Departments of Biochemistry and The University of Texas Health Science Center, San Antonio, Texas 78229.
Greehey Children's Cancer Research Institute, The University of Texas Health Science Center, San Antonio, Texas 78229; Department of Pediatrics and The University of Texas Health Science Center, San Antonio, Texas 78229.
J Biol Chem. 2012 May 18;287(21):17554-17567. doi: 10.1074/jbc.M111.319277. Epub 2012 Mar 30.
c-Jun N-terminal kinase (JNK) is a serine/threonine phosphotransferase whose sustained activation in response to genotoxic stress promotes apoptosis. In Drosophila, the normally rapid JNK-dependent apoptotic response to genotoxic stress is significantly delayed in Dmp53 (Drosophila p53) mutants. Likewise, the extent of JNK activity after UV irradiation is dependent on p53 in murine embryonic fibroblasts with loss of p53 resulting in diminished JNK activity. Together, these results suggest that p53 potentiates the JNK-dependent response to genotoxic stress; however, the mechanism whereby p53 stimulates JNK activity remains undefined. Here, we demonstrate that both Drosophila and human p53 can directly stimulate JNK activity independently of p53-dependent gene transcription. Furthermore, we demonstrate that both the Drosophila and human p53 orthologs form a physical complex with diphosphorylated JNK ((DP)JNK) both in vivo and in vitro, suggesting that the interaction is evolutionarily conserved. Focusing on human p53, we demonstrate that the interaction maps to the DNA binding domain (hp53(DBD)). Intriguingly, binding of p53(DBD) alone to (DP)JNK prevented its inactivation by MAPK phosphatase (MKP)-5; however, JNK was still able to phosphorylate c-Jun while in a complex with the p53(DBD). Apparent dissociation constants for the p53(DBD)·(DP)JNK (274 ± 14 nm) and MKP-5·(DP)JNK (55 ± 8 nm) complexes were established; however, binding of MKP-5 and p53 to JNK was not mutually exclusive. Together, these results suggest that stress-dependent increases in p53 levels potentiate JNK activation by preventing its rapid dephosphorylation by MKPs and that the simultaneous activation of p53 and JNK may constitute a "fail-safe" switch for the JNK-dependent apoptotic response.
c-Jun N-末端激酶(JNK)是一种丝氨酸/苏氨酸磷酸转移酶,其在应对遗传毒性应激时的持续激活促进细胞凋亡。在果蝇中,Dmp53(果蝇 p53)突变体中对遗传毒性应激的正常快速 JNK 依赖性凋亡反应明显延迟。同样,在 p53 缺失的鼠胚胎成纤维细胞中,紫外线照射后 JNK 活性的程度依赖于 p53,导致 JNK 活性降低。这些结果表明 p53 增强了 JNK 对遗传毒性应激的依赖性反应;然而,p53 刺激 JNK 活性的机制尚不清楚。在这里,我们证明果蝇和人类 p53 都可以直接刺激 JNK 活性,而不依赖于 p53 依赖性基因转录。此外,我们证明果蝇和人类 p53 同源物都可以在体内和体外与双磷酸化的 JNK((DP)JNK)形成物理复合物,表明这种相互作用是进化保守的。聚焦于人类 p53,我们证明该相互作用映射到 DNA 结合域(hp53(DBD))。有趣的是,p53(DBD) 与 (DP)JNK 的单独结合阻止了 MAPK 磷酸酶(MKP)-5 对其的失活;然而,JNK 仍然能够在与 p53(DBD) 形成复合物的同时磷酸化 c-Jun。确定了 p53(DBD)·(DP)JNK(274±14nm)和 MKP-5·(DP)JNK(55±8nm)复合物的表观解离常数;然而,MKP-5 和 p53 与 JNK 的结合并非相互排斥。综上所述,这些结果表明,应激诱导的 p53 水平增加通过防止 MKP 快速去磷酸化来增强 JNK 的激活,并且 p53 和 JNK 的同时激活可能构成 JNK 依赖性凋亡反应的“故障安全”开关。