Fibroblast Growth Factor Receptor Peptoid Agonists for Wound Healing

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Xin Qi
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Anita Rao
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Patent Protection
PCT Patent Application WO 2017/127528

Peptoid Ligands That Are Stable and Cost Efficient to Make

These peptoid ligands provide more stability and cost efficiency than their peptide counterparts and act as fibroblast growth factor receptor agonists for treatment of wounds specifically after radiation treatments. Recently, the medicinal chemistry field has taken great interest in fibroblast growth factor receptors (FGFRs) targeting drugs. Fibroblast growth factors (FGFs) bind to FGFRs in angiogenesis, wound healing, embryonic development, and various endocrine signaling pathways. The focus has been on developing peptide ligands of FGFR, but because of the complexity, instability, and high cost of synthesizing long-chain peptide ligands, it is important to identify more potent peptidomimetic FGFR ligands to treat diseases associated with fibroblast growth factor receptors. Researchers at the University of Florida have developed receptor specific peptoid ligands that function as FGFR agonists.

Application

Peptoid ligands that function as FGFR agonists, effective as radiation mitigators with potential therapeutic application in FGFR-based drug discovery for anti-acute radiation syndrome and wound healing

Advantages

  • Enhances stability toward proteolysis, preventing abnormal accumulation
  • Increases resistance to denaturation induced by solvent, temperature, or chemicals, allowing peptoids to reach desired cells
  • Has low immunogenicity, decreasing chance of immune response
  • Is receptor specific, increasing efficacy of treatment
  • Built by highly available primary amines, decreasing cost

Technology

These peptoids are easily synthesized by a two-step solid-phase synthetic method using acylation and amination. Researchers discovered these peptoids by way of microarray screening. These peptoids act as fibroblast growth factor receptor agonists, meaning they chemically bind to the receptors and cause or intensify the biological response, leading to induction of neurite outgrowth and protection against apoptosis, etc. Peptoids have more rigid backbone structures than peptides, allowing more stable chemical scaffolding, less expensive production, better cell penetration and lower immunogenicity. They are administered intravenously and aid in wound healing and anti-acute radiation syndrome. This would be especially beneficial after radiation treatment for diseases such as cancer, neurological diseases, and gastrointestinal disorders.