Of R415 and R483 were accompanied by major differences in affinityīetween ligands. Significantly altered thermodynamic profile. Of a coordinated water molecule from the Keap1 binding site and a Ligand optimization resulted in the displacement Units for productive interactions with key residues of Keap1, including The macrocyclic core of the nanomolar inhibitors positions three pharmacophore Optimization, resulted in a 100-fold improvement in inhibitory potency. Of the structure-activity relationship of the lead, followed by structure-guided We reportĪ structurally unique series of nanomolar Keap1 inhibitors obtainedįrom a natural product-derived macrocyclic lead. ![]() ![]() The interaction with its negative regulator Keap1 constitutes an opportunityįor the treatment of disease caused by oxidative stress. Transcription factor Nrf2 by inhibition of
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