摘要
SUMO化修饰途径参与众多不同细胞功能的调节,内核及外核。所以,SUMO途径组件与各种疾病如囊性纤维化、肿瘤神经退行性有关就不奇怪了。因此,SUMO化修饰途径的组件应提供有效的治疗靶点。而相关泛素化系统包括大量的酶作为潜在的药物靶点,只有少数的部件组成了SUMO化级联。这就减轻了目标冗余的问题,它可能会使实现药物特异性的可能性复杂化。小分子抑制剂针对SUMO通路组件的开发是在其早期阶段。本文概述并总结了针对个别SUMO化修饰途径成分的药物研发工作,强调了CFTR蛋白处理可能会受到的影响。
关键词: SAE1/SAE2,Ubc9,SUMO E3,Hsp27,SUMO,SUMO肽酶,SUMO 相关修饰物
图形摘要
Current Drug Targets
Title:SUMOylation Modulates CFTR Biogenesis: Is the Pathway Druggable?
Volume: 16 Issue: 9
Author(s): Annette Ahner and Raymond A. Frizzell
Affiliation:
关键词: SAE1/SAE2,Ubc9,SUMO E3,Hsp27,SUMO,SUMO肽酶,SUMO 相关修饰物
摘要: The SUMOylation pathway is involved in the regulation of numerous and diverse cellular functions, nuclear as well as extra-nuclear. Thus, it is not surprising that SUMO pathway components are implicated in diseases as diverse as cystic fibrosis, cancer and neurodegenerative diseases. Therefore, the components of the SUMOylation pathway should provide valid therapeutic targets for manipulation. While the related ubiquitylation system encompasses a vast number of enzymes as potential drug targets, there are only a handful of components that comprise the SUMOylation cascade. Whereas this alleviates the problem of target redundancy, it may complicate the potential to achieve drug specificity. The development of small molecule inhibitors aimed at SUMO pathway components is in its early stages. This review provides an outline of the pathway and summarizes drug development efforts targeted at individual SUMOylation pathway components, with an emphasis on how CFTR protein processing may be affected.
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Cite this article as:
Annette Ahner and Raymond A. Frizzell , SUMOylation Modulates CFTR Biogenesis: Is the Pathway Druggable?, Current Drug Targets 2015; 16 (9) . https://dx.doi.org/10.2174/1389450116666150531152236
DOI https://dx.doi.org/10.2174/1389450116666150531152236 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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