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Ref Type Journal Article
PMID (24658273)
Authors Hendriks RW, Yuvaraj S, Kil LP
Title Targeting Bruton's tyrosine kinase in B cell malignancies.
Journal Vol Issue Date Pages Journal Short Title
Nature reviews. Cancer 14 4 2014 Apr 219-32 Nat Rev Cancer
URL
Abstract Text Bruton's tyrosine kinase (BTK) is a key component of B cell receptor (BCR) signalling and functions as an important regulator of cell proliferation and cell survival in various B cell malignancies. Small-molecule inhibitors of BTK have shown antitumour activity in animal models and, recently, in clinical studies. High response rates were reported in patients with chronic lymphocytic leukaemia and mantle cell lymphoma. Remarkably, BTK inhibitors have molecular effects that cannot be explained by the classic role of BTK in BCR signalling. In this Review, we highlight the importance of BTK in various signalling pathways in the context of its therapeutic inhibition.

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Molecular Profile Treatment Approach
BTK over exp BTK inhibitor
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
BTK NCBI AGMX1|AT|ATK|BPK|IGHD3|IMD1|PSCTK1|XLA BTK, Bruton tyrosine kinase, is a non-receptor tyrosine kinase involved in B-cell activation and development (PMID: 24658273). BTK is commonly overexpressed in various hematological malignancies (PMID: 24658273) and BTK mutations have been linked to BTK inhibitor drug resistance (PMID: 28235842). Both: Oncogene and Tumor suppressor
Therapy Name Drugs Efficacy Evidence Clinical Trials
CNX-774 CNX-774 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
CNX-774 BTK inhibitor 39 CNX-774 is a small molecule that binds BTK and prevents its kinase activity (PMID: 24658273, PMID: 28328081).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References