Chen Chia-Chi, Liao Ruo-Yu, Yeh Fang-Yu, Lin Yu-Rou, Wu Tze-You, Pastor Alexa Escobar, Zul Danny Danilo, Hsu Yun-Chien, Wu Kuan-Yo, Liu Ke-Fang, Kannagi Reiji, Chen Jang-Yi, Cai Bi-He
School of Medicine, I-Shou University, Kaohsiung City 82445, Taiwan.
Department of Physical Therapy, I-Shou University, Kaohsiung City 82445, Taiwan.
Biomedicines. 2023 Apr 28;11(5):1310. doi: 10.3390/biomedicines11051310.
(1) Background: A premature termination codon (PTC) can be induced by a type of point mutation known as a nonsense mutation, which occurs within the coding region. Approximately 3.8% of human cancer patients have nonsense mutations of p53. However, the non-aminoglycoside drug PTC124 has shown potential to promote PTC readthrough and rescue full-length proteins. The COSMIC database contains 201 types of p53 nonsense mutations in cancers. We built a simple and affordable method to create different nonsense mutation clones of p53 for the study of the PTC readthrough activity of PTC124. (2) Methods: A modified inverse PCR-based site-directed mutagenesis method was used to clone the four nonsense mutations of p53, including W91X, S94X, R306X, and R342X. Each clone was transfected into p53 null H1299 cells and then treated with 50 μM of PTC124. (3) Results: PTC124 induced p53 re-expression in H1299-R306X and H1299-R342X clones but not in H1299-W91X and H1299-S94X clones. (4) Conclusions: Our data showed that PTC124 more effectively rescued the C-terminal of p53 nonsense mutations than the N-terminal of p53 nonsense mutations. We introduced a fast and low-cost site-directed mutagenesis method to clone the different nonsense mutations of p53 for drug screening.
(1)背景:一种称为无义突变的点突变可在编码区内诱导产生提前终止密码子(PTC)。约3.8%的人类癌症患者存在p53基因的无义突变。然而,非氨基糖苷类药物PTC124已显示出促进PTC通读并挽救全长蛋白的潜力。COSMIC数据库包含癌症中201种p53无义突变类型。我们构建了一种简单且经济的方法来创建p53的不同无义突变克隆,用于研究PTC124的PTC通读活性。(2)方法:采用改良的基于反向PCR的定点诱变方法克隆p53的四种无义突变,包括W91X、S94X、R306X和R342X。将每个克隆转染到p53基因缺失的H1299细胞中,然后用50μM的PTC124处理。(3)结果:PTC124在H1299-R306X和H1299-R342X克隆中诱导p53重新表达,但在H1299-W91X和H1299-S94X克隆中未诱导。(4)结论:我们的数据表明,PTC124挽救p53无义突变的C末端比挽救p53无义突变的N末端更有效。我们引入了一种快速且低成本的定点诱变方法来克隆p53的不同无义突变用于药物筛选。