Practical Fragments

RNA helicases present an intriguing but challenging opportunity for drug discovery. Their importance for cell growth makes them attractive c...

Last week we highlighted a study in which an attempt to optimize a covalent fragment led to a non-covalent fragment that bound in a differe...

Werner syndrome helicase, or WRN, is an interesting target both for its biological mechanism and its flexible structure. Two years ago we hi...

Despite its ubiquitous use as a model organism, Escherichia coli causes nearly a million deaths each year worldwide. Antibiotics provoke ra...

Last week some 875 people attended the CHI Drug Discovery Chemistry ( DDC ) meeting in San Diego. I can’t do justice to the 40 or so present...

Last week we highlighted work out of Steve Fesik’s lab at Vanderbilt University about PLPro. This week we’ll highlight another paper just p...

The most successful drug against COVID-19, nirmatrelvir, targets the main protease of SARS-CoV-2. As we discussed just last year, this prot...

Last month we highlighted a paper from Iwan de Esch and colleagues at Vrije Universiteit Amsterdam about assessing molecular shapeliness....

The YEATS domain of the protein GAS41 is an epigenetic reader that modulates gene expression by binding to acetylated lysine residues in chr...

Synthetic lethality is a relatively new approach to treating cancer by targeting proteins whose inhibition is lethal to cancer cells that h...

As our poll last year demonstrated, there is no shortage of methods to find fragments. But that doesn’t mean new approaches aren’t welcome,...