Eszter Boros

Metal-Dependent Coordination Geometry Controls Autolytic Amide Bond Cleavage to Enable Prodrug Activation

Abstract We introduce a peptide prodrug activation strategy that employs the trivalent Lewis-acidic metal ions Ga3+, Fe3+, In3+, and Co3+, chelated by triazacyclononanediacetic acid monoamides. The metal chelates trigger rate-tunable, metal-mediated, autolytic amide bond cleavage...

Rational Design of a Synthetic Galliphore for the Diagnostic Nuclear Imaging and Treatment of Bacterial Infections

ABSTRACT We introduce a solid‐phase synthesis platform for the rapid, modular, and scalable synthesis of the synthetic metallophore KO‐NH 2 , which is readily recognized by bacterial siderophore transporters, but has optimized affinity for Ga 3+ over Fe 3+ . Four synthetic protoc...