Insights into ligand stimulation effects on gastro-intestinal stromal tumors signalling.
Sign Up to like & getrecommendations! Published in 2017 at "Cellular signalling"
DOI: 10.1016/j.cellsig.2016.10.009
Abstract: Mutations in KIT or PDGFRA are responsible for >85% of gastrointestinal stromal tumors. The introduction of imatinib in the GIST therapy scheme revolutionized the patient outcome. Unfortunately, the therapy allows the disease stabilization instead of… read more here.
Keywords: kinase activity; stromal tumors; gist; kit mutants ... See more keywords
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01845
Abstract: Drug resistance due to acquired mutations that constitutively activate c-KIT is a significant challenge in the treatment of patients with gastrointestinal stromal tumors (GISTs). Herein, we identified 1-(5-ethyl-isoxazol-3-yl)-3-(4-{2-[6-(4-ethylpiperazin-1-yl)pyrimidin-4-ylamino]-thiazol-5-yl}phenyl)urea (10a) as a potent inhibitor against unactivated… read more here.
Keywords: discovery conformational; activated kit; kit; control inhibitors ... See more keywords