Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment
Sign Up to like & getrecommendations! Published in 2018 at "Nature Communications"
DOI: 10.1038/s41467-018-05707-2
Abstract: Targeting specific protein–protein interactions (PPIs) is an attractive concept for drug development, but hard to implement since intracellular antibodies do not penetrate cells and most small-molecule drugs are considered unsuitable for PPI inhibition. A potential… read more here.
Keywords: protein interactions; ras effector; small molecule; antibody ... See more keywords
Structure-based development of new RAS-effector inhibitors from a combination of active and inactive RAS-binding compounds
Sign Up to like & getrecommendations! Published in 2019 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1811360116
Abstract: Significance The RAS family of oncogenic proteins is important as therapy targets because of the frequency of activating mutations in almost all major cancers. An important approach is development of small molecules with drug-like properties… read more here.
Keywords: ras binding; ras effector; protein protein; structure based ... See more keywords
BRET-based RAS biosensors that show a novel small molecule is an inhibitor of RAS-effector protein-protein interactions
Sign Up to like & getrecommendations! Published in 2018 at "eLife"
DOI: 10.7554/elife.37122
Abstract: The RAS family of proteins is amongst the most highly mutated in human cancers and has so far eluded drug therapy. Currently, much effort is being made to discover mutant RAS inhibitors and in vitro… read more here.
Keywords: ras effector; based ras; protein protein; bret based ... See more keywords