Eukayotic protein kinases evolved as a family of highly dynamic molecules with strictly
organized internal architecture. A single hydrophobic F-helix serves as a central scaffold for …

For the past decade, the number of molecular targets for approved drugs has been debated.
Here, we reconcile apparently contradictory previous reports into a comprehensive survey …

Motivation In bioinformatics, machine learning-based methods that predict the compound–
protein interactions (CPIs) play an important role in the virtual screening for drug discovery …

The ATP site of kinases displays remarkable conformational flexibility when accommodating
chemically diverse small molecule inhibitors. The so-called activation segment, whose …

The majority of kinase inhibitors that have been developed so far—known as type I inhibitors—
target the ATP binding site of the kinase in its active conformation, in which the activation …

Synthesizing over thirty years of advances into a comprehensive textbook, Biomolecular
Crystallography describes the fundamentals, practices, and applications of protein …

The mitogen-activated kinases JNK1/2/3 are key enzymes in signaling modules that
transduce and integrate extracellular stimuli into coordinated cellular response. Here, we …

Background The stem cell factor receptor, KIT, is a target for the treatment of cancer,
mastocytosis, and inflammatory diseases. Here, we characterise the in vitro and in vivo …

Structure-based drug design is now used widely in modern medicinal chemistry. The
application of structural biology to medicinal chemistry has heralded the 'rational drug …

The Src, Syk, and Tec family kinases are three of the most well characterized tyrosine kinase
families found in the human genome. Members of these kinase families function …