Practical Fragments

The first FBDD-related meeting of 2016 has already come and gone, but there are still plenty of events ahead. Below are several updates as w...

Epigenetics involves turning genes on or off without changing their sequence. This often relies on modifications to proteins or DNA that a...

Among NMR-based fragment screening methods, saturation transfer difference ( STD ) came in as most popular in a recent poll . The technique...

It’s a common problem: you find a fragment that binds to your target and want to grow it to improve affinity. A search for commercial analo...

In 2006, Wolfgang Jahnke and I co-edited the very first book on fragment-based drug discovery. Half a dozen books have followed, most of w...

Plasmodium , which causes malaria, is a nasty bag of tricks. These include the plasmepsins, aspartic proteases that – among other duties – ...

One of the less commonly used fragment-finding methods is microscale thermophoresis ( MST ). This measures the movement of proteins in a t...

A couple years ago we highlighted a paper from Eddy Arnold’s group at Rutgers University in which crystallographic fragment screening reve...

Anyone who has been exposed to much crystallography will have seen examples where a ligand binds somewhere besides the active site of a pro...

Happy 2016! This looks like a good year for fragment events, so start planning now! February 21-24 :  Zing conferences is holding its inau...

In the Northern Hemisphere the winter solstice has passed but the days are still short, and 2015 is hurtling into history. As we did in 201...

Last week saw the first-ever fragment-based symposium at Pacifichem . These are massive meetings held in Honolulu every 5 years to bring to...

The mitogen-activated protein kinase (MAPK) signaling pathway is a rich source of targets, particularly for inflammation. Within this casca...

Independent teams have reported using fragments to identify structurally distinct inhibitors against a popular psychiatric target. Last...

G protein-coupled receptors (GPCRs) are common drug targets that present challenges for fragment-based approaches. Biophysical studies of t...

Computational approaches for discovering hits often involve sorting through many possibilities and examining a few closely. With luck, some...

People often wonder how selective fragments need to be. According to molecular complexity theory , the answer is “not very”. After all, it ...