Schwaighofer S
Tracking and blocking interdependencies of cellular BRAF-MEK oncokinase activities
The selective targeting of mutated kinases in cancer therapies has the potential to improve therapeutic success and thereby the survival of patients. In the case of melanoma, the constitutively active MAPK pathway is targeted by a combinatorial inhibition of BRAF and MEK activities.
ReadAllosteric Kinase Inhibitors Reshape MEK1 Kinase Activity Conformations in Cells and In Silico
Mutations at different stages of the mitogen-activated protein kinase (MAPK) signaling pathway lead to aberrant activation of the involved protein kinase entities. These oncogenic modifications alter signal propagation which converge on the gatekeeper kinases MEK1/2, transmitting the input signal to ERK1/2.
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