Cys54 或 Cys347 处链间二硫键形成的存在或不存在的影响,Cys54 位于 NEMO 的 IKKβ 结合域内,Cys347 表明 NEMO 作为非共价二聚体存在,独立于其半胱氨酸的氧化还原状态。这一结论得到了以下观察结果的证实,即 NEMO 的二级结构含量及其热稳定性不受链间二硫键存在与否的影响。

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