Department of Biotechnology, Manipal Institute of Technology, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.
Department of Bioinformatics, S.S. and L.S. Patkar College, Mumbai, India.
Mol Biotechnol. 2024 Oct;66(10):2792-2803. doi: 10.1007/s12033-023-00879-9. Epub 2023 Sep 28.
Lung adenocarcinoma (LUAD) is one of the most prevalent and leading causes of cancer deaths globally, with limited diagnostic and clinically significant therapeutic targets. Identifying the genes and processes involved in developing and progressing LUAD is crucial for developing effective targeted therapeutics and improving patient outcomes. Therefore, the study aimed to explore the RNA sequencing data of LUAD from The Cancer Genome Atlas (TCGA) and gene expression profile datasets involving GSE10072, GSE31210, and GSE32863 from the Gene Expression Omnibus (GEO) databases. The differential gene expression and the downstream analysis determined clinically significant biomarkers using a network-based approach. These therapeutic targets predominantly enriched the dysregulation of mitotic cell cycle regulation and revealed the co-overexpression of Aurora-A Kinase (AURKA) and Targeting Protein for Xklp2 (TPX2) with high survival risk in LUAD patients. The hydrophobic residues of the AURKA-TPX2 interaction were considered as the target site to block the autophosphorylation of AURKA during the mitotic cell cycle. The tyrosine kinase inhibitor (TKI) dacomitinib demonstrated the strong binding potential to hinder TPX2, shielding the AURKA destabilization. This in silico study lays the foundation for repurposing targeted therapeutic options to impede the Protein-Protein Interactions (PPIs) in LUAD progression and aid in future translational investigations.
肺腺癌(LUAD)是全球最常见和主要的癌症死亡原因之一,其诊断和具有临床意义的治疗靶点有限。确定参与 LUAD 发生和进展的基因和过程对于开发有效的靶向治疗方法和改善患者预后至关重要。因此,本研究旨在探索来自癌症基因组图谱(TCGA)的 LUAD 的 RNA 测序数据,以及基因表达谱数据集,包括来自基因表达综合数据库(GEO)的 GSE10072、GSE31210 和 GSE32863。通过基于网络的方法,对差异基因表达和下游分析确定了具有临床意义的生物标志物。这些治疗靶点主要富集了有丝分裂细胞周期调节的失调,并揭示了 Aurora-A 激酶(AURKA)和靶向 Xklp2 的蛋白(TPX2)的共过表达,这与 LUAD 患者的高生存风险相关。AURKA-TPX2 相互作用的疏水性残基被认为是靶位点,以阻断有丝分裂细胞周期中 AURKA 的自动磷酸化。酪氨酸激酶抑制剂(TKI)达可替尼表现出与 TPX2 强烈结合的潜力,从而阻止 AURKA 失稳。这项计算机研究为重新利用靶向治疗选择以阻止 LUAD 进展中的蛋白质-蛋白质相互作用(PPIs)奠定了基础,并有助于未来的转化研究。