Evolutionary Divergence in the Conformational Landscapes of Tyrosine vs Serine/Threonine Kinases

Inactive conformations of protein kinase catalytic domains where the DFG motif has a "DFG-out" orientation and the activation loop is folded present a druggable binding pocket that is targeted by FDA-approved "type-II inhibitors" in the treatment of cancers. Tyrosine Kinases (TKs) typically show strong binding affinity with a wide spectrum... Show more