Browsing Biology by Subject "Structure-Activity Relationship"
Now showing items 1-4 of 4
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10 years into the resurgence of covalent drugs.
(2021-01)In the first decade of targeted covalent inhibition, scientists have successfully reversed the previous trend that had impeded the use of covalent inhibition in drug development. Successes in the clinic, mainly in the field ... -
Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity
(American Chemical Society (ACS), 2018-10-11) -
Targeting the substrate preference of a type I nitroreductase to develop antitrypanosomal quinone-based prodrugs.
(2012-11)Nitroheterocyclic prodrugs are used to treat infections caused by Trypanosoma cruzi and Trypanosoma brucei. A key component in selectivity involves a specific activation step mediated by a protein homologous with type I ...