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 str...

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Autors principals:	Joan Gizzio, Abhishek Thakur, Allan Haldane, Ronald M Levy
Format:	Artigo
Idioma:	Inglês
Publicat:	eLife Sciences Publications Ltd 2022-12-01
Col·lecció:	eLife
Matèries:	protein kinases conformational landscape free-energy simulations coevolution type-II inhibitors tyrosine kinase evolution
Accés en línia:	https://elifesciences.org/articles/83368
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