Ontology highlight
ABSTRACT:
INSTRUMENT(S): Orbitrap Fusion Lumos
ORGANISM(S): Homo Sapiens (human)
TISSUE(S): Cell Culture
SUBMITTER: Eric Fischer
LAB HEAD: Eric S. Fischer
PROVIDER: PXD010568 | Pride | 2019-01-25
REPOSITORIES: Pride
Dobrovolsky Dennis D Wang Eric S ES Morrow Sara S Leahy Catharine C Faust Tyler T Nowak Radosław P RP Donovan Katherine A KA Yang Guang G Li Zhengnian Z Fischer Eric S ES Treon Steven P SP Weinstock David M DM Gray Nathanael S NS
Blood 20181213 9
The covalent Bruton tyrosine kinase (BTK) inhibitor ibrutinib is highly efficacious against multiple B-cell malignancies. However, it is not selective for BTK, and multiple mechanisms of resistance, including the C481S-BTK mutation, can compromise its efficacy. We hypothesized that small-molecule-induced BTK degradation may overcome some of the limitations of traditional enzymatic inhibitors. Here, we demonstrate that BTK degradation results in potent suppression of signaling and proliferation i ...[more]