异肽酶抑制剂NSC632839靶向前列腺癌细胞

0 UROLOGY & NEPHROLOGY
Ummuhan Demir, Rabia Erdogdu
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引用次数: 0

摘要

目的:蛋白质翻译后修饰对蛋白质功能的微调至关重要。NSC632839是一种双重去泛素化和去氧基化抑制剂。去氧基化酶SENP2是NSC632839的靶标之一。本研究旨在评估NSC632839在前列腺癌(PCa)中的抗增殖作用。方法:采用结晶紫染色法测定NSC632839在PCa细胞系PC3、LNCaP和正常成纤维细胞CCD-1072Sk中的IC50值。通过二维集落形成实验评估NSC632839处理后PC3和LNCaP细胞的集落形成能力。利用公开数据集研究了SENP2的表达水平及其与雄激素受体(AR)的相关性。结果:NSC632839对LNCaP、PC3和CCD- 1072Sk的IC50值分别为3.1、1.9和17.7。在此IC50浓度下,NSC632839完全破坏了PC3细胞的集落形成能力。SENP2在转移性PCa组织样本中的表达水平升高,且与AR相关。结论:NSC632839在低剂量下对PCa细胞具有抗增殖作用。因此,NSC632839是一个需要进一步研究的强有力的候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Targeting Prostate Cancer Cells by an Isopeptidase Inhibitor NSC632839.

Objective: Posttranslational protein modifications are crucial for fine-tuning protein function. NSC632839 is a dual deubiquitination and desumoylation inhibitor. The desumoylation enzyme SENP2 is one of the targets of NSC632839. This study aimed to evaluate NSC632839 as an antiproliferative agent in prostate cancer (PCa). Methods: The IC50 values for NSC632839 were determined in PCa cell lines PC3 and LNCaP and normal fibroblast cells CCD-1072Sk by crystal violet staining. The colony- formation ability of PC3 and LNCaP cells upon NSC632839 treatment was evaluated by a 2D colony-formation assay. The expression level of SENP2 and its correlation with androgen receptor (AR) were investigated in PCa tissue samples using publicly avail- able datasets. Results: The IC50 values of NSC632839 were 3.1, 1.9, and 17.7 for LNCaP, PC3, and CCD- 1072Sk, respectively. In this IC50 concentration, NSC632839 completely abolished the colony-formation ability of PC3 cells. The expression level of SENP2 was elevated in metastatic PCa tissue samples and was correlated with the AR. Conclusion: NSC632839 was an antiproliferative agent in PCa cells at low doses. Therefore, NSC632839 is a strong drug candidate requiring further studies.

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