The number of ways to find fragments just keeps growing. A few weeks ago we discussed WAC, which takes its place alongside ITC, SPR, MS, TINS, and more traditional methods such as NMR, X-ray and biochemical screening. However, all of these approaches are somewhat reductionist, relying on isolated target proteins. In an effort to bring the whole organism into the picture, our friends at the University of Shutka, Russia, have come up with an approach they call “Fragments in Bodies,” or FIB.
The researchers have assembled a collection of very small fragments, purchased for the most part from Lilliput Pharmaceuticals. These are then screened in mouse models to look for positive phenotypic effects.
The researchers face some unique challenges. For example, it is difficult to measure changes in body mass as the animals need to consume such large amounts of fragments that they can become somewhat bloated. Still, if the animals can be safely dosed with massive amounts of micro-molecules, "FIB"ing could provide very good starting points for further work!
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2 comments:
This technique really seems to be taking off, I've already heard quite a few FIBs today. I wouldn't be surprised if FIBing was the next big thing in drug discovery!
Although this post was an April Fools’ joke, perhaps it is not as crazy as it sounds. We previously highlighted an example of fragment-screening in bacterial cells, and last year Dyeison Antonow published an editorial in Drug Discovery Today suggesting that prodrugs could be designed that would self-assemble in vivo.
Practical Fragments’ first April Fools’ post was inadvertently close to actual research. Perhaps life will imitate art (or science will imitate fancy) again!
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