Bruton's Tyrosine Kinase (BTK)

Bruton's Tyrosine Kinase Overview

Bruton's tyrosine kinase (BTK) is a cytoplasmic, non-receptor tyrosine kinase that plays a central role in the development, maturation, and signaling of B cells. It is essential for transmitting signals from the pre-B cell receptor after successful immunoglobulin heavy chain rearrangement. BTK's activation triggers several downstream pathways including Phospholipase C gamma 2, PI3K/Akt, and NF-kappaB. Mutations leading to loss-of-function of BTK cause X-linked agammaglobulinemia (XLA). Because malignant B cells often depend on active BTK signaling for survival and proliferation, small molecule inhibitors targeting BTK have become important therapies for various B-cell malignancies.

Mechanism of Action

Small molecule inhibitors that bind to and inhibit the enzymatic activity of BTK, preventing its phosphorylation of downstream targets and subsequent activation of signaling pathways.

Biological Functions

Safety Considerations

Interacting Drugs

Associated Biomarkers