Structural basis for the action of the drug trametinib at KSR-bound MEK

The MAPK/ERK kinase MEK is a shared effector of the frequent cancer drivers KRAS and BRAF that has long been pursued as a drug target in oncology 1 , and more recently in immunotherapy 2 , 3 and ageing 4 . However, many MEK inhibitors are limited owing to on-target toxicities 5 – 7 and drug resistan...

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Veröffentlicht in:	Nature (London) 2020-12, Vol.588 (7838), p.509-514
Hauptverfasser:	Khan, Zaigham M., Real, Alexander M., Marsiglia, William M., Chow, Arthur, Duffy, Mary E., Yerabolu, Jayasudhan R., Scopton, Alex P., Dar, Arvin C.
Format:	Artikel
Sprache:	eng
Schlagworte:	13 631/45/535/1266 631/45/607/275 631/67/1059/153 631/92 692/699/67 82 Allosteric properties Amino Acid Sequence Animals Binding Binding Sites - drug effects Crystal structure Drug development Extracellular signal-regulated kinase FDA approval Humanities and Social Sciences Humans Inhibitor drugs Kinases MAP kinase MEK inhibitors Mice Mitogen-Activated Protein Kinase Kinases - antagonists & inhibitors Mitogen-Activated Protein Kinase Kinases - chemistry Mitogen-Activated Protein Kinase Kinases - metabolism Models, Molecular Molecular structure multidisciplinary Protein Binding - drug effects Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinases - chemistry Protein Kinases - metabolism Pyridones - chemistry Pyridones - pharmacology Pyrimidinones - chemistry Pyrimidinones - pharmacology raf Kinases - chemistry raf Kinases - metabolism Science Science (multidisciplinary) Structure-function relationships Substrate Specificity Targeted cancer therapy Therapeutic targets
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