Article

Stereoselective Covalent Targeting of BTK(C481S) and Kinases with β-Lactone Electrophiles

2026-07-06

Abstract excerpt

<h4>ABSTRACT</h4> The cysteine to serine mutation at residue 481 of Bruton’s tyrosine kinase (BTK) is the most common mechanism of clinical resistance against ibrutinib for the treatment of mantle cell lymphoma and chronic lymphocytic leukemia. We report small molecule ligands containing chiral β-lactone electrophiles to address this challenge. The asymmetric warhead enabled stereoselective covalent modification...

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Literature Corpus work: c0cb6e9f-4458-51a3-9b6d-94e0622a18f7
DOI: 10.64898/2026.07.03.736436

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