Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Drug resistance develops in nearly all patients with colon cancer, leading to a decrease in
the therapeutic efficacies of anticancer agents. This review provides an up-to-date summary …

Lung cancer has a high prevalence, with a growing number of new cases and mortality
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …

The availability of 3 generations of epidermal growth factor receptor (EGFR) tyrosine kinase
inhibitors (TKIs) with different pharmacologic characteristics and clinical profiles has …

Because dysregulation of protein kinases owing to mutations or overexpression plays
causal roles in human diseases, this family of enzymes has become one of the most …

Kinases are key regulatory signalling proteins governing numerous essential biological
processes and cellular functions. Dysregulation of many protein kinases is associated with …

Both the first‐generation reversible epidermal growth factor receptor (EGFR) inhibitors
gefitinib and erlotinib and the second‐generation covalent epidermal growth factor receptor …

Abstract EGFR T790M mutation leads to resistance to most of clinically available EGFR TKIs.
Third-generation EGFR TKIs against the T790M mutation have been in active clinical …