The evolving landscape of drug targets.
This Review map and quantify key elements of changes in the number and type of targets through which drugs mediate their therapeutic effects, which now include 686 biomolecules modulated by 1,702 drugs.
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This Review map and quantify key elements of changes in the number and type of targets through which drugs mediate their therapeutic effects, which now include 686 biomolecules modulated by 1,702 drugs.
Covalent probes and therapeutics must balance electrophilicity and stability for function in biological systems, yet gains in stability can sacrifice proteome coverage and limit ligand discovery. Here, we show that single-atom N-to-C substitutions of sulfonyl purines at the nucleofuge position decouple reactivity fro...
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