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Cell Signaling Modulation

Enzo’s therapeutic platform provides a basis for the development of pharmaceutical agents that modulate protein-protein interactions. Our scientists and collaborators have unlocked the secrets of a major cell signaling pathway and developed a means to modify biologic activity in several metabolic systems through the use of small molecule drug candidates.

Screening System:
We have used metabolic systems to determine the structures of key regulatory proteins and to identify active sites as potential targets for Enzo’s proprietary drug discovery system. Our technology is capable of generating active compounds that range from orally delivered small molecules to peptides and antibodies. We have performed pioneering work on the structure and function of the LDL receptor-related protein “LRP” and its ligands, and we have developed a screening technology to identify active compounds and synthetic proprietary molecules capable of producing biological effects in cell-based systems and animal models. Specifically, our drug discovery platform enables us to:

  • generate biological and genetic information concerning LRP;
  • determine the structure of LRP-ligand docking sites;
  • identify the functionally important residues;
  • build a fine structure map of LRP and employ it as the basis for virtual screening;
  • establish in vitro biological assays capable of identifying active compounds;
  • design and synthesize proprietary molecules that are active in animal models of disease.

 

Active Drug Candidate Compounds:
Through this novel, proprietary functional screening system we have identified small molecules capable of modulating ligand-receptor interactions. Preclinical animal studies have identified lead compounds that:

  • indicate a new path for the treatment of osteoporosis and/or osteonecrosis by producing significant increases in total and femoral bone density through new bone formation and significant reduction in alveolar bone loss.

  • demonstrate significant glucose lowering activities in standard animal models of diabetes and have the potential to reduce fasting and postprandial glucose levels in these animals.

 

Other important applications of Enzo’s LRP-centered platform include cancer, skin and hair growth.