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通过基于自动显示的片库选来识别一种强大的PCNA-p15相互作用抑制剂

Sarah Hardebeck¹, Natalie Jácobo Goebbels¹, Caroline Michalski¹

¹University of Münster, Institute of Pharmaceutical and Medicinal Chemistry, Münster, Germany.

Microbial biotechnology

|April 22, 2024

概括

研究人员开发了一种新型的自显示选方法,以找到针对增殖细胞核抗原 (PCNA) 的受体抑制剂. 一种变体,P3,表现出高亲和力和抑制PCNA相互作用,为癌症治疗提供了潜力.

科学领域:

分子生物学分子生物学
生物化学生物化学
癌症研究癌症研究

背景情况:

增殖细胞核抗原 (PCNA) 对DNA代谢,复制和修复至关重要.
在瘤中PCNA的高表达使其成为癌症治疗的重要目标.

研究的目的:

开发一种基于自动显示的选方法,用于识别PCNA的抑制剂.
发现和描述与PCNA功能相互作用并抑制的新型.

主要方法:

使用自动显示器对大肠杆菌进行12mer随机化库的构建和表面显示.
通过光激活细胞分类 (FACS) 丰富PCNA结合,使用光标记PCNA.
使用流细胞计对-PCNA相互作用的表征和对PCNA-蛋白相互作用的抑制活性的评估.

主要成果:

发现了五种与mScarlet-I-PCNA有亲和力的变体.
对PCNA.P3 (TCPLRWITHDHP) 具有0.62μM的解离常数 (Kd) 的的鉴定.
P3证明了PCNA-p15相互作用的强烈抑制,其半最大抑制度 (IC50) 为16.2μM.

结论:

自动显示方法成功识别了高亲和度PCNA相互作用.
P3是PCNA-p15相互作用的强有力的抑制剂,突出其作为高PCNA表达的癌症治疗剂的潜力.

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相关概念视频

Protein-protein Interfaces

Protein-protein Interfaces

Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...