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 …

In current scenario, various heterocycles have come up exhibiting crucial role in various
medicinal agents which are valuable for mankind. Out of diverse range of heterocycle …

Background: Ibrutinib is a Bruton tyrosine kinase inhibitor with remarkable efficacy against B-
cell cancers. Ibrutinib also increases the risk of atrial fibrillation (AF), which remains poorly …

Drugs with prolonged on-target residence times often show superior efficacy, yet general
strategies for optimizing drug-target residence time are lacking. Here we made progress …

Therapy based on Bruton's tyrosine kinase (BTK) inhibitors one of the major treatment
options currently recommended for lymphoma patients. The first generation of BTK inhibitor …

Introducing a reactive carbonyl to a scaffold that does not otherwise have an electrophilic
functionality to create a reversible covalent inhibitor is a potentially useful strategy for …

The discovery and development of targeted protein degraders have become important areas
of research in the field of medicinal chemistry. Inducing degradation of a target protein …

Bruton tyrosine kinase (BTK) is a key kinase in the B cell antigen receptor signal
transduction pathway, which is involved in the regulation of the proliferation, differentiation …

Simple Summary Dysregulated B-cell receptor (BCR) signaling is considered a potent
contributor to tumor survival in different subtypes of B-cell non-Hodgkin lymphomas (B …

New opportunities to advance small-molecule kinase ligands that downregulate their
cognate target binding proteins are discussed. Rationally designed heterobifunctional …