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BTK

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

34 views | Jul 16 2019

Honigberg LA et al. support Btk inhibition as a therapeutic approach for the treatment of human diseases associated with activation of the BCR pathway. [Read the Full Post]

Ibrutinib for the treatment of chronic lymphocytic leukemia

138 views | Mar 30 2019

Novel, extremely promising, combination strategies, based on the association of ibrutinib with chemoimmunotherapy, antiCD20 monoclonal antibody or other targeted agents, are currently being investigated, with the goal of achieving greater depth of remission, especially MRD-negativity, and removing the need for indefinite treatment. [Read the Full Post]

A novel oncogenic BTK isoform is overexpressed in colon cancers and required for RAS-mediated transformation

532 views | Jul 20 2018

Grassilli E et al. revealed that BTK, via p65BTK expression, is a novel and powerful oncogene acting downstream of the RAS/MAPK pathway and suggest that its targeting may be a promising therapeutic approach. [Read the Full Post]

BTK inhibition is a potent approach to block IgE-mediated histamine release in human basophils

395 views | Jul 19 2018

Smiljkovic D et al. indicated that BTK-targeting drugs are potent inhibitors of IgE-dependent histamine release in human basophils. The clinical value of BTK inhibition in the context of allergic diseases remains to be determined. [Read the Full Post]

FcγRIIB mediates antigen-independent inhibition on human B lymphocytes through Btk and p38 MAPK

493 views | Jun 29 2018

Tzeng SJ et al. found the importance of antigen-independent inhibition by FcγRIIB in the prevention from antibody-mediated autoimmune diseases and in the regulation of B cell homeostasis. [Read the Full Post]

Substitution scanning identifies a novel, catalytically active ibrutinib-resistant BTK cysteine 481 to threonine (C481T) variant

0 views | Aug 04 2017

Hamasy A et al. identified three potential ibrutinib resistance scenarios for cysteine 481 replacement. [Read the Full Post]

Metalloproteinase-9 contributes to endothelial dysfunction in atherosclerosis via protease activated receptor-1

823 views | Jul 13 2017

Florence JM et al. demonstrated that metalloproteinase-9 could activate endothelial cells and induce their apoptosis via cleavage of protease activated receptor-1. In summary, better understanding of metalloproteinase-9's pathogenic capabilities as well as novel signaling pathways involved may lead to development of treatments which may provide additional benefits to atherosclerosis patients with a history of second hand smoke exposure. [Read the Full Post]

Reconstructing the temporal progression of HIV-1 immune response pathways

2048 views | Dec 13 2016

Jain S et al. experimentally validated several of TimePaths' predictions highlighting the usefulness of temporal models. [Read the Full Post]

Substitution scanning identifies a novel, catalytically active ibrutinib-resistant BTK cysteine 481 to threonine (C481T) variant

1157 views | Dec 11 2016

Hamasy A et al. identified three potential ibrutinib resistance scenarios for cysteine 481 replacement: (1) Serine, being catalytically active and therefore predominating among patients. (2) Threonine, also being catalytically active, but predicted to be scarce, because two nucleotide changes are needed. (3) As BTK variants replaced with other residues are catalytically inactive, they presumably need compensatory mutations, therefore being very scarce. [Read the Full Post]