Potent, Simplified Derivatives of Immunosuppressive Agents

C04420: Potent, Simplified Derivatives of Immunosuppressive Agents
Technical Details:
Pateamine A (PatA), a metabolite from the marine sponge Mycale, is a potent inhibitor of the intracellular signal transduction pathway that emanates from the T-cell receptor and leads to the transcription of cytokines such as interleukin-2 (IL-2). Researchers at Johns Hopkins and Texas A&M have identified distinct binding and scaffolding domains in the PatA structure with respect to interactions with its putative cellular receptor(s). Based on these domains, a simplified PatA derivative (DMDAPatA) was generated that can be prepared in fewer synthetic steps relative to PatA and was found to exhibit greater potency in inhibition of IL-2 production relative to PatA. In addition, several other PatA derivatives were synthesized that displayed lower potency but marked stability relative to the natural product.
Looking for Partners:
These compounds may provide new pharmaceutical compounds for treating immune mediated disease and conditions.

Category(s):