Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Sign Up to like & getrecommendations! Published in 2021 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2021.01.003
Abstract: There is increasing evidence of a significant correlation between prolonged drug-target residence time and increased drug efficacy. Here, we report a structural rationale for kinetic selectivity between two closely related kinases: focal adhesion kinase (FAK)… read more here.
Keywords: kinetic selectivity; fak inhibitors; structure kinetic; selectivity ... See more keywords
Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00864
Abstract: Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side-effects (EPS) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with contrasting… read more here.
Keywords: dopamine receptor; kinetic profiling; haloperidol; structure kinetic ... See more keywords