AFN941 binding WT EGFR TKD(L) & G719S mutant(R)

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EGFR is a receptor tyrosine kinase playing a pivotal role in cell proliferation and differentiation through signal transduction pathways. Its tyrosine kinase domain, or TKD, binds ATP, facilitating phosphate transfer and driving EGFR function. To combat this process, researchers have developed inhibitors targeting the ATP binding cleft of EGFR TKD, effectively blocking substrate phosphorylation and halting signal transduction. Notably, specific EGFR TKD mutations, such as G719S, are responsible for a subset of non-small cell lung cancers. This comparison highlights how AFN941 interacts with wild-type EGFR TKD and the mutated G719S variant, revealing that protein mutations can significantly alter drug binding interactions.