Article

Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms

2019-12-10

Abstract excerpt

<h4>ABSTRACT</h4> Bruton’s tyrosine kinase (Btk) is a key component for B-cell maturation and activation. Btk loss-of-function mutations cause human X-linked agammaglobulinemia (XLA). In contrast, constitutive Btk signaling drives several B-cell neoplasms, which may be treated with tyrosine kinase inhibitors (TKIs). Here, we uncovered the molecular mechanism by which a subset of XLA mutations in the SH2 domain st...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: c9a2a584-23ac-5033-9dcf-e62dade95755
DOI: 10.1101/862276

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasmsDOI 10.1101/862276Read

Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms.Semantic proximity Read

Bruton tyrosine kinase (BTK) in X-linked agammaglobulinemia (XLA).Semantic proximity Read

A regulatory SH2 domain-targeting protein binder effectively inhibits the activity of Bruton's tyrosine kinase and its drug-resistant variants.Semantic proximity Read

Screening and Characterization of Allosteric Small Molecules Targeting Bruton's Tyrosine Kinase.Semantic proximity Read

Bruton's tyrosine kinase: from X-linked agammaglobulinemia toward targeted therapy for B-cell malignancies.Semantic proximity Read

TEC family kinases in health and disease--loss-of-function of BTK and ITK and the gain-of-function fusions ITK-SYK and BTK-SYK.Semantic proximity Read

X-linked agammaglobulinemia (XLA): a genetic tyrosine kinase (Btk) disease.Semantic proximity Read

Differential impact of BTK active site inhibitors on the conformational state of full-length BTK.Semantic proximity Read

Role of Bruton’s tyrosine kinase in B cells and malignanciesSemantic proximity Read

Computational insights into mutation-induced binding changes in Bruton's Tyrosine Kinase with non-covalent inhibitors.Semantic proximity Read

More than an attachment module: covalent inhibitor warheads influence BTK dynamics and functionSemantic proximity Read

The SH3 domain of Bruton's tyrosine kinase interacts with Vav, Sam68 and EWS.Semantic proximity Read