They do so because when an RTK becomes activated, the result is phosphorylation of specific tyrosines on the cytoplasmic tail, the intracellular portion of the receptor. This phosphorylation leads ...
MAPK pathway: uncontrolled growth via the MAPK pathway promotes melanoma cell growth.The pathway provides several sites for potential pharmacologic inhibition.RTK: Receptor tyrosine kinase.
“So much of drug development is ‘me-too’, with multiple companies targeting the latest activating mutation in a particular RTK [receptor tyrosine kinase] target,” Hembrough added.
Genetic mechanisms of resistance to kinase inhibitors include mutations in the target receptor and mutations or gene amplification of compensatory receptors or other signaling effectors.