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Computationally Assessing The Specificity Of Receptor Tyrosine Kinase Inhibitors, Htoo Say
Computationally Assessing The Specificity Of Receptor Tyrosine Kinase Inhibitors, Htoo Say
Theses/Capstones/Creative Projects
Receptor tyrosine kinases (RTKs) are vital to cell signaling processes such as growth, survival, and differentiation. Dysregulation through mutation or overexpression often contributes to cancer, making RTKs key therapeutic targets for tyrosine kinase inhibitors (TKIs). However, the low specificity of many TKIs leads to off-target effects. This project uses molecular docking to evaluate the binding affinities and selectivity of FDA-approved TKIs across 18 RTK subtypes. The dockings conducted revealed significant variability in binding affinities, with Sorafenib exhibiting strong specificity for EphB2 (-7.6 kcal/mol) and poor compatibility with EphA7 and ErbB4 (-3.0 kcal/mol). These findings underscore the role of specific molecular …