FOXP3 Stapled Peptides to Deactivate Regulatory T Cells



    • Regulatory T cells (Tregs) modulate immune function by preventing autoreactive T cell responses, including those that would normally target cancer cells. Treg activity can significantly limit the efficacy of immunotherapies designed to stimulate CD8+ T cells, and therefore a strategy for reducing Treg activity as an aspect of immunotherapy is highly desirable.
    • The FOXP3 transcription factor is selectively expressed in Tregs and is necessary for Treg function. The inventors have synthesized stapled alpha helix peptides that inhibit the FOXP3 homo and heterodimerization necessary to form a functional complex. These peptides block FOXP3 signaling, and consequently indirectly inhibit Treg function. 
    • The product is (1) stapled alpha helix peptides that inhibit FOXP3 transcriptional activity and (2) intracellular delivery of the stapled alpha helix peptides using targeted nanoparticles.
    • In initial proof-of-concept studies, the stapled alpha helix peptides bound to recombinant FOXP3 with nanomolar affinity and reduced expression of FOXP3 regulated genes. 


    Fluorescent polarization binding curves of select stapled alpha helix (SAH) peptide designs targeting the leucine zipper domain of FOXP3. Recombinant FOXP3 was used in binding experiments that lacked the N-terminal domain (FOXP3DN), but retained the leucine zipper domain.



    • Lower drug resistance potential than therapeutic antibodies
    • Fewer off-target effects than small molecules



    • Immuno-oncology
    • Combination therapy: (Chemotherapy, Radiotherapy, Immunotherapy)
    • US Nationalized PCT: PCT/US2017/065147




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