Practical Fragments

There are many great testaments to humanity's perseverance.   The Pyramids at Giza , the Cathedral of Notre Dame , the Great Wall of Chi...

Our latest poll asked just this question. We received 72 responses, and the results are shown here. Almost half of respondents said ...

Docking can sometimes seem like the Rodney Dangerfield of FBDD: it don’t get no respect. In last year’s poll of fragment finding methods,...

Anyone who has paid any attention to health news will be aware of concerns over high fructose corn syrup . Just a few years ago the stuff w...

Last year we discussed the application of dynamic combinatorial chemistry ( DCC ) to fragment linking. The idea is that a protein will shif...

The cyclin-dependent kinases ( CDKs ) are targets for a variety of diseases, particularly cancers. One of the earliest posts at Practical ...

The kinase CK2 is an intriguing anti-cancer target, but most of the reported inhibitors bind in the conserved hinge region and so also hi...

Chirality underpins all life. Nineteen of the twenty amino acids contain at least one stereocenter , as do all nucelosides, sugars, and mo...

What do you do when you find a fragment? After checking for artifacts and getting as much structural information as possible, the next ste...

Five years ago Teddy highlighted a paper from GlaxoSmithKline that reported the discovery and characterization of several different fragme...

Last year we highlighted a paper from academia in which modeling was used to discover potent inhibitors of the lysine demethylase KDM4C, a...

As discussed last year, secondary binding sites on proteins appear to be quite common. Some of these sites have no functional relevance, b...

Ligandability refers to the ability to find small-molecule leads against a target. A protein might be ligandable but not druggable if, for...

Of the more than 30 fragment-derived drugs that have entered clinical development , more than a third target kinases. While most of these a...

Last month we highlighted how fragments could be used to discover inhibitors of protein-protein interactions (PPIs). Today we continue the...

Native electrospray ionization mass spectrometry (ESI-MS) is one of the less-commonly used fragment finding methods . The technique relies ...

Covalent drugs are a thing these days: as long as you can get selectivity, there’s nothing like a covalent bond to juice up affinity for a ...

The year is halfway behind us, but there are still a couple upcoming fragment-based events, and next year is already taking shape. 2017 ...

Disrupting protein-protein interactions (PPIs) tends to be challenging: interfaces are often large and flat, with few deep pockets in which...

Bromodomains, epigenetic targets that recognize acetylated lysine residues, have received considerable attention from the fragment communit...