Nucleotide based covalent inhibitors of KRas can only be efficient in vivo if they bind reversibly with GTP-like affinity
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-03973-6
Abstract: Simple reversible competitive inhibition of nucleotide binding of GTP to Ras family GTPases has long been recognized as an unlikely approach to manipulating the activity of such proteins for experimental or therapeutic purposes. This is… read more here.
Keywords: based covalent; nucleotide based; covalent inhibitors; affinity ... See more keywords
Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "eLife"
DOI: 10.1101/2022.07.25.501348
Abstract: Mutations within Ras proteins represent major drivers in human cancer. In this study, we report the structure-based design, synthesis, as well as biochemical and cellular evaluation of nucleotide-based covalent inhibitors for KRasG13C, an important oncogenic… read more here.
Keywords: covalent inhibitors; nucleotide based; krasg13c covalently; based covalent ... See more keywords