Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Bruton's tyrosine kinase (BTK) is an essential component of multiple signaling pathways that
regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising …

Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …

Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

The cytoplasmic protein-tyrosine kinase BTK plays an essential role for differentiation and
survival of B-lineage cells and, hence, represents a suitable drug target. The number of BTK …

Aberrant activation of Bruton's tyrosine kinase (BTK) plays an important role in pathogenesis
of B-cell lymphomas, suggesting that inhibition of BTK is useful in the treatment of …

Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

Background Irreversible inhibition of Bruton's tyrosine kinase (BTK) by ibrutinib represents
an important therapeutic advance for the treatment of chronic lymphocytic leukemia (CLL) …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Targeted protein degradation using the PROTAC technology is emerging as a novel
therapeutic method to address diseases driven by the aberrant expression of a disease …