Design, synthesis, and evaluation of cystargolide-based beta-lactones as potent proteasome inhibitors.

@article{Niroula2018DesignSA,
  title={Design, synthesis, and evaluation of cystargolide-based beta-lactones as potent proteasome inhibitors.},
  author={Doleshwar Niroula and Liam P. Hallada and Camille Le Chapelain and Susantha K Ganegamage and Devon Dotson and Snezna Rogelj and Michael Groll and Rodolfo Tello-Aburto},
  journal={European Journal of Medicinal Chemistry},
  year={2018},
  volume={157},
  pages={962-977}
}
The peptidic β-lactone proteasome inhibitors (PIs) cystargolides A and B were used to conduct structure-activity relationship (SAR) studies in order to assess their anticancer potential. A total of 24 different analogs were designed, synthesized and evaluated for proteasome inhibition, for cytotoxicity towards several cancer cell lines, and for their ability to enter intact cells. X-ray crystallographic analysis and subunit selectivity was used to determine the specific subunit binding… 
2 Citations
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.
Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors
TLDR
The following review discusses the efforts made in the field to isolate and identify natural products as inhibitors of the proteasome and some of the modifications made to natural products in order to discover more potent and selective inhibitors for potential disease treatment.

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