Department of Biochemical Sciences, Sapienza University of Rome, 00185 Rome, Italy.
Institute of Molecular Biology and Pathology, National Research Council of Italy, Sapienza University of Rome, 00185 Rome, Italy.
Int J Mol Sci. 2023 Mar 1;24(5):4746. doi: 10.3390/ijms24054746.
Myc transcription factors are key regulators of many cellular processes, with Myc target genes crucially implicated in the management of cell proliferation and stem pluripotency, energy metabolism, protein synthesis, angiogenesis, DNA damage response, and apoptosis. Given the wide involvement of Myc in cellular dynamics, it is not surprising that its overexpression is frequently associated with cancer. Noteworthy, in cancer cells where high Myc levels are maintained, the overexpression of Myc-associated kinases is often observed and required to foster tumour cells' proliferation. A mutual interplay exists between Myc and kinases: the latter, which are Myc transcriptional targets, phosphorylate Myc, allowing its transcriptional activity, highlighting a clear regulatory loop. At the protein level, Myc activity and turnover is also tightly regulated by kinases, with a finely tuned balance between translation and rapid protein degradation. In this perspective, we focus on the cross-regulation of Myc and its associated protein kinases underlying similar and redundant mechanisms of regulation at different levels, from transcriptional to post-translational events. Furthermore, a review of the indirect effects of known kinase inhibitors on Myc provides an opportunity to identify alternative and combined therapeutic approaches for cancer treatment.
Myc 转录因子是许多细胞过程的关键调节剂,Myc 靶基因在细胞增殖和干细胞多能性、能量代谢、蛋白质合成、血管生成、DNA 损伤反应和细胞凋亡的调控中起着至关重要的作用。鉴于 Myc 在细胞动态中的广泛参与,其过度表达常与癌症有关也就不足为奇了。值得注意的是,在 Myc 水平维持较高的癌细胞中,常观察到 Myc 相关激酶的过度表达,并且需要这些激酶来促进肿瘤细胞的增殖。Myc 和激酶之间存在相互作用:后者是 Myc 的转录靶点,可磷酸化 Myc,使其转录活性增强,这凸显了一个明确的调控循环。在蛋白质水平上,Myc 的活性和周转率也受到激酶的严格调控,在翻译和快速蛋白降解之间存在精细的平衡。在这方面,我们重点关注 Myc 与其相关蛋白激酶的交叉调控,这些激酶在不同水平(从转录到翻译后事件)上具有相似且冗余的调控机制。此外,对已知激酶抑制剂对 Myc 的间接影响的综述提供了一个机会,可以确定用于癌症治疗的替代和联合治疗方法。