Great talk by David Heppner (@heppnerd.bsky.social) at #CovModDrugDiscov.
He gave exciting insights into rigorously characterizing #CovalentInhibitors using crystal structures and kinetics.

@heppnerd.bsky.social
Medicinal Chemistry π | Drug Discovery π‘ | Cancer Biology π§« | Structural Biology 𧬠The State University of New York at Buffalo π¦¬
Great talk by David Heppner (@heppnerd.bsky.social) at #CovModDrugDiscov.
He gave exciting insights into rigorously characterizing #CovalentInhibitors using crystal structures and kinetics.
Greatly looking forward to joining this crew tomorrow!!
How can covalency be used in the most effective way to accelerate drug discovery?
I am very happy to be on the way to the conference "Covalent Modulation in Drug Discovery" by the @britpharmsoc.bsky.social in Cambridge to discuss this and related question in the coming two days.
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New work published today in @angewandtechemie.bsky.social (Very Important Paper) on gaining drug selectivity by "Thinking Outside the Binding Site." onlinelibrary.wiley.com/doi/10.1002/...
A p38 delta inhibitor achieved 12,000-fold greater selectivity by causing a flexible protein loop to kink and wrap around it. A distant amino acid helps stabilize this unusual fit. doi.org/hcjqf7