Practical Fragments

The protein β-glucocerebrosidase, also called GCase and GBA, is a lysosomal enzyme that cleaves glucosylceramide. People with inactivating m...

Practical Fragments has covered bromodomains extensively, most recently just a couple months ago. But these epigenetic readers are not the...

COVID-19 is deservedly engaging most of our collective mindspace when it comes to infectious diseases. Unfortunately, plenty other threats...

Just over a decade ago Ernesto Freire suggested that small molecules whose binding energy is dominated by the enthalpic – rather than the e...

Most drugs – and small molecule modulators in general – inhibit something, often an enzyme. Enzyme activation , on the other hand, is rare;...

Epigenetic readers recognize modified amino acids in histone proteins to cause changes in gene expression. Readers containing bromodomains,...

This year is finally coming to an end, and as we've done for the past four years , Practical Fragments will highlight some of the r...

Three years ago we highlighted work out of Chris Abell’s lab at the University of Cambridge targeting CYP121, an important enzyme for the ...

Protein-protein disruptions are notoriously difficult because the interfaces between proteins tend to be large and flat, with few of the de...

Today’s post continues the theme of July as bromodomain month at Practical Fragments . The 61 human bromodomains (found in 46 proteins – ...

As we mentioned last week, July is bromodomain month at Practical Fragments . Today we’ll start by looking at two closely related bromodo...

Biophysics and fragment-based drug discovery go together like Nutella and strawberries. Indeed, SAR by NMR ushered in the dawn of fragment...

Fragment linking, growing, and merging: these are the main methods for enhancing affinity. Two years ago we highlighted a fragment screeni...

Science is based upon incremental advances of previous work.  A year ago, Dan blogged about worked on BioA.  The key take home from that wo...

As we’ve noted ( repeatedly ), epigenetics is big. However, much of the focus has been on bromodomains , which recognize acetylated lysine...

Two years ago we highlighted a paper in which Cambridge University researchers identified fragments that bind to the protein RAD51, which ...

About half of all approved drugs are small molecules that inhibit enzymes. This makes sense intuitively: an enzyme is like a complicated li...

So, not everybody agrees with me on what a fragment is .  As has been pointed out years ago, FBDD can be a FADD .  In this paper , from ea...