Light‐Induced Unlocking Reactivity of Fragments for Fast Target‐Guided Synthesis of Carbonic Anhydrase Inhibitors
Chloé Puteaux,
Isabelle Toubia,
Lina Truong
et al.
Abstract:We showcase the successful combination of photochemistry and kinetic target‐guided synthesis (KTGS) for rapidly pinpointing enzyme inhibitors. KTGS is a fragment‐based drug discovery (FBDD) methodology in which the biological target (BT) orchestrates the construction of its own ligand from fragments featuring complementary reactive functionalities. Notably, fragments interacting with the protein binding sites leverage their spatial proximity, facilitating a preferential reaction. Consequently, the resulting bi… Show more
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