Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

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

INTRODUCTION Molecularly targeted drugs such as imatinib and crizotinib have
revolutionized the treatment of certain blood and lung cancers because of their remarkable …

Medicinal chemistry has discovered thousands of potent protein and lipid kinase inhibitors.
These may be developed into therapeutic drugs or chemical probes to study kinase biology …

Imiquimod is a small-molecule ligand of Toll-like receptor-7 (TLR7) that is licensed for the
treatment of viral infections and cancers of the skin. Imiquimod has TLR7-independent …

Metabolism research is undergoing a renaissance because many diseases are increasingly
recognized as being characterized by perturbations in intracellular metabolic regulation …

Drugs that target histone deacetylase (HDAC) entered the pharmacopoeia in the 2000s.
However, some enigmatic phenotypes suggest off-target engagement. Here, we developed …

The RAF family kinases function in the RAS–ERK pathway to transmit signals from activated
RAS to the downstream kinases MEK and ERK. This pathway regulates cell proliferation …

For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological
mechanism. Although a number of acellular techniques have been developed to measure …

Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in
immunity and is considered an attractive target for treating autoimmune diseases. The use of …