Practical Fragments

We’ve written previously about the concept of synthetic lethality, in which changes to one protein make cancer cells more dependent on anot...

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

Last month Practical Fragments wrote about make-on-demand libraries, such as those offered by Enamine. We’ve also written about fluorine-...

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 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 week the Twelfth Novalix Biophysics in Drug Discovery Conference was held for the first time in La Jolla, California. It’s been severa...

Transcription factors can be difficult drug targets, particularly those whose primary structure is a “leucine zipper” in which two α -helice...

Turning and turning in the widening gyre The falcon cannot hear the falconer…   In our small, annual counterweight to Yeats’ “ mere a...

As noted in our poll last year, ligand-detected NMR ranks among the most popular fragment-finding approaches. The various methods are able ...

Migraines are the third leading cause of disability worldwide. Although the pathology is complex, blocking the interaction of calcitonin gen...

Last week we highlighted work suggesting that small molecule binding sites in RNA are most likely to be found in complex structures. A new ...

At the Drug Discovery Chemistry meeting last month chemist John Taylor described efforts against the oncology target RAS. This story was re...

Last week we highlighted a protein-detected NMR method that does not require expensive and sometimes difficult isotopic labeling of protein...