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Article

Differential impact of BTK active site inhibitors on the conformational state of full-length BTK.

eLife - 23 Nov 2020

Joseph Raji E, Amatya Neha, Fulton D Bruce, Engen John R, Wales Thomas E, Andreotti Amy

Abstract excerpt

Bruton's tyrosine kinase (BTK) is targeted in the treatment of B-cell disorders including leukemias and lymphomas. Currently approved BTK inhibitors, including Ibrutinib, a first-in-class covalent inhibitor of BTK, bind directly to the kinase active site. While effective at blocking the catalytic activity of BTK, consequences of drug binding on the global conformation of full-length BTK are unknown. Here, we...

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PMID: 33226337
DOI: 10.7554/eLife.60470
PMCID: PMC7834017

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