Over the past 25 years, biophysical technologies such as X-ray crystallography, nuclear
magnetic resonance spectroscopy, surface plasmon resonance spectroscopy and …

It is over 20 years since the first fragment-based discovery projects were disclosed. The
methods are now mature for most 'conventional'targets in drug discovery such as enzymes …

NMR spectroscopy is currently extensively used in binding assays for hit identification, but its
use in dissociation constant determination is more limited when compared to other …

Fragment-based drug discovery (FBDD) has emerged in the past decade as a powerful tool
for discovering drug leads. The approach first identifies starting points: very small molecules …

In his philosophic musings “Meditations” the Emperor Marcus Aurelius asks “This thing, what
is it in itself, in its own constitution? What is its substance and material? And what its causal …

In the past 15 years, fragment-based lead discovery (FBLD) has been adopted widely
throughout academia and industry. The approach entails discovering very small molecular …

Inhibitors of the Hsp90 molecular chaperone are showing considerable promise as potential
molecular therapeutic agents for the treatment of cancer. Here we describe novel 2 …

Recognizing acetyllysine of histone is a vital process of epigenetic regulation that is
mediated by a protein module called bromodomain. To contribute novel scaffolds for …

The serine/threonine kinase DYRK1A has been implicated in regulation of a variety of
cellular processes associated with cancer progression, including cell cycle control, DNA …

Fragment-based methods have emerged as a new strategy for drug discovery. The main
advantages are that useful starting points for lead identification for most targets can be …