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Article

Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations.

ACS chemical biology - 21 Oct 2016

Johnson Adam R, Kohli Pawan Bir, Katewa Arna, Gogol Emily, Belmont Lisa D, Choy Regina, Penuel Elicia, Burton Luciana, Eigenbrot Charles, Yu Christine, Ortwine Daniel F, Bowman Krista, Franke Yvonne, Tam Christine, Estevez Alberto, Mortara Kyle, Wu Jiansheng, Li Hong, Lin May, Bergeron Philippe, Crawford James J, Young Wendy B

Abstract excerpt

The Bruton's tyrosine kinase (Btk) inhibitor ibrutinib has shown impressive clinical efficacy in a range of B-cell malignancies. However, acquired resistance has emerged, and second generation therapies are now being sought. Ibrutinib is a covalent, irreversible inhibitor that modifies Cys481 in the ATP binding site of Btk and renders the enzyme inactive, thereby blocking B-cell receptor signal transduction. Not...

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PMID: 27571029
DOI: 10.1021/acschembio.6b00480

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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