Over the past decade, therapeutics that target subsets of the 518 human protein kinases
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …

Recent studies on cyclin-dependent kinase (CDK) inhibitors have revealed that small
molecule drugs have become very attractive for the treatment of cancer and …

DNA-templated organic synthesis enables the translation of DNA sequences into synthetic
small-molecule libraries suitable for in vitro selection. Previously, we described the DNA …

Bisubstrate inhibitors consist of two conjugated fragments, each targeted to a different
binding site of a bisubstrate enzyme. The design of bisubstrate inhibitors presupposes the …

Fibroblast growth factor receptors (FGFRs) are implicated in a range of cancers with several
pan-kinase and selective-FGFR inhibitors currently being evaluated in clinical trials. Pan …

Many members of the protein kinase family have emerged as key targets for
pharmacological intervention, most notably in cancer. However, the high sequence and …

As described in the previous chapter, most kinase inhibitors that have been developed for
use in the clinic act by blocking ATP binding; however, there is growing interest in identifying …

Protein kinases are key players in a large number of cellular signaling pathways.
Dysregulated kinase activity has been implicated in a number of diseases, and members of …

Bivalent molecules consisting of groups connected through bridging linkers often exhibit
strong target binding and unique biological effects. However, developing bivalent inhibitors …

Identifying the protein targets of bioactive small molecules remains a major problem in the
discovery of new chemical probes and therapeutics. While activity-based probes and photo …