Pediatric Diabetes Research Center, University of California, San Diego, School of Medicine, La Jolla, California 92037, USA.
J Biol Chem. 2013 Jan 25;288(4):2428-40. doi: 10.1074/jbc.M112.425884. Epub 2012 Nov 21.
The mixed lineage kinase MLK3 plays a crucial role in compromising mitochondrial integrity and functions as a proapoptotic competence factor in the early stages of cytokine-induced pancreatic β cell death. In an effort to identify mechanisms that regulate MLK3 activity in β cells, we discovered that IL-1β stimulates Lys-63-linked ubiquitination of MLK3 via a conserved, TRAF6-binding peptapeptide motif in the catalytic domain of the kinase. TRAF6-mediated ubiquitination was required for dissociation of inactive monomeric MLK3 from the scaffold protein IB1/JIP1, facilitating the subsequent dimerization, autophosphorylation, and catalytic activation of MLK3. Inability to ubiquitinate MLK3, or the presence of A20, an upstream Lys-63-linked deubiquitinase, strongly curtailed the ability of MLK3 to affect the proapoptotic translocation of BAX in cytokine-stimulated pancreatic β cells, an early step in the progression toward β cell death. These studies suggest a novel mechanism for MLK3 activation and provide new clues for therapeutic intervention in promoting β cell survival.
混合谱系激酶 MLK3 在损害线粒体完整性方面发挥着关键作用,并作为细胞因子诱导的胰岛β细胞死亡早期的促凋亡效应因子发挥作用。为了鉴定调控β细胞中 MLK3 活性的机制,我们发现 IL-1β 通过激酶催化结构域中的保守 TRAF6 结合肽段基序刺激 MLK3 的 Lys-63 连接泛素化。TRAF6 介导的泛素化对于无活性单体 MLK3 从支架蛋白 IB1/JIP1 上的解离是必需的,从而促进随后的二聚化、自磷酸化和 MLK3 的催化激活。MLK3 不能泛素化,或存在 A20(一种上游 Lys-63 连接去泛素化酶),强烈限制了 MLK3 影响细胞因子刺激的胰岛β细胞中 BAX 促凋亡易位的能力,这是β细胞死亡进展的早期步骤。这些研究为 MLK3 的激活提供了一种新的机制,并为促进β细胞存活的治疗干预提供了新的线索。