Explore
Home 
Literature 
Links 
Posts 
Molecules 
Blogs 
Zeitgeist 
Markup Help 
News 
All posts Reviews Conferences Research

Posts linking to this one

A special case of fragment linking is dimerization, in which two copies of the same fragment bind to adjacent sites in a protein and are subsequently linked together (see for example here, here, and here). A recent example was published in J. Med. Chem. by...
Our latest poll (please vote on the right-hand side of the page!) is about fragment libraries. Once you have your library, you can screen it using a variety of approaches. But what do you do once you get hits? Computational methods are increasingly being adopted;...
The first fragment-based drug to reach the market, vemurafenib, targets a mutant form of the kinase BRAF. Initial responses can be miraculous, but metastatic melanoma is an implacable foe, and patients often relapse. One mechanism of resistance involves...
A common question in library design concerns novelty: should you populate your library with custom-made, hitherto unseen molecules, or just buy off-the shelf compounds? While the first strategy might make it easier to get patentable leads, the second approach...
Multiple clinical candidates derived from fragments were described at the recent CHI FBDD Meeting. The story behind one of these has just appeared in J. Med. Chem. in a paper published by Siegfried Reich and colleagues at eFFECTOR Therapeutics.The researchers...
As mentioned last week, CHIs FBDD Meeting was chock-full of success stories. Some of these have recently been published, including work in J. Med. Chem. by Jenny Viklund (Sprint Biosciences) and collaborators at Bayer, the University of Oxford, and the Structural...
Membrane-bound proteins such as GPCRs are often ignored by practitioners of FBLD in part because Heptares notwithstanding they are usually difficult to characterize structurally. This seems like a missed opportunity. A large fraction of drugs target GPCRs,...
The enzyme lipoprotein-associated phospholipase A2 (Lp-PLA2) cleaves phospholipids into inflammatory molecules. As such, it has been pursued as a target for several indications, from atherosclerosis to Alzheimers disease. In 2016 we highlighted two fragment...
The year is done, and the darknessFalls from the wings of Night.As we've done since 2012, Practical Fragments is using the last post of the year to highlight conferences as well as reviews not previously discussed.Significant events included the venerable CHI...
A common assumption in fragment growing is that the binding mode of the fragment remains the same throughout optimization (for example here, here, and here). However, this is not always the case (as described here, here, and here). A recent paper in Bioorg....