Prostate cancer (PCa) seriously threatens male health, and targeting dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) has been verified to reduce PCa burden, while the research progress on the DYRK2 inhibitors was relatively slow. In this work, we discovered DYRK2 inhibitor (IC = 9681 nM) through virtual screening. Subsequently, we performed systematic structural optimization to obtain (IC = 14 nM).
View Article and Find Full Text PDFBackground: Diffuse large B-cell lymphoma (DLBCL) exhibits remarkable heterogeneity but still remains undiagnosed in identifying the subpopulation of DLBCL to predict the prognosis and guide clinical treatment.
Methods: Molecular subgroups were identified in gene expression data from GSE10846 by a consensus clustering algorithm. And gene set enrichment analysis, immune infiltration, and the proposed cell cycle algorithm were applied to explore the biological functions of different subtypes.
Comprehensive multiplatform analysis of Luminal B breast cancer (LBBC) specimens identifies two molecularly distinct, clinically relevant subtypes: Cluster A associated with cell cycle and metabolic signaling and Cluster B with predominant epithelial mesenchymal transition (EMT) and immune response pathways. Whole-exome sequencing identified significantly mutated genes including , , , and with recurrent somatic mutations. Alterations in DNA methylation or transcriptomic regulation in genes (, , , and ) result in tumor microenvironment reprogramming.
View Article and Find Full Text PDFProstate cancer (PCa) is a common male cancer with high incidence and mortality, and hormonal therapy as the major treatment for PCa patients is troubled by the inevitable resistance that makes us identify novel targets for PCa. Dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) was found to be an effective target for the treatment of PCa, but the research on its inhibitors is rather little. In this work, a potent DYRK2 inhibitor (IC = 0.
View Article and Find Full Text PDFBackground: Currently, predictive models were not developed based on the signaling pathway signatures of immune-related lncRNAs in breast cancer (BRCA) patients.
Methods: We selected unsupervised hierarchical clustering algorithm to classify patients with BRCA based on the significant immune-derived lncRNAs from the TCGA dataset. And different methods including ESTIMATE, ImmuneCellAI, and CIBERSORT were performed to evaluate the immune infiltration of tumor microenvironment.