Practical Fragments

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

The shape of a molecule influences its properties. While this is true on a per-compound level, things get a little more controversial when d...

Lots of interesting events coming up this year - hope to see you at one! February 17-19 :  The  Twelfth NovAliX Conference  will be held fo...

As covalent drug discovery becomes increasingly common , researchers are becoming more rigorous in how they characterize their molecules. Th...

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

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

Earlier this year I wrote about archiving crystallographic fragment data, and indeed a meeting is planned for early next year to establish ...

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

Four years ago we highlighted a fragment-merging approach targeting fat mass and obesity-associated protein (FTO), an RNA demethylase impli...

Ligand efficiency ( LE ) has been discussed repeatedly and extensively on Practical Fragments , most recently in September . Two criticisms ...

Back in 2023 we highlighted a computational fragment linking/merging approach which was used to find high nanomolar inhibitors of the SARS-...

Many readers of this blog will be familiar with KRAS, a mutant form of which was successfully targeted a few years ago by a covalent, fragme...

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

Halogen bonds (or X-bonds) are one of the less appreciated protein-ligand interactions. As we discussed in 2022, the polarized nature of a ...

Ivermectin is a miracle drug. It cures infections caused by several types of parasitic roundworms, including those that cause river blindnes...

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,...