Feoli Alessandra, Viviano Monica, Cipriano Alessandra, Milite Ciro, Castellano Sabrina, Sbardella Gianluca
Department of Pharmacy, Epigenetic Med Chem Lab, University of Salerno via Giovanni Paolo II 132 I-84084 Fisciano SA Italy
RSC Chem Biol. 2021 Dec 13;3(4):359-406. doi: 10.1039/d1cb00196e. eCollection 2022 Apr 6.
Protein lysine methyltransferases constitute a large family of epigenetic writers that catalyse the transfer of a methyl group from the cofactor -adenosyl-l-methionine to histone- and non-histone-specific substrates. Alterations in the expression and activity of these proteins have been linked to the genesis and progress of several diseases, including cancer, neurological disorders, and growing defects, hence they represent interesting targets for new therapeutic approaches. Over the past two decades, the identification of modulators of lysine methyltransferases has increased tremendously, clarifying the role of these proteins in different physio-pathological states. The aim of this review is to furnish an updated outlook about the protein lysine methyltransferases disclosed modulators, reporting their potency, their mechanism of action and their eventual use in clinical and preclinical studies.
蛋白质赖氨酸甲基转移酶构成了一个庞大的表观遗传书写蛋白家族，可催化辅因子S-腺苷-L-甲硫氨酸上的甲基转移至组蛋白和非组蛋白特异性底物。这些蛋白质表达和活性的改变与包括癌症、神经疾病和生长缺陷在内的多种疾病的发生和发展有关，因此它们是新治疗方法的有趣靶点。在过去二十年中，赖氨酸甲基转移酶调节剂的鉴定大幅增加，阐明了这些蛋白质在不同生理病理状态中的作用。本综述的目的是提供关于已披露的蛋白质赖氨酸甲基转移酶调节剂的最新观点，报告它们的效力、作用机制以及它们在临床和临床前研究中的最终用途。
