Department of Cardiology and Institute of Vascular Medicine, Peking University Third Hospital; Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides, Ministry of Health; Key Laboratory of Molecular Cardiovascular Sciences, Ministry of Education; Beijing Key Laboratory of Cardiovascular Receptors Research, Beijing, 100191, China.
Acta Pharmacol Sin. 2022 Mar;43(3):634-644. doi: 10.1038/s41401-021-00741-1. Epub 2021 Jul 30.
Transforming growth factor β (TGF-β) is a multifunctional polypeptide that plays critical roles in regulating a broad range of cellular functions and physiological processes. TGF-β signalling dysfunction contributes to many disorders, such as cardiovascular diseases, cancer and immunological diseases. The homoeostasis of negative feedback regulation is critical for signal robustness, duration and specificity, which precisely control physiological and pathophysiological processes. However, the underlying mechanism by which the negative regulation of TGF-β signalling is integrated and coordinated is still unclear. Here, we reveal that haematopoietic progenitor kinase-interacting protein of 55 kDa (HIP-55) was upregulated upon TGF-β stimulation, while the loss of HIP-55 caused TGF-β signalling overactivation and the abnormal accumulation of downstream extracellular matrix (ECM) genes. HIP-55 interacts with Smad7 and competes with Smad7/Axin complex formation to inhibit the Axin-mediated degradation of Smad7. HIP-55 further couples Smad7 to TβRI but not TβRII, driving TβRI degradation. Altogether, our findings demonstrate a new mechanism by which the effector and negative feedback functions of HIP-55 are coupled and may provide novel strategies for the treatment of TGF-β signalling-related human diseases.
转化生长因子β(TGF-β)是一种多功能多肽,在调节广泛的细胞功能和生理过程中起着关键作用。TGF-β信号功能障碍与许多疾病有关,如心血管疾病、癌症和免疫性疾病。负反馈调节的动态平衡对于信号的稳健性、持续时间和特异性至关重要,这些特性可以精确控制生理和病理生理过程。然而,TGF-β信号负调控如何整合和协调的潜在机制尚不清楚。在这里,我们揭示了造血祖细胞激酶相互作用蛋白 55kDa(HIP-55)在 TGF-β刺激下上调,而 HIP-55 的缺失导致 TGF-β信号过度激活和下游细胞外基质(ECM)基因的异常积累。HIP-55 与 Smad7 相互作用,并与 Smad7/Axin 复合物竞争,抑制 Axin 介导的 Smad7 降解。HIP-55 进一步将 Smad7 与 TβRI 偶联,但不与 TβRII 偶联,从而驱动 TβRI 的降解。总之,我们的研究结果表明了一种新的机制,即 HIP-55 的效应子和负反馈功能是偶联的,这可能为治疗与 TGF-β 信号相关的人类疾病提供新的策略。