Ontology highlight
ABSTRACT:
SUBMITTER: Totaro KA
PROVIDER: S-EPMC4562813 | biostudies-literature | 2015 Sep
REPOSITORIES: biostudies-literature
Totaro Kyle A KA Barthelme Dominik D Simpson Peter T PT Sauer Robert T RT Sello Jason K JK
Bioorganic & medicinal chemistry 20150726 18
Natural products that inhibit the proteasome have been fruitful starting points for the development of drug candidates. Those of the syringolin family have been underexploited in this context. Using the published model for substrate mimicry by the syringolins and knowledge about the substrate preferences of the proteolytic subunits of the human proteasome, we have designed, synthesized, and evaluated syringolin analogs. As some of our analogs inhibit the activity of the proteasome with second-or ...[more]