Design, synthesis and biological evaluation of 2H-[1,4]oxazino-[2,3-f]quinazolin derivatives as potential EGFR inhibitors for Non-small cell lung cancer

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have emerged as the first-line treatment for patients with EGFR-mutant non-small cell lung cancer (NSCLC). A series of [1,4]oxazino[2,3-f]quinazolin derivatives were synthesized and evaluated as irreversible EGFR-TKIs for the treatment of NSCLC. Most of the synthesized compounds demonstrated strong inhibitory activity against the EGFR kinase and the… Continue reading Design, synthesis and biological evaluation of 2H-[1,4]oxazino-[2,3-f]quinazolin derivatives as potential EGFR inhibitors for Non-small cell lung cancer

Unravelling lung adenocarcinoma with mucinous histology and its translational implications

Compared with non-mucinous lung adenocarcinoma (LUAD), mucinous LUAD are rare (3%-10% of all LUAD) and include invasive mucinous adenocarcinoma (IMA) and the exceedingly rare colloid adenocarcinoma.1 IMA differ from invasive non-mucinous LUAD by histomorphology, clinical course and genomic characteristics.2,3 Histologically, IMA feature malignant goblet or columnar cells with abundant intracytoplasmic mucin.1 Previous studies have shown… Continue reading Unravelling lung adenocarcinoma with mucinous histology and its translational implications

Discovery of isoquinoline-tethered quinazoline derivatives with enhanced HER2 inhibition over EGFR

Human epidermal growth factor receptor 2 (HER2) is a critical therapeutic target for HER2-positive or HER2-dependent cancers. While several HER2 kinase inhibitors have been identified, achieving high selectivity for HER2 over EGFR remains a significant challenge. In this study, we aimed to develop HER2-selective inhibitors with enhanced cellular activity. To improve the limited cellular activity… Continue reading Discovery of isoquinoline-tethered quinazoline derivatives with enhanced HER2 inhibition over EGFR

GUK1 enzyme plays crucial role in lung cancer metabolism and growth

Lung cancer is a particularly challenging form of cancer. It often strikes unexpectedly and aggressively with little warning, and it can shapeshift in unpredictable ways to evade treatment. While researchers have gleaned important insights into the basic biology of lung cancer, some of the disease’s molecular maneuvers have remained elusive. Now, a team led by… Continue reading GUK1 enzyme plays crucial role in lung cancer metabolism and growth

AI accurately identifies targetable alterations in lung cancer histological images

DeepGEM, an artificial intelligence (AI)-based model, accurately predicts the presence of key genomic alterations in histological slides prepared from samples obtained from patients with lung cancer. This approach provides a cost-effective alternative to genomic testing, generates spatial mutation maps and might support personalized treatment strategies. Validated in diverse datasets, DeepGEM highlights the potential of AI… Continue reading AI accurately identifies targetable alterations in lung cancer histological images