Dorry Sam, Perla Sravan, Bennett Anton M
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, USA.
Yale Center for Molecular and Systems Metabolism, Yale University School of Medicine, New Haven, Connecticut, USA.
bioRxiv. 2024 Jun 27:2024.06.27.600976. doi: 10.1101/2024.06.27.600976.
Mitogen-activated protein kinase (MAPK) phosphatases (MKPs) constitute members of the dual-specificity family of protein phosphatases that dephosphorylate the MAPKs. MKP-5 dephosphorylates the stress-responsive MAPKs, p38 MAPK and JNK, and has been shown to promote tissue fibrosis. Here, we provide insight into how MKP-5 regulates the transforming growth factor-β (TGF-β) pathway, a well-established driver of fibrosis. We show that MKP-5-deficient fibroblasts in response to TGF-β are impaired in SMAD2 phosphorylation at canonical and non-canonical sites, nuclear translocation, and transcriptional activation of fibrogenic genes. Consistent with this, pharmacological inhibition of MKP-5 is sufficient to block TGF-β signaling, and that this regulation occurs through a JNK-dependent pathway. By utilizing RNA sequencing and transcriptomic analysis, we identify TGF-β signaling activators regulated by MKP-5 in a JNK-dependent manner, providing mechanistic insight into how MKP-5 promotes TGF-β signaling. This study elucidates a novel mechanism whereby MKP-5-mediated JNK inactivation is required for TGF-β signaling and provides insight into the role of MKP-5 in fibrosis.
丝裂原活化蛋白激酶(MAPK)磷酸酶(MKPs)是双特异性蛋白磷酸酶家族的成员,可使MAPKs去磷酸化。MKP-5可使应激反应性MAPKs、p38 MAPK和JNK去磷酸化,并已被证明可促进组织纤维化。在此,我们深入探讨了MKP-5如何调节转化生长因子-β(TGF-β)信号通路,这是一种公认的纤维化驱动因素。我们发现,对TGF-β产生反应的MKP-5缺陷型成纤维细胞在SMAD2的经典和非经典位点的磷酸化、核转位以及纤维化基因的转录激活方面均受损。与此一致的是,MKP-5的药理学抑制足以阻断TGF-β信号传导,并且这种调节是通过JNK依赖性途径发生的。通过利用RNA测序和转录组分析,我们鉴定出由MKP-5以JNK依赖性方式调节的TGF-β信号激活剂,从而为MKP-5如何促进TGF-β信号传导提供了机制性见解。这项研究阐明了一种新机制,即MKP-5介导的JNK失活是TGF-β信号传导所必需的,并为MKP-5在纤维化中的作用提供了见解。