Activation of bruton's tyrosine kinase (BTK) by a point mutation in …
1995年5月1日 · Using a random mutagenesis scheme, we isolated a gain-of-function mutant called BTK* whose expression drives growth of NIH 3T3 cells In soft agar. BTK* results from a …
Dissection of the Effects of JAK and BTK Inhibitors on the ...
2019年10月15日 · We compared functional effects of the JAK1/2 inhibitors momelotinib and ruxolitinib, the BTK inhibitors ibrutinib and tirabrutinib, and PI3Kδ inhibitor idelalisib on …
Phosphatidylinositol 3-Kinase-dependent Membrane …
1999年4月16日 · In NIH 3T3 cells coexpressing BtkPH-GFP and the epidermal growth factor receptor, activation of epidermal growth factor or endogenous platelet-derived growth factor …
Human T-bet+ B cell development is associated with BTK activity …
2022年8月8日 · Recent clinical trials have shown promising results for the next-generation Bruton’s tyrosine kinase (BTK) inhibitor evobrutinib in the treatment of multiple sclerosis (MS). …
In BTK, phosphorylated Y223 in the SH3 domain mirrors catalytic ...
2024年4月23日 · We gene-edited mice substituting tyrosine 223 for nonphosphorylatable phenylalanine and found no difference from wild-type animals. Bruton’s tyrosine kinase (BTK) …
Wild-type Btk and Btk* were expressed in NIH 3T3 cells by retroviral infection. Following in vivo 32P-orthophos-phate labeling, Btk proteins were immunoprecipitated from cell extracts and …
PKCβ modulates antigen receptor signaling via regulation of Btk ...
2001年10月15日 · We provide direct evidence that PKCβ acts as a feedback loop inhibitor of Btk activation. Inhibition of PKCβ results in a dramatic increase in B‐cell receptor (BCR)‐mediated …
Discovery of new non-covalent reversible BTK inhibitors: …
2024年11月1日 · Bruton's Tyrosine Kinase (BTK) played a key role in the B cell antigen receptor (BCR) signaling pathway, and was considered a hotspot in the treatment of B cell malignant …
Targeted Protein Degradation of BTK As a Unique Therapeutic …
2019年11月13日 · We have identified multiple CTMs that catalyze BTK degradation in multiple B cell lines; the concentration of one of such CTM, NRX0492, required to degrade 50% BTK (DC …
PROTAC-induced BTK degradation as a novel therapy for mutated BTK …
2018年6月6日 · In this study, for the first time, we report the development of BTK-targeting degraders using the PROTAC strategy. These PROTACs could efficiently degrade ibrutinib …