Potent, Simplified Derivatives of Immunosuppressive Agents

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. Description (Set) Proposed Use (Set) These compounds may provide new pharmaceutical compounds for treating immune mediated disease and conditions.

Inventor(s): Liu, Jun

Type of Offer: Licensing



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