Prolonged and tunable residence time using reversible covalent kinase inhibitors
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چکیده
منابع مشابه
Prolonged and tunable residence time using reversible covalent kinase inhibitors
Drugs with prolonged on-target residence times often show superior efficacy, yet general strategies for optimizing drug-target residence time are lacking. Here we made progress toward this elusive goal by targeting a noncatalytic cysteine in Bruton's tyrosine kinase (BTK) with reversible covalent inhibitors. Using an inverted orientation of the cysteine-reactive cyanoacrylamide electrophile, we...
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ژورنال
عنوان ژورنال: Nature Chemical Biology
سال: 2015
ISSN: 1552-4450,1552-4469
DOI: 10.1038/nchembio.1817