Zhai Dayong, Ke Ning, Zhang Haichao, Ladror Uri, Joseph Mary, Eichinger Andreas, Godzik Adam, Ng Shi-Chung, Reed John C
The Burnham Institute, La Jolla, CA 92037, USA.
Biochem J. 2003 Nov 15;376(Pt 1):229-36. doi: 10.1042/BJ20030374.
Bcl-B protein is an anti-apoptotic member of the Bcl-2 family protein that contains all the four BH (Bcl-2 homology) domains (BH1, BH2, BH3 and BH4) and a predicted C-terminal transmembrane domain. Our previous results showed that Bcl-B binds Bax and suppresses apoptosis induced by over-expression of Bax; however, Bcl-B does not bind or suppress Bak. To explore the molecular basis for the differential binding and suppression of Bax and Bak, we studied the BH3 dimerization domains of Bax and Bak. Chimeric mutants of Bax and Bak were generated that swapped the BH3 domains of these pro-apoptotic proteins. Bcl-B associated with and blocked apoptosis induced by mutant Bak containing the BH3 domain of Bax, but not mutant Bax containing the BH3 domain of Bak. In contrast, Bcl-X(L) protein bound and suppressed apoptosis induction by Bax, Bak and both BH3-domain chimeras. A strong correlation between binding and apoptosis suppression was also obtained using a series of alanine substitutions spanning the length of the Bax BH3 domain to identify critical residues for Bcl-B binding. Conversely, using structure-based modelling to design mutations in the BH3-binding pocket of Bcl-B, we produced two Bcl-B mutants (Leu86-->Ala and Arg96-->Gln) that failed to bind Bax and that also were unable to suppress apoptosis induced by Bax over-expression. In contrast, other Bcl-B mutants that still bound Bax retained protective activity against Bax-induced cell death, thus serving as a control. We conclude that, in contrast with some other anti-apoptotic Bcl-2-family proteins, a strong correlation exists for Bcl-B between binding to pro-apoptotic multidomain Bcl-2 family proteins and functional apoptosis suppression.
Bcl-B蛋白是Bcl-2家族蛋白中的一种抗凋亡成员,它包含所有四个BH(Bcl-2同源)结构域(BH1、BH2、BH3和BH4)以及一个预测的C末端跨膜结构域。我们之前的结果表明,Bcl-B与Bax结合并抑制由Bax过表达诱导的细胞凋亡;然而,Bcl-B不与Bak结合或抑制其活性。为了探究Bcl-B对Bax和Bak的差异性结合及抑制作用的分子基础,我们研究了Bax和Bak的BH3二聚化结构域。构建了Bax和Bak的嵌合突变体,将这些促凋亡蛋白的BH3结构域进行了交换。Bcl-B与含有Bax的BH3结构域的突变型Bak结合,并阻断其诱导的细胞凋亡,但不与含有Bak的BH3结构域的突变型Bax结合。相反,Bcl-X(L)蛋白与Bax、Bak以及两种BH3结构域嵌合体结合并抑制它们诱导的细胞凋亡。通过对Bax BH3结构域全长进行一系列丙氨酸取代以确定Bcl-B结合的关键残基,也得到了结合与凋亡抑制之间的强相关性。相反,利用基于结构的建模方法在Bcl-B的BH3结合口袋中设计突变,我们产生了两个Bcl-B突变体(Leu86→Ala和Arg96→Gln),它们无法与Bax结合,也不能抑制由Bax过表达诱导的细胞凋亡。相比之下,其他仍能与Bax结合的Bcl-B突变体保留了对Bax诱导的细胞死亡的保护活性,从而作为对照。我们得出结论,与其他一些抗凋亡的Bcl-2家族蛋白不同,Bcl-B在与促凋亡的多结构域Bcl-2家族蛋白结合和功能性凋亡抑制之间存在强相关性。