Gentry Leanna R, Nishimura Akiyuki, Cox Adrienne D, Martin Timothy D, Tsygankov Denis, Nishida Motohiro, Elston Timothy C, Der Channing J
From the Departments of Pharmacology and.
the Division of Cardiocirculatory Signaling, Okazaki Institute for Integrative Bioscience (National Institute for Physiological Sciences), National Institutes of Natural Sciences, 5-1 Higashiyama, Myoudaiji-cho, Okazaki, Aichi 444-8787, Japan.
J Biol Chem. 2015 Sep 11;290(37):22851-61. doi: 10.1074/jbc.M115.656710. Epub 2015 Jul 27.
The Ras-like small GTPases RalA and RalB are well validated effectors of RAS oncogene-driven human cancer growth, and pharmacologic inhibitors of Ral function may provide an effective anti-Ras therapeutic strategy. Intriguingly, although RalA and RalB share strong overall amino acid sequence identity, exhibit essentially identical structural and biochemical properties, and can utilize the same downstream effectors, they also exhibit divergent and sometimes opposing roles in the tumorigenic and metastatic growth of different cancer types. These distinct biological functions have been attributed largely to sequence divergence in their carboxyl-terminal hypervariable regions. However, the role of posttranslational modifications signaled by the hypervariable region carboxyl-terminal tetrapeptide CAAX motif (C = cysteine, A = aliphatic amino acid, X = terminal residue) in Ral isoform-selective functions has not been addressed. We determined that these modifications have distinct roles and consequences. Both RalA and RalB require Ras converting CAAX endopeptidase 1 (RCE1) for association with the plasma membrane, albeit not with endomembranes, and loss of RCE1 caused mislocalization as well as sustained activation of both RalA and RalB. In contrast, isoprenylcysteine carboxylmethyltransferase (ICMT) deficiency disrupted plasma membrane localization only of RalB, whereas RalA depended on ICMT for efficient endosomal localization. Furthermore, the absence of ICMT increased stability of RalB but not RalA protein. Finally, palmitoylation was critical for subcellular localization of RalB but not RalA. In summary, we have identified striking isoform-specific consequences of distinct CAAX-signaled posttranslational modifications that contribute to the divergent subcellular localization and activity of RalA and RalB.
类Ras小GTP酶RalA和RalB是RAS致癌基因驱动的人类癌症生长的经过充分验证的效应器,Ral功能的药理抑制剂可能提供一种有效的抗Ras治疗策略。有趣的是,尽管RalA和RalB在整体氨基酸序列上有很强的一致性,表现出基本相同的结构和生化特性,并且可以利用相同的下游效应器,但它们在不同癌症类型的致瘤性和转移性生长中也表现出不同甚至有时相反的作用。这些不同的生物学功能很大程度上归因于它们羧基末端高变区的序列差异。然而,高变区羧基末端四肽CAAX基序(C = 半胱氨酸,A = 脂肪族氨基酸,X = 末端残基)所引发的翻译后修饰在Ral亚型选择性功能中的作用尚未得到研究。我们确定这些修饰具有不同的作用和后果。RalA和RalB都需要Ras转换CAAX内肽酶1(RCE1)才能与质膜结合,尽管不是与内膜结合,RCE1的缺失会导致RalA和RalB的定位错误以及持续激活。相比之下,异戊二烯基半胱氨酸羧基甲基转移酶(ICMT)缺乏仅破坏了RalB的质膜定位,而RalA依赖ICMT进行有效的内体定位。此外,ICMT的缺失增加了RalB而非RalA蛋白的稳定性。最后,棕榈酰化对RalB的亚细胞定位至关重要,但对RalA并非如此。总之,我们已经确定了不同的CAAX信号翻译后修饰所产生的显著亚型特异性后果,这些后果导致了RalA和RalB不同的亚细胞定位和活性。