Department of Cell and Chemical Biology, Leiden University Medical Center, Oncode Institute, Leiden, The Netherlands.
Department of Cell and Chemical Biology, Leiden University Medical Center, Leiden, The Netherlands.
J Pathol. 2021 Nov;255(3):330-342. doi: 10.1002/path.5774. Epub 2021 Sep 6.
Chondrocytes in mice developing osteoarthritis (OA) exhibit an aberrant response to the secreted cytokine transforming growth factor (TGF)-β, consisting in a potentiation of intracellular signaling downstream of the transmembrane type I receptor kinase activin receptor-like kinase (ALK)1 against canonical TGF-β receptor ALK5-mediated signaling. Unfortunately, the underlying mechanisms remain elusive. In order to identify novel druggable targets for OA, we aimed to investigate novel molecules regulating the ALK1/ALK5 balance in OA chondrocytes. We performed gene expression analysis of TGF-β signaling modulators in joints from three different mouse models of OA and found an upregulated expression of the TGF-β co-receptor Cripto (Tdgf1), which was validated in murine and human cartilage OA samples at the protein level. In vitro and ex vivo, elevated expression of Cripto favors the hypertrophic differentiation of chondrocytes, eventually contributing to tissue calcification. Furthermore, we found that Cripto participates in a TGF-β-ALK1-Cripto receptor complex in the plasma membrane, thereby inducing catabolic SMAD1/5 signaling in chondrocytes. In conclusion, we demonstrate that Cripto is expressed in OA and plays a functional role promoting chondrocyte hypertrophy, thereby becoming a novel potential therapeutic target in OA, for which there is no efficient cure or validated biomarker. © 2021 The Authors. The Journal of Pathology published by John Wiley & Sons, Ltd. on behalf of The Pathological Society of Great Britain and Ireland.
在发生骨关节炎 (OA) 的小鼠中,软骨细胞对细胞因子转化生长因子 (TGF)-β的分泌表现出异常反应,这包括激活素受体样激酶 (ALK)1 跨膜型 I 受体激酶下游细胞内信号的增强,而这种信号是由经典 TGF-β受体 ALK5 介导的。不幸的是,其潜在机制仍不清楚。为了确定 OA 的新的可治疗靶点,我们旨在研究调节 OA 软骨细胞中 ALK1/ALK5 平衡的新分子。我们对三种不同的 OA 小鼠模型关节中的 TGF-β信号转导调节剂进行了基因表达分析,发现 TGF-β共受体 Cripto(Tdgf1)的表达上调,在鼠类和人类软骨 OA 样本中进行蛋白水平验证。在体外和离体,Cripto 的表达升高有利于软骨细胞的肥大分化,最终导致组织钙化。此外,我们发现 Cripto 参与质膜中的 TGF-β-ALK1-Cripto 受体复合物,从而在软骨细胞中诱导分解代谢 SMAD1/5 信号。总之,我们证明 Cripto 在 OA 中表达,并发挥促进软骨细胞肥大的功能作用,因此成为 OA 的一种新的潜在治疗靶点,而 OA 目前尚无有效的治疗方法或经过验证的生物标志物。© 2021 作者。The Journal of Pathology 由 John Wiley & Sons,Ltd. 代表英国和爱尔兰的病理学会出版。