Laboratory of Hereditary Kidney Diseases, Imagine Institute, Université Paris Cité, INSERM UMR 1163, Paris, France.
Medetia Pharmaceuticals, Imagine Institute, Paris, France.
Kidney Int. 2023 Aug;104(2):245-253. doi: 10.1016/j.kint.2023.04.027. Epub 2023 May 25.
Nephronophthisis is an autosomal recessive tubulointerstitial nephropathy, belonging to the ciliopathy disorders, characterized by fibrosis and/or cysts. It is the most common genetic cause of kidney failure in children and young adults. Clinically and genetically heterogeneous, it is caused by variants in ciliary genes, resulting in either an isolated kidney disease or syndromic forms in association with other manifestations of ciliopathy disorders. No curative treatment is currently available. Over the past 2 decades, advances in understanding disease mechanisms have identified several dysregulated signaling pathways, some shared with other cystic kidney diseases. Notably, molecules previously developed to target these pathways have shown promising beneficial effects in orthologous mouse models. In addition to these knowledge-based repurposing approaches, unbiased "in cellulo" phenotypic screens of "repurposing" libraries identified small molecules able to rescue the ciliogenesis defects observed in nephronophthisis conditions. Those compounds appeared to act on relevant pathways and, when tested, showed beneficial nephronophthisis-associated kidney and/or extrarenal defects in mice. In this review, we have summarized those studies that highlight the drug repurposing strategies in the context of a rare disorders, such as nephronophthisis-related ciliopathies, with broad genetic heterogeneity and systemic manifestations but with shared disease mechanisms.
肾单位肾痨是一种常染色体隐性肾小管间质性肾病,属于纤毛病,其特征为纤维化和/或囊肿。它是儿童和青年肾衰竭的最常见遗传原因。临床表现和遗传异质性,是由纤毛基因变异引起的,导致孤立性肾病或与纤毛病其他表现相关的综合征形式。目前尚无治愈方法。在过去的 20 年中,对疾病机制的认识的进步确定了几个失调的信号通路,其中一些与其他囊性肾病共享。值得注意的是,以前为靶向这些途径而开发的分子在同源小鼠模型中显示出有希望的有益效果。除了这些基于知识的重新利用方法外,“重新利用”文库的无偏“在细胞内”表型筛选还鉴定出能够挽救肾单位肾痨情况下观察到的纤毛发生缺陷的小分子。这些化合物似乎作用于相关途径,并且在测试时,在小鼠中显示出有益的与肾单位肾痨相关的肾脏和/或肾外缺陷。在这篇综述中,我们总结了那些强调药物再利用策略的研究,这些策略针对的是罕见疾病,如肾单位肾痨相关纤毛病,具有广泛的遗传异质性和全身表现,但具有共同的疾病机制。