The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Currently, humans are immersed in a pandemic caused by the emerging severe acute
respiratory syndrome coronavirus 2 (SARS-CoV-2), which threatens public health …

Current methods used for measuring amino acid side-chain reactivity lack the throughput
needed to screen large chemical libraries for interactions across the proteome. Here we …

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 …

Small molecule covalent kinase inhibitors (CKIs) have entered a new era in drug discovery,
which have the advantage for sustained target inhibition and high selectivity. An increased …

The emerging use of covalent ligands as chemical probes and drugs would benefit from an
expanded repertoire of cysteine-reactive electrophiles for efficient and diverse targeting of …

The ERK pathway is one of the most important signaling cascades involved in
tumorigenesis. So far, eight noncovalent inhibitors of RAF and MEK kinases in the ERK …

Abstract Adaptor-Associated Kinase 1 (AAK1), a Ser/Thr protein kinase, responsible for
regulating clathrin-mediated endocytosis, is ubiquitous in the central nervous system (CNS) …

Protein kinases are essential mediators of cellular signal transduction and are often
dysregulated in disease. Among these, protein tyrosine kinases (PTKs) have received …

Proteins form complex biological machineries whose functions in the cell are highly
regulated at both the cellular and molecular levels. Cellular regulation of protein functions …