Division of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Leiden, The Netherlands.
Sci Rep. 2022 Mar 14;12(1):4374. doi: 10.1038/s41598-022-08356-0.
Immune checkpoint inhibitors targeting the programmed cell death protein 1 (PD-1)/programmed cell death protein ligand 1 (PD-L1) axis have been remarkably successful in inducing tumor remissions in several human cancers, yet a substantial number of patients do not respond to treatment. Because this may be partially due to the mechanisms giving rise to high PD-L1 expression within a patient, it is highly relevant to fully understand these mechanisms. In this study, we conduct a bioinformatic analysis to quantify the relative importance of transcription factor (TF) activity, microRNAs (miRNAs) and mutations in determining PD-L1 (CD274) expression at mRNA level based on data from the Cancer Genome Atlas. To predict individual CD274 levels based on TF activity, we developed multiple linear regression models by taking the expression of target genes of the TFs known to directly target PD-L1 as independent variables. This analysis showed that IRF1, STAT1, NFKB and BRD4 are the most important regulators of CD274 expression, explaining its mRNA levels in 90-98% of the patients. Because the remaining patients had high CD274 levels independent of these TFs, we next investigated whether mutations associated with increased CD274 mRNA levels, and low levels of miRNAs associated with negative regulation of CD274 expression could cause high CD274 levels in these patients. We found that mutations or miRNAs offered an explanation for high CD274 levels in 81-100% of the underpredicted patients. Thus, CD274 expression is largely explained by TF activity, and the remaining unexplained cases can largely be explained by mutations or low miRNA abundance.
针对程序性细胞死亡蛋白 1 (PD-1)/程序性细胞死亡蛋白配体 1 (PD-L1) 轴的免疫检查点抑制剂在几种人类癌症中显著诱导肿瘤消退,但相当数量的患者对治疗无反应。因为这可能部分是由于导致患者体内 PD-L1 高表达的机制,所以充分了解这些机制是非常相关的。在这项研究中,我们基于癌症基因组图谱的数据,进行了生物信息学分析,以量化转录因子 (TF) 活性、微小 RNA (miRNA) 和突变在决定 PD-L1 (CD274) 表达水平方面的相对重要性。为了根据 TF 活性预测个体 CD274 水平,我们通过将已知直接靶向 PD-L1 的 TF 的靶基因的表达作为自变量,开发了多个线性回归模型。该分析表明,IRF1、STAT1、NFKB 和 BRD4 是 CD274 表达的最重要调节剂,可解释 90-98%患者的 CD274 mRNA 水平。因为其余患者的 CD274 水平不受这些 TF 的影响,所以我们接下来研究了与增加的 CD274 mRNA 水平相关的突变以及与 CD274 表达负调控相关的低水平 miRNA 是否会导致这些患者的 CD274 水平升高。我们发现,突变或 miRNA 可以解释 81-100%预测不足患者的 CD274 高表达。因此,CD274 表达主要由 TF 活性解释,其余未解释的情况主要可以由突变或低 miRNA 丰度解释。