Ontology highlight
ABSTRACT:
SUBMITTER: Smith CC
PROVIDER: S-EPMC4522415 | biostudies-literature | 2015 Jun
REPOSITORIES: biostudies-literature
Smith Catherine C CC Zhang Chao C Lin Kimberly C KC Lasater Elisabeth A EA Zhang Ying Y Massi Evan E Damon Lauren E LE Pendleton Matthew M Bashir Ali A Sebra Robert R Perl Alexander A Kasarskis Andrew A Shellooe Rafe R Tsang Garson G Carias Heidi H Powell Ben B Burton Elizabeth A EA Matusow Bernice B Zhang Jiazhong J Spevak Wayne W Ibrahim Prabha N PN Le Mai H MH Hsu Henry H HH Habets Gaston G West Brian L BL Bollag Gideon G Shah Neil P NP
Cancer discovery 20150406 6
<h4>Unlabelled</h4>Tyrosine kinase domain mutations are a common cause of acquired clinical resistance to tyrosine kinase inhibitors (TKI) used to treat cancer, including the FLT3 inhibitor quizartinib. Mutation of kinase "gatekeeper" residues, which control access to an allosteric pocket adjacent to the ATP-binding site, has been frequently implicated in TKI resistance. The molecular underpinnings of gatekeeper mutation-mediated resistance are incompletely understood. We report the first cocrys ...[more]