Results 21 to 30 of about 7,833 (210)

PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors.

open access: yesPLoS ONE, 2017
Activated B-cell-like diffuse large B-cell lymphoma relies on B-cell receptor signaling to drive proliferation and survival. Downstream of the B-cell receptor, the key signaling kinases Bruton's tyrosine kinase and phosphoinositide 3-kinase δ offer ...
Anella Yahiaoui   +9 more
doaj   +1 more source

The role of B-cell receptor inhibitors in the treatment of patients with chronic lymphocytic leukemia

open access: yesHaematologica, 2015
Chronic lymphocytic leukemia is a malignancy of mature auto-reactive B cells. Genetic and functional studies implicate B-cell receptor signaling as a pivotal pathway in its pathogenesis.
Adrian Wiestner
doaj   +1 more source

A covalent BTK ternary complex compatible with targeted protein degradation

open access: yesNature Communications, 2023
Bridging covalent ligand discovery with chimeric degrader design has emerged as a mechanism to target proteins that lack enzymatic activity or are intractable.
James Schiemer   +8 more
doaj   +1 more source

Switching immune signals on and off

open access: yeseLife, 2015
Bruton's tyrosine kinase, an enzyme that is important for B cell function, can be activated in a number of ways.
Nam Chu, Philip A Cole
doaj   +1 more source

Current understanding of tyrosine kinase BMX in inflammation and its inhibitors

open access: yesBurns & Trauma, 2014
Tec family kinases, which include tyrosine kinase expressed in hepatocellular carcinoma (TEC), Bruton's tyrosine kinase (BTK), interleukin (IL)-2-inducible T-cell kinase (ITK), tyrosine-protein kinase (TXK), and bone marrow tyrosine kinase on chromosome ...
Le Qiu, Fei Wang, Sheng Liu, Xu-Lin Chen
doaj   +1 more source

Mechanism of Covalent Binding of Ibrutinib to Bruton’s Tyrosine Kinase revealed by QM/MM Calculations

open access: yes, 2020
Ibrutinib is the first covalent inhibitor of Bruton’s tyrosine kinase (BTK) to be used in the treatment of B-cell cancers. Understanding the mechanism of covalent inhibition is crucial for the design of safer and more selective covalent inhibitors that ...
Angus, Voice   +4 more
core   +1 more source

ANKRD54 preferentially selects Bruton's Tyrosine Kinase (BTK) from a Human Src-Homology 3 (SH3) domain library. [PDF]

open access: yesPLoS ONE, 2017
Bruton's Tyrosine Kinase (BTK) is a cytoplasmic protein tyrosine kinase with a fundamental role in B-lymphocyte development and activation. The nucleocytoplasmic shuttling of BTK is specifically modulated by the Ankyrin Repeat Domain 54 (ANKRD54) protein
Manuela O Gustafsson   +8 more
doaj   +1 more source

A ROR1 small molecule inhibitor (KAN0441571C) induced significant apoptosis of ibrutinib‐resistant ROR1+ CLL cells

open access: yeseJHaem, 2021
ROR1 – a receptor tyrosine kinase – is overexpressed in CLL. Ibrutinib, a Bruton's tyrosine kinase inhibitor, is clinically effective in CLL but patients may develop resistance. We evaluated the effect of an ROR1 inhibitor, KAN0441571C, in CLL cells from
Amineh Ghaderi   +9 more
doaj   +1 more source

Bruton’s Tyrosine Kinase Inhibitors: A New Generation of Promising Agents for Multiple Sclerosis Therapy

open access: yes, 2021
B cells play a central role in the pathogenesis of multiple sclerosis (MS), as demonstrated through the success of various B cell-depleting monoclonal antibodies.
Antonio García-Merino
core   +1 more source

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

open access: yesNature Communications, 2020
PROTACs have emerged as promising therapeutic agents but their cellular uptake is often inefficient. Here, the authors show that reversible covalent warhead chemistry improves PROTAC intracellular accumulation and target engagement, and develop a dual ...
Wen-Hao Guo   +18 more
doaj   +1 more source

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