From the Departments of Gastroenterology, The University of Tokyo, Tokyo 113-8655, Japan.
the Departments of Medicine and Clinical Oncology, Graduate School of Medicine, Chiba University, Chiba 260-8677, Japan.
J Biol Chem. 2010 Feb 5;285(6):4185-4194. doi: 10.1074/jbc.M109.038232. Epub 2009 Dec 7.
Gli transcription factors are central effectors of Hedgehog signaling in development and tumorigenesis. Using a tandem affinity purification (TAP) strategy and mass spectrometry, we have found that Gli1 interacts with 14-3-3epsilon, and that Gli2 and Gli3 also bind to 14-3-3epsilon through homologous sites. This interaction depends on their phosphorylation, and cAMP-dependent protein kinase (PKA), a known negative regulator of Hedgehog signaling serves as a responsible kinase. A Gli2 mutant engineered to eliminate this interaction exhibited increased transcriptional activity (2 approximately 3x). Transcriptional repression by 14-3-3 binding was also observed with Gli3, when its N-terminal repressor domain was deleted. The phosphorylation sites responsible for the binding to 14-3-3 are distinct from those required for proteolysis, the known mechanism for PKA-induced repression of Hh signaling. Our data propose a novel mechanism in which PKA down-regulates Hedgehog signaling by promoting the interaction between Gli and 14-3-3 as well as proteolysis. Given the certain neuronal or malignant disorders in human caused by the abnormality of 17p13 encompassing 14-3-3epsilon overlap with increased Hh signaling, the Gli-14-3-3 interaction may have pathological significance for those human diseases.
转录因子是 Hedgehog 信号在发育和肿瘤发生中的核心效应物。我们使用串联亲和纯化(TAP)策略和质谱技术发现,Gli1 与 14-3-3epsilon 相互作用,而 Gli2 和 Gli3 也通过同源位点与 14-3-3epsilon 结合。这种相互作用依赖于它们的磷酸化,而环腺苷酸依赖性蛋白激酶(PKA),作为 Hedgehog 信号的已知负调控因子,充当负责的激酶。通过工程改造消除这种相互作用的 Gli2 突变体表现出增加的转录活性(2 倍左右)。当删除其 N 端抑制域时,也观察到 14-3-3 结合对 Gli3 的转录抑制。负责与 14-3-3 结合的磷酸化位点与已知的 PKA 诱导的 Hh 信号抑制所需的蛋白酶解位点不同。我们的数据提出了一种新的机制,其中 PKA 通过促进 Gli 与 14-3-3 的相互作用以及蛋白酶解来下调 Hedgehog 信号。鉴于人类由包含 14-3-3epsilon 的 17p13 异常引起的某些神经元或恶性疾病与增加的 Hh 信号重叠,Gli-14-3-3 相互作用可能对这些人类疾病具有病理意义。