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Message History

Exactly 17 years ago, I highlighted a paper from Brian Shoichet’s lab in which he hypothesized that only tiny regions of chemical space are biologically relevant. If so, Practical Fragments quoted, “a major reason why ...

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Last week we highlighted a study in which an attempt to optimize a covalent fragment led to a non-covalent fragment that bound in a different location. A new open-access

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The seven members of the 14-3-3 family act as “hub proteins” that bind to other proteins, bringing them together or affecting their subcellular localization. Some of the client proteins, such as estrogen receptor alpha (ERα), are associated with diseases such as cancer, and stabilizing the interaction with 14-3-3 could thus be useful therapeutically. The idea is that a small “mo...

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Just over two years ago we highlighted a new clinical candidate targeting WRN, a covalent inhibitor then called VVD-133214. An open-access 

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