Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

EGFR mutations account for the majority of druggable targets in lung adenocarcinoma. Over
the past decades the optimization of EGFR inhibitors revolutionized the treatment options for …

Lung cancer is frequently caused by activating mutations in the epidermal growth factor
receptor (EGFR). Allosteric EGFR inhibitors offer promise as the next generation of …

Covalent inhibition has become more accepted in the past two decades, as illustrated by the
clinical approval of several irreversible inhibitors designed to covalently modify their target …

The altered activation or overexpression of protein kinases (PKs) is a major subject of
research in oncology and their inhibition using small molecules, protein kinases inhibitors …

Enzyme inhibitors that form covalent bonds with their targets are being increasingly pursued
in drug development. Assessing their biochemical activity relies on time-dependent assays …

Advanced non-small-cell lung cancer (NSCLC) patients with EGFR T790M-positive tumours
benefit from osimertinib, an epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR …

Lung cancer is the second most common cause of morbidity and mortality among cancer
types worldwide, with non-small cell lung cancer (NSCLC) representing the majority of most …

Background Preoperative assessment of the acquired resistance T790M mutation in patients
with metastatic non‐small cell lung cancer (NSCLC) based on brain metastasis (BM) is …

Tyrosine kinase inhibitors (TKIs) are used to treat non-small cell lung cancers (NSCLC)
driven by epidermal growth factor receptor (EGFR) mutations in the tyrosine kinase domain …