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New Opportunities In Covalent Inhibition: Targeting Lysine

Targeting-Lysine

(This post originally appeared on LinkedIn)

 

Notoriously toxic, covalent inhibitors have been nearly excluded from major drug discovery programs in the not so distant past. Ironically, a great amount of the important drugs exploit covalent inhibition as their mechanism of action (MOA). The view on covalent inhibitors is shifting towards a wider consideration, however, inspired by recent successes with EGFR inhibitors for treating cancer and many other promising examples. A recent publication in Nature provides a chemical proteomic platform for the global and quantitative analysis of lysine residues in native biological systems, offering further insights and ideas in this area.

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