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

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

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 ac...

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Bibliographic Details
Main Authors: Raji E Joseph, Neha Amatya, D Bruce Fulton, John R Engen, Thomas E Wales, Amy Andreotti
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2020-11-01
Series:eLife
Subjects:
bruton tyrosine kinase
kinase inhibitor
drug resistance
allostery
hydrogen/deuterium exchange mass spectrometry
nuclear magnetic resonance
Online Access:https://elifesciences.org/articles/60470

Internet

https://elifesciences.org/articles/60470

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