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盘状结构域受体 1(DDR1)酪氨酸激酶在 PKD 肾脏中上调,但在多囊肾病的发病机制中不起作用。

Discoidin Domain Receptor 1 (DDR1) tyrosine kinase is upregulated in PKD kidneys but does not play a role in the pathogenesis of polycystic kidney disease.

机构信息

Division of Nephrology, New York University Langone Medical Center, New York, New York, United States of America.

Departments of Biochemistry and Molecular Pharmacology, New York University Langone Medical Center, New York, New York, United States of America.

出版信息

PLoS One. 2019 Jul 1;14(7):e0211670. doi: 10.1371/journal.pone.0211670. eCollection 2019.

Abstract

Tolvaptan is the only drug approved to slow cyst growth and preserve kidney function in patients with autosomal dominant polycystic kidney disease (ADPKD). However, its limited efficacy combined with significant side effects underscores the need to identify new and safe therapeutic drug targets to slow progression to end stage kidney disease. We identified Discoidin Domain Receptor 1 (DDR1) as receptor tyrosine kinase upregulated in vivo in 3 mouse models of ADPKD using a novel mass spectrometry approach to identify kinases upregulated in ADPKD. Previous studies demonstrating critical roles for DDR1 to cancer progression, its potential role in the pathogenesis of a variety of other kidney disease, along with the possibility that DDR1 could provide new insight into how extracellular matrix impacts cyst growth led us to study the role of DDR1 in ADPKD pathogenesis. However, genetic deletion of DDR1 using CRISPR/Cas9 failed to slow cyst growth or preserve kidney function in both a rapid and slow mouse model of ADPKD demonstrating that DDR1 does not play a role in PKD pathogenesis and is thus a not viable drug target. In spite of the negative results, our studies will be of interest to the nephrology community as it will prevent others from potentially conducting similar experiments on DDR1 and reinforces the potential of performing unbiased screens coupled with in vivo gene editing using CRISPR/Cas9 to rapidly identify and confirm new potential drug targets for ADPKD.

摘要

托伐普坦是唯一被批准用于减缓常染色体显性多囊肾病 (ADPKD) 患者囊肿生长并维持肾功能的药物。然而,其有限的疗效加上显著的副作用,突显了需要确定新的、安全的治疗药物靶点,以减缓进展为终末期肾病的速度。我们使用一种新的质谱方法来鉴定 ADPKD 中上调的激酶,在 3 种 ADPKD 小鼠模型中鉴定出盘状结构域受体 1 (DDR1) 作为受体酪氨酸激酶上调。先前的研究表明 DDR1 在癌症进展中的关键作用、其在多种其他肾脏疾病发病机制中的潜在作用,以及 DDR1 可能为了解细胞外基质如何影响囊肿生长提供新的见解,这些都促使我们研究 DDR1 在 ADPKD 发病机制中的作用。然而,使用 CRISPR/Cas9 对 DDR1 进行基因敲除未能减缓快速和慢速 ADPKD 小鼠模型中的囊肿生长或维持肾功能,这表明 DDR1 不在 PKD 发病机制中发挥作用,因此不是一个可行的药物靶点。尽管结果为阴性,但我们的研究将引起肾脏病学界的兴趣,因为它将阻止其他人可能对 DDR1 进行类似的实验,并加强使用 CRISPR/Cas9 进行无偏筛选结合体内基因编辑以快速鉴定和确认 ADPKD 新的潜在药物靶点的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63be/6602183/2a828838ca68/pone.0211670.g001.jpg

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