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ID: ALA3627636

Journal: Bioorg Med Chem Lett

Title: Novel bivalent inhibitors with sub-nanomolar affinities towards human glyoxalase I.

Authors: Sang Y, Shi Q, Mo M, Ni C, Li Z, Liu B, Deng Q, Creighton DJ, Zheng ZB.

Abstract: The zinc metalloenzyme glyoxalase I (GlxI) catalyzes the glutathione-dependent inactivation of cytotoxic methylglyoxal. Two competitive bivalent GlxI inhibitors, polyBHG2-62 (Ki=1.0 nM) and polyBHG2-54 (Ki=0.3 nM), were synthesized based on the transition-state analog S-(N-bromophenyl-N-hydroxycarbamoyl) glutathione (BHG). The most effective inhibitor, polyBHG2-54, is the first subnanomolar inhibitor of GlxI, and is over 50-fold more potent than BHG itself.

CiteXplore: 26320622

DOI: 10.1016/j.bmcl.2015.08.055