Researchers at St. Jude and the University of Illinois at Urbana-Champaign have designed Toll-like receptor (TLR) signaling inhibitors useful in the treatment of diseases or conditions resulting from excessive activity of the Toll-like receptors. TLRs have been shown to play a role in the pathogenesis of many diseases, including autoimmunity, infectious and inflammatory diseases. Exaggerated or prolonged TLR activation leads to pathological inflammation and diverse diseases, such as bacterial sepsis, metabolic and autoimmune diseases, cancer or stroke.
This series of methyl-piperidino-pyrazole (MPP) compounds may be used for research involving blocking the TLR pathway, including in vivo research. Based on these studies and further research, optimized forms of these compounds may be used for treating patients.
Toll-like receptors (TLRs), inflammation, immune response, bacterial sepsis, metabolic disease, autoimmune disease, cancer, stroke, drug screening, Nitrogen heterocycles; immune response; pathological inflammation; signal transduction; toll like receptors
Granted Patents or Published Applications
Patent application pending
Related Scientific References
Pollock, Sharma, Ippagunta, Redecke, Häcker, Katzenellenbogen. “Triaryl Pyrazole Toll-Like Receptor Signaling Inhibitors: Structure-Activity Relationships Governing Pan- and Selective Signaling Inhibitors.” ChemMedChem. 2018 Aug 16. doi: 10.1002/cmdc.201800417.
Ippagunta, Pollock, Sharma, Lin, Chen, Tawaratsumida, High, Min, Chen, Guy, Redecke, Katzenellenbogen, Häcker. “Identification of Toll-like receptor signaling inhibitors based on selective activation of hierarchically acting signaling proteins.” Sci Signal. 2018 Aug 14;11(543). pii: eaaq1077. doi: 10.1126/scisignal.aaq1077.
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