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The goal of this experiment was the confirmation of ZAK as a covalent target of Ibrutinib by an affinity enrichment experiment with a linkable analogue of Ibrutinib.
ORGANISM(S): Homo sapiens (Human) 
2017-10-13 | PXD007638 | Pride
Ibrutinib,a novel Bruton'styrosine kinase inhibitor, demonstrated high response rates in B-cell lymphomas but a growing number of ibrutinib treated patients relapse with resistance, fulminant progression and accelerated mortality. Using chemical proteomics and a high-throughput ex vivo assay in a re...
ORGANISM(S): Homo sapiens (Human) 
2018-10-26 | PXD005734 | Pride
Diffuse large B-cell lymphoma (DLBCL) is the most common aggressive B-cell lymphoma. Although many patients respond well to R-CHOP immunochemotherapy, those with the activated B-cell (ABC) subtype are often refractory or relapse. Bruton tyrosine kinase (BTK) inhibitors such as ibrutinib have improve...
ORGANISM(S): Homo sapiens 
The goal of this experiment was to identify the reaction site of Ibrutinib and 5Z-7-Oxozeaenol to ZAK by determination of mass shifts according to a covalent modification by the inhibitors using mass spectrometry.
ORGANISM(S): Homo sapiens (Human) 
2017-10-13 | PXD007752 | Pride
EGR1-mediated ibrutinib resistance
In this study, we investigated the target landscape of the drug ibrutinib using thermal proteome profiling (TPP) and proteoform detection. Our findings demonstrated that ibrutinib interacts with multiple proteoforms, beyond its known targets. Specifically, we identified interactions related to immun...
ORGANISM(S): Homo sapiens (Human) 
2024-11-24 | PXD047187 | Pride
Chronic lymphocytic leukaemia (CLL) is the most common haematological malignancy in developed countries. Ibrutinib (PCI-32765), a specific and irreversible inhibitor of Bruton's Tyrosine Kinase (BTK) represents a major step forward in the treatment of CLL, but cases of resistance are emerging. We ha...
ORGANISM(S): Homo sapiens 
Clonal evolution in CLL patients treated with ibrutinib
Chronic lymphocytic leukaemia (CLL) is the most common haematological malignancy in developed countries. Ibrutinib (PCI-32765), a specific and irreversible inhibitor of Bruton's Tyrosine Kinase (BTK) represents a major step forward in the treatment of CLL. We have undertaken a detailed analysis of t...
ORGANISM(S): Homo sapiens 
Mutations in PLCγ, a substrate of the tyrosine kinase BTK, are often found in patients who develop resistance to the BTK inhibitor Ibrutinib. However, the mechanisms by which these PLCγ mutations cause Ibrutinib resistance are unclear. Under normal signaling conditions, BTK mediated phosphorylation ...
ORGANISM(S): Rattus norvegicus (Rat) 
2022-01-19 | PXD028923 | Pride
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