Peroxisome proliferator-activated receptors (PPARs) are a family of nuclear hormone receptors and ligand-activated transcription factors that play significant roles in cellular processes. Some isoforms have been validated as therapeutic targets in certain diseases. The role of isoform PPARdelta has not yet been fully explored due to its ubiquitous expression. However, with recent identification of selective chemical probes specific to PPARdelta, this receptor/transcription factor may emerge as a potentially promising pharmacological target for the treatment of a range of neurodegenerative diseases, including Alzheimer's Disease, Multiple sclerosis, Huntington's Disease, and Parkinson's disease.
This technology evolved from the elucidation that a specific phosphonate moiety (a P-C bond) acts as the pharmacopore for PPARdelta agonists, and proposes a potentially structurally novel scaffold for the design of PPARdelta agonists, and shows potential for a prodrug capable of crossing the blood-brain barrier that displays neuroprotective activity to the treatment of neurodegenerative disease(s).
Reference number: D-1262
Features, Benefits, & Advantages:
Increased drug specificity
Able to cross the blood-brain barrier
Prodrug, therefore, increased pool of distribution in theory and possibly longevity
Intellectual Property: A US provisional patent, serial number 62422797, was filed on 11/16/16.
Development Stage: This technology is still under development.
Paul Trippier, Pharmaceutical Sciences, Texas Tech University, Lubbock, Texas
Paul Webb, Genomic Medicine, Houston Methodist Research Institute, Houston, Texas
Keywords: peroxisome proliferator-activated receptor delta agonists, neurodegerative therapeutics (prodrugs, lipophilic[ity], and blood-brain barrier), phosphoiodyn A, esters