Use of anti-aging glycopeptides to enhance pancreatic cell health, survival and improve transplant outcome

{
  "publication_number": "US2026102436A1",
  "country": "US",
  "kind": "A1",
  "title": "Use of anti-aging glycopeptides to enhance pancreatic cell health, survival and improve transplant outcome",
  "abstract": "The present disclosure relates to an in vitro method for enhancing engraftment of isolated pancreatic cells comprising the step of contacting an isolated pancreatic cell prior to a transplantation in a subject in need thereof, with a gem-difluorinated C-glycopeptide compound of general formula I, or a pharmaceutically acceptable base, addition salt with an acid, hydrate or solvate of the compound of general formula I:",
  "claims": [
    "1. A method for improving cell integrity and/or survival of isolated human pancreatic islet cells, isolated human pancreatic islet progenitor cells, or both following a transplantation in a human patient in need thereof and immunosuppressed with an immunosuppressant drug, comprising the steps of: a) contacting an isolated human pancreatic islet cell, an isolated human pancreatic islet progenitor cell, or both with a gem-difluorinated C-glycopeptide compound of formula III, or a pharmaceutically acceptable base, addition salt with an acid, hydrate or solvate thereof: wherein the immunosuppressant drug is sirolimus, tacrolimus, cyclosporine, or any combination thereof; wherein the cell integrity and/or survival of the transplanted isolated human pancreatic islet cells, isolated human pancreatic islet progenitor cells, or both, contacted with the compound of formula III, is improved in comparison to transplanted isolated human pancreatic islet cells, isolated human pancreatic islet progenitor cells, or both, contacted with the immunosuppressant drug and not contacted with the compound of formula III. 2. The method of claim 1, further comprising b) contacting the isolated human pancreatic islet cell, the isolated human pancreatic islet progenitor cells, or both of step a), prior to the transplantation in said human patient, with the immunosuppressant drug. 3. The method of claim 1, further comprising c) transplanting the treated isolated human pancreatic islet cell, the isolated human pancreatic islet progenitor cell, or both, of step a) in said human patient. 4. The method of claim 1, further comprising step a′) before step a): a′) isolating human pancreatic islet cells, human pancreatic islet progenitor cells, or both. 5. The method of claim 1, wherein said isolated human pancreatic islet cell is an isolated human alpha cell, an isolated human beta cell, an isolated human delta cell, an isolated human gamma cell, an isolated human epsilon cell, or a combination thereof. 6. The method of claim 1, wherein said isolated human pancreatic islet cell is an isolated human beta cell. 7. The method of claim 1, wherein said isolated human pancreatic islet cell is isolated from a live human donor, a cadaveric human donor, or combinations thereof. 8. The method of claim 1, wherein the isolated human pancreatic islet cell, the isolated human pancreatic islet progenitor cell, or both are contacted with the compound for an hour. 9. The method of claim 1, wherein concentration of said compound is from about 1 mg/ml to about 5 mg/ml. 10. The method of claim 1, wherein improving cell integrity and/or survival comprises increasing cell count, reducing apoptosis, improving inflammatory response; improving insulin secretory function and/or insulin secretion, or combinations thereof. 11. A method for improving cell integrity and/or survival of isolated human pancreatic islet cells, isolated human pancreatic islet progenitor cells, or both following a transplantation in a human patient in need thereof and immunosuppressed with an immunosuppressant drug, comprising the steps of: a) isolating human pancreatic islet cells, human pancreatic islet progenitor cells, or both; b) contacting the isolated human pancreatic islet cell, the isolated human pancreatic islet progenitor cell, or both of step a) with a gem-difluorinated C-glycopeptide compound of formula III, or a pharmaceutically acceptable base, addition salt with an acid, hydrate or solvate thereof: c) contacting the isolated human pancreatic islet cell, the isolated human pancreatic islet progenitor cells, or both of step b) with the immunosuppressant drug; and d) transplanting the treated isolated human pancreatic islet cell, the isolated human pancreatic islet progenitor cell, or both, of step c) in said human patient; wherein the immunosuppressant drug is sirolimus, tacrolimus, cyclosporine, or any combination thereof; wherein the cell integrity and/or survival of the transplanted isolated human pancreatic islet cells, isolated human pancreatic islet progenitor cells, or both, contacted with the compound of formula III, is improved in comparison to transplanted isolated human pancreatic islet cells, isolated human pancreatic islet progenitor cells, or both, contacted with the immunosuppressant drug and not contacted with the compound of formula III."
  ],
  "description_excerpt": "The subject matter disclosed generally relates to the use of anti-aging glycopeptides. More particularly, the subject matter relates to the use of anti-aging glycopeptides to enhance human pancreatic cells engraftment.\n\nAntifreeze biological compounds, and particularly glycoproteins, exist in the natural environment. These compounds are present for example in some fishes, enabling them to survive in a low temperature environment (i.e. near zero or sub-zero temperatures). Scientists have been investigating how antifreeze compounds taken from the natural environment (fish, amphibians, plants, insects, etc.) have an influence on these phenomena. Research has focused on the synthesis of analogous compounds that are sufficiently stable and whose activity is at least equal to or even greater than the activity of the natural molecules, for commercial applications.\n\nAnti-freeze proteins (AFP) have generated increasing interest for their ability to protect cells under a variety of conditions. They are naturally encountered in Arctic and Antarctic fish as well as other cold-climate dwelling invertebrates, and are responsible for maintaining cells and tissue functional at sub-zero temperatures. AFP were successfully isolated in the 1950s and have demonstrated the ability to non-colligatively lower the freezing temperature of body fluids by binding to ice crystals.\n\nEarly experiments with these compounds in the field of organ and tissue transplantation showed promising results, making them attractive therapeutic candidates to protect cells against harmful conditions associated with the process of retrieval-preservation-reperfusion.",
  "cpc": [
    "A61K 35/39",
    "C12N 2501/90",
    "C12N 2501/998",
    "C12N 2501/999",
    "C12N 5/0676"
  ],
  "assignees": [
    "Protokinetix Inc"
  ],
  "inventors": [
    "Lachlan Grant Young",
    "A.M. James Shapiro"
  ],
  "filing_date": "2025-12-08",
  "publication_date": "2026-04-16",
  "priority_date": "2014-06-04",
  "application_number": "US-202519412509-A",
  "cited_by_count": 0
}