Design of Small Molecules That Compete with Nucleotide Binding to an Engineered Oncogenic KRAS Allele.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemistry"
DOI: 10.1021/acs.biochem.7b01113
Abstract: RAS mutations are found in 30% of all human cancers, with KRAS the most frequently mutated among the three RAS isoforms (KRAS, NRAS, and HRAS). However, directly targeting oncogenic KRAS with small molecules in the… read more here.
Keywords: nucleotide binding; oncogenic kras; binding site; small molecules ... See more keywords
Farnesyltransferase-Mediated Delivery of a Covalent Inhibitor Overcomes Alternative Prenylation to Mislocalize K-Ras.
Sign Up to like & getrecommendations! Published in 2017 at "ACS chemical biology"
DOI: 10.1021/acschembio.7b00374
Abstract: Mutationally activated Ras is one of the most common oncogenic drivers found across all malignancies, and its selective inhibition has long been a goal in both pharma and academia. One of the oldest and most… read more here.
Keywords: mediated delivery; alternative prenylation; covalent inhibitor; farnesyltransferase mediated ... See more keywords
Discovery of a Potent and Selective Covalent Inhibitor and Activity-Based Probe for the Deubiquitylating Enzyme UCHL1, with Antifibrotic Activity
Sign Up to like & getrecommendations! Published in 2020 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.0c04527
Abstract: Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a deubiquitylating enzyme that is proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung fibrosis. Herein we report the discovery of the most potent and… read more here.
Keywords: potent selective; discovery potent; probe; deubiquitylating enzyme ... See more keywords
Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4.
Sign Up to like & getrecommendations! Published in 2019 at "Chemical communications"
DOI: 10.1039/c9cc02052g
Abstract: Biochemical and structural studies provide information on the mode of action of FGF401 as a selective, reversible covalent inhibitor of FGFR4. Kinase and proliferation assays reveal that FGF401 has the ability to overcome gatekeeper mutations… read more here.
Keywords: covalent inhibitor; characterization fgf401; reversible covalent; fgf401 reversible ... See more keywords