Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules
Baku Acharya,
Debasmita Saha,
Daniel Armstrong
et al.
Abstract:The development of macrocycles has emerged as an innovative approach to improve kinase inhibitor selectivity, as well as pharmacokinetic and pharmacodynamic properties.
Human kinases are recognized as one of the most important drug targets associated with cancer. There are FDA-approved kinase inhibitors to date, most of which work by inhibiting ATP binding...
Human kinases are recognized as one of the most important drug targets associated with cancer. There are FDA-approved kinase inhibitors to date, most of which work by inhibiting ATP binding...
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.