Tuned out

Controlling kinase inhibitors’ residence time via reversible covalent binding is of high interest in drug discovery. Tuning reversible covalent binding kinetics using a pan-kinase inhibitor that reacts with the catalytic lysine enabled exquisite temporal selectivity in vitro and in vivo.

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Bibliographische Detailangaben
Veröffentlicht in:	Nature chemical biology 2022-09, Vol.18 (9), p.917-918
1. Verfasser:	Ferguson, Fleur M.
Format:	Artikel
Sprache:	eng
Schlagworte:	631/154/309 631/92/275 631/92/475 631/92/613 Binding Binding sites Biochemical Engineering Biochemistry Biology Bioorganic Chemistry Cell Biology Chemistry Chemistry and Materials Science Chemistry/Food Science Drugs Enzyme inhibitors FDA approval Kinases Lysine News & Views news-and-views Pharmaceuticals Proteins Selectivity
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Beschreibung
Zusammenfassung:	Controlling kinase inhibitors’ residence time via reversible covalent binding is of high interest in drug discovery. Tuning reversible covalent binding kinetics using a pan-kinase inhibitor that reacts with the catalytic lysine enabled exquisite temporal selectivity in vitro and in vivo.
ISSN:	1552-4450 1552-4469
DOI:	10.1038/s41589-022-01037-z