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...

Exactly 17 years ago, I  highlighted a paper from Brian Shoichet’s lab in which he hypothesized that only tiny regions of chemical space ar...

Last year we highlighted a paper out of Novartis describing a fragment-to-lead story for interleukin-1 beta (IL-1β), a pro-inflammatory cyt...

The annual Practical Fragments look-back on the preceding year may not be the most highly anticipated year-end tradition, but I hope you f...

Roughly speaking there are three ways to advance fragments to leads: growing, linking, or merging. Growing is the most common , but as the n...

With all the attention on COVID-19 over the past few years, it’s easy to forget about bacteria. But they haven’t forgotten about us. Indeed,...

The winter solstice is behind us in the Northern Hemisphere, which means 2022 is rapidly drawing to a close. As we have done for the past d...

Virtual screening is continuing to make impressive strides. The latest example , in Nature , comes from William Wetsel (Duke), John Irwin (...

Fragment-based screening is often funnel-shaped: a virtual screen might identify dozens or hundreds of potential hits that are tested in var...

Four of the six approved fragment-derived drugs are kinase inhibitors, and three of these bind in the active site. Despite these successes,...

The drugging of HIV-1 protease is a classic structure-based design success story, as discussed in a guest post by Glyn Williams from the ea...

Wnt proteins are implicated in a variety of diseases, from Alzheimer’s to colorectal cancer. The enzyme Notum shuts down signaling by removi...

Today marks exactly two years since Practical Fragments first mentioned SARS-CoV-2. Since then, COVID-19 has killed more than 6 million pe...