基因表达通过许多调控元素及其相关转录因子（TFs）的整合进行调节。TFs与特定的DNA序列结合并激活或抑制转录活动。经过几十年的研究，已经确定，TFs的异常表达或功能异常可能导致细胞不受控制地分裂和癌症的发生。在癌症转录调控的最初研究中，重点放在将TFs作为转录激活因子上。然而，最近的研究表明，在癌症中存在着几种不同的转录抑制机制，这些机制可能是特定抗癌药物的潜在治疗靶点。在本文的第一部分"转录抑制因子在癌症发展中的新作用"中，我们概述了当前对转录抑制因子及其在癌症进程的分子过程中的参与的理解。在随后的"治疗应用"部分，我们提供了更新的药物发现的可用靶点的概述，并讨论这些应用的新前沿。 ©2023年，韩国药学会。

Gene expression is modulated through the integration of many regulatory elements and their associated transcription factors (TFs). TFs bind to specific DNA sequences and either activate or repress transcriptional activity. Through decades of research, it has been established that aberrant expression or functional abnormalities of TFs can lead to uncontrolled cell division and the development of cancer. Initial studies on transcriptional regulation in cancer have focused on TFs as transcriptional activators. However, recent studies have demonstrated several different mechanisms of transcriptional repression in cancer, which could be potential therapeutic targets for the development of specific anti-cancer agents. In the first section of this review, "Emerging roles of transcriptional repressors in cancer development," we summarize the current understanding of transcriptional repressors and their involvement in the molecular processes of cancer progression. In the subsequent section, "Therapeutic applications," we provide an updated overview of the available therapeutic targets for drug discovery and discuss the new frontier of such applications.© 2023. The Pharmaceutical Society of Korea.