肺癌是最常见的恶性肿瘤之一。尽管过去几十年取得了进展,需要进一步的研究来改善目前肺癌的治疗方法.由甲基转移酶和去甲基酶动态控制,组蛋白上赖氨酸和精氨酸残基的甲基化调节染色质组织,从而调节基因转录。组蛋白甲基化的异常改变已被证明与包括肺癌在内的多种癌症的进展有关。甲基转移酶和脱甲基酶的抑制剂在肺癌中表现出抗肿瘤活性,多个主要候选人正在接受临床试验。这里,我们总结了组蛋白甲基化在肺癌中的作用,强调小分子抑制剂治疗肺癌的最新进展。
Lung cancer is one of the most common malignancies. In spite of the progress made in past decades, further studies to improve current therapy for lung cancer are required. Dynamically controlled by methyltransferases and demethylases, methylation of lysine and arginine residues on histone proteins regulates chromatin organization and thereby gene transcription. Aberrant alterations of histone methylation have been demonstrated to be associated with the progress of multiple cancers including lung cancer. Inhibitors of methyltransferases and demethylases have exhibited anti-tumor activities in lung cancer, and multiple lead candidates are under clinical trials. Here, we summarize how histone methylation functions in lung cancer, highlighting most recent progresses in small molecular inhibitors for lung cancer treatment.