Single cell imaging of Bruton's Tyrosine Kinase using an irreversible inhibitor [PDF]
A number of Bruton's tyrosine kinase (BTK) inhibitors are currently in development, yet it has been difficult to visualize BTK expression and pharmacological inhibition in vivo in real time.
Kim, Eunha +4 more
core +1 more source
ABSTRACT Introduction Novel targeted agents have transformed the treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), including continuous BTK inhibitor (BTKi) therapy and time‐limited regimens such as venetoclax‐obinutuzumab (Ven‐O) and ibrutinib‐venetoclax (I + V).
Rebecca Tidswell +7 more
wiley +1 more source
Proliferation tracing with single-cell mass cytometry optimizes generation of stem cell memory-like T cells. [PDF]
Selective differentiation of naive T cells into multipotent T cells is of great interest clinically for the generation of cell-based cancer immunotherapies. Cellular differentiation depends crucially on division state and time.
Bendall, Sean C +7 more
core
ABSTRACT The GAIA‐CLL13 trial showed that venetoclax‐obinutuzumab (Ven‐O) based regimens, with or without ibrutinib, offer superior efficacy compared to chemoimmunotherapy (CIT) with regards to progression free survival (PFS) in fit, treatment‐naïve (TN) CLL patients. However, their higher costs warrant a cost‐effectiveness evaluation.
Lars Holger Ehlers +6 more
wiley +1 more source
HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib [PDF]
Activating mutations in MYD88 are present in approximately 95% of patients with Waldenstrom Macroglobulinemia (WM), as well as other B-cell malignancies including ABC DLBCL. In WM, mutated MYD88 triggers activation of BTK. Ibrutinib, a pleiotropic kinase
Advani +60 more
core +2 more sources
Acalabrutinib in Chronic Lymphocytic Leukemia: Pharmacology and Emerging Clinical Perspectives
ABSTRACT Acalabrutinib, a second‐generation Bruton's tyrosine kinase inhibitor (BTKi), is characterized by enhanced specificity and selectivity for BTK with minimal off‐target effects, offering a significant evolution in the treatment of chronic lymphocytic leukemia (CLL). Its mechanism of action, a covalent binding to Cys481 within the BTK active site,
Gianluca Gaidano, Romano Danesi
wiley +1 more source
Real-world clinical experience in the Connect® chronic lymphocytic leukaemia registry: a prospective cohort study of 1494 patients across 199 US centres. [PDF]
The clinical course of chronic lymphocytic leukaemia (CLL) is heterogeneous, and treatment options vary considerably. The Connect® CLL registry is a multicentre, prospective observational cohort study that provides a real-world perspective on the ...
Farber, Charles M +15 more
core +1 more source
ABSTRACT Primary refractory Diffuse Large B‐Cell Lymphoma is associated with poor outcomes and limited responsiveness to conventional salvage therapies. Although CAR T‐cell therapy represents the standard of care in this setting, a substantial proportion of patients cannot receive it despite meeting disease‐related criteria. In this review, “unsuitable”
Santino Caserta +12 more
wiley +1 more source
Prolonged and tunable residence time using reversible covalent kinase inhibitors. [PDF]
Drugs with prolonged on-target residence times often show superior efficacy, yet general strategies for optimizing drug-target residence time are lacking.
Angelina Bisconte +23 more
core
MicroRNA-214 targets PTK6 to inhibit tumorigenic potential and increase drug sensitivity of prostate cancer cells. [PDF]
Prostate cancer is the most commonly diagnosed cancer in men with African American men disproportionally suffering from the burden of this disease.
Aqeel, Rasha +10 more
core +1 more source

