Department of Theoretical Informatics, Institute of Informatics, Department of Theoretical Informatics, Federal University of Rio Grande do Sul, Porto Alegre, RS Brazil; Department of Genetics, Institute of Bioscience, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil; Department of Biophysics, Institute of Bioscience, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil.
Department of Microbiology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, SP, Brazil.
Mutat Res Rev Mutat Res. 2022 Jul-Dec;790:108436. doi: 10.1016/j.mrrev.2022.108436. Epub 2022 Aug 8.
POLη, encoded by the POLH gene, is a crucial protein for replicating damaged DNA and the most studied specialized translesion synthesis polymerases. Mutations in POLη are associated with cancer and the human syndrome xeroderma pigmentosum variant, which is characterized by extreme photosensitivity and an increased likelihood of developing skin cancers. The myriad of structural information about POLη is vast, covering dozens of different mutants, numerous crucial residues, domains, and posttranslational modifications that are essential for protein function within cells. Since POLη is key vital enzyme for cell survival, and mutations in this protein are related to aggressive diseases, understanding its structure is crucial for biomedical sciences, primarily due to its similarities with other Y-family polymerases and its potential as a targeted therapy-drug for tumors. This work provides an up-to-date review on structural aspects of the human POLη: from basic knowledge about critical residues and protein domains to its mutant variants, posttranslational modifications, and our current understanding of therapeutic molecules that target POLη. Thus, this review provides lessons about POLη's structure and gathers critical discussions and hypotheses that may contribute to understanding this protein's vital roles within the cells.
POLη 由 POLH 基因编码,是一种在复制受损 DNA 时必不可少的蛋白质,也是研究最为深入的专门跨损伤合成聚合酶之一。POLη 的突变与癌症和人类着色性干皮病变异型有关,该变异型的特征是极度光敏和皮肤癌发病几率增加。关于 POLη 的结构信息非常丰富,涵盖了数十种不同的突变体、许多关键残基、结构域和翻译后修饰,这些对于蛋白质在细胞内的功能至关重要。由于 POLη 是细胞存活的关键酶,并且该蛋白的突变与侵袭性疾病有关,因此了解其结构对于生物医学科学至关重要,主要是因为它与其他 Y 家族聚合酶具有相似性,并且具有作为肿瘤靶向治疗药物的潜力。这项工作提供了关于人类 POLη 结构方面的最新综述:从关键残基和蛋白质结构域的基本知识到其突变体、翻译后修饰,以及我们目前对靶向 POLη 的治疗分子的理解。因此,本综述提供了有关 POLη 结构的经验教训,并汇集了可能有助于理解该蛋白质在细胞内重要作用的关键讨论和假设。