Article
Allosteric Kinase Inhibitors Reshape MEK1 Kinase Activity Conformations in Cells and In Silico.
Biomolecules - 30 Mar 2021
Fleischmann Jakob, Feichtner Andreas, DeFalco Louis, Kugler Valentina, Schwaighofer Selina, Huber Roland G, Stefan Eduard
Abstract excerpt
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. Thus, targeted MEK inhibition causes qualitative alterations of carcinogenic MAPK signals. Phosphorylation...
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