Université Paris-Sud, Orsay, France.
Trends Mol Med. 2012 Nov;18(11):679-88. doi: 10.1016/j.molmed.2012.09.008. Epub 2012 Oct 17.
Ten percent of inherited diseases are caused by premature termination codon (PTC) mutations that lead to degradation of the mRNA template and to the production of a non-functional, truncated polypeptide. In addition, many acquired mutations in cancer introduce similar PTCs. In 1999, proof-of-concept for treating these disorders was obtained in a mouse model of muscular dystrophy, when administration of aminoglycosides restored protein translation by inducing the ribosome to bypass a PTC. Since, many studies have validated this approach, but despite the promise of PTC readthrough therapies, the mechanisms of translation termination remain to be precisely elucidated before even more progress can be made. Here, we review the molecular basis for PTC readthrough in eukaryotes and describe currently available compounds with significant therapeutic potential for treating genetic disorders and cancer.
10%的遗传性疾病是由导致 mRNA 模板降解和产生无功能的截断多肽的提前终止密码子 (PTC) 突变引起的。此外,许多癌症中的获得性突变也会引入类似的 PTC。1999 年,在肌营养不良症的小鼠模型中,通过氨基糖苷类药物诱导核糖体绕过 PTC 恢复蛋白质翻译,为治疗这些疾病提供了概念验证。此后,许多研究已经验证了这种方法,但尽管 PTC 通读治疗有希望,在取得更大进展之前,仍需要精确阐明翻译终止的机制。在这里,我们回顾了真核生物中 PTC 通读的分子基础,并描述了目前具有治疗遗传疾病和癌症的显著治疗潜力的化合物。