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Article |
Simplified immunosuppressive and neuroprotective agents based on gracilin A
Pharmacophore-directed retrosynthesis targets a potential pharmacophore from early on in a natural product synthesis and incremental increases in the complexity of this minimal structure enable a SAR profile to develop over the course of the campaign. The method is applied to gracilin A, finding simplified derivatives displaying potent immunosuppressive effects or selective neuroprotective effects in cell-based assays.
- Mikail E. Abbasov
- , Rebeca Alvariño
- & Daniel Romo
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Article |
Development of a minimal saponin vaccine adjuvant based on QS-21
Adjuvants are used to increase the immune response to molecular vaccines. A minimal synthetic variant of the saponin natural product QS-21 has been developed as a potent, non-toxic adjuvant, enabling dissection of structural requirements in the triterpene domain and in vivo biodistribution studies to probe mechanisms of action.
- Alberto Fernández-Tejada
- , Eric K. Chea
- & David Y. Gin
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Research Highlights |
Advancing vaccines
Replacing readily hydrolysable ester linkages with amides in a natural adjuvant has resulted in not only more stable, but significantly more active and less toxic analogues.
- Georgia Tsoukala
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