Lung cancer is a major cause of cancer deaths worldwide, and has a very low survival rate.
Non-small cell lung cancer (NSCLC) is the largest subset of lung cancers, which accounts …

Lung cancers with a mutated epidermal growth factor receptor (EGFR) are a major
contributor to cancer fatalities globally. Targeted tyrosine kinase inhibitors (TKIs) have been …

Highlights•Non-synonymous point mutations affect the conformational landscape of
proteins.•Free energy calculations are used to quantify the effect of mutations.•Pathogenic …

Experimental studies have demonstrated that L858R mutation in the EGF receptor (EGFR)
confers tumor sensitivity whereas T790M and L858R/T790M mutations cause resistance to …

The L858R mutation in EGFR is particularly responsive to small tyrosine kinase inhibitors
(TKIs) such as gefitinib and erlotinib. This efficacy decreases due to drug resistance …

The recent studies have revealed that most BRAF inhibitors can paradoxically induce kinase
activation by promoting dimerization and enzyme transactivation. Despite rapidly growing …

Receptor tyrosine kinase KIT controls many signal transduction pathways and represents a
typical allosterically regulated protein. The mutation-induced deregulation of KIT activity …

The ErbB protein tyrosine kinases are among the most important cell signaling families and
mutation-induced modulation of their activity is associated with diverse functions in …

Fms‐like tyrosine kinase 3 (FLT3) is a receptor tyrosine kinase that is a drug target for
leukemias. Several potent inhibitors of FLT3 exist, and bind to the inactive form of the …

Non-small cell lung cancer (NSCLC) patients carrying specific EGFR kinase activating
mutations (L858R, delE746-A750) respond well to tyrosine kinase inhibitors (TKIs) …