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Novel Peptide and Small Molecule Peptidomimetics for Inhibition and Destruction of Biofilms (08044)

詳細技術說明

Key Benefit: Novel compositions with high specificity and low toxicity that are well-suited for topical administration in dental applications

*Abstract

         

The University of Louisville is seeking a business partner interested in commercializing novel peptides and/or small molecule inhibitors of oral biofilm adherence and development.  The inhibitory peptide and/or small molecules specifically target P.gingivalis within biofilms and could be the first pathogen-specific treatment for oral diseases such as periodontitis.  Efficacy/toxicity testing of the peptide in an in vivo model is has been performed, and studies on the small molecule peptide mimics are currently underway.

    

Advantages 

    
■    Highly specific for the pathogenic organism; does not target benign or helpful organisms in the oral cavity
■    Long term control of P.gingivalis populations via formulation strategies allowing for daily administration
■    Topical administration can target the general population via OTC products.

    

Market Applications

    
■    Possible ingredient in chewing gum, mouthwash and/or toothpaste formulations
■    Development of therapies to treat or prevent the onset of periodontal disease.
■    Limiting P.gingivalis adherence may have a dramatic effect on pathogen associated systemic diseases like atherosclerosis and heart disease.

    

         

Technology 

   
In the oral cavity, P.gingivalis resides in the subgingival pocket and exists in concert with a complex microbial community collectively known as a biofilm.  In order for P.gingivalis to reach its primary niche, it must first attach to organisms like Streptococcus gordonii. This adherence is mediated by the P.gingivalis fimbrial protein Mfa with streptococcal antigen I/II polypeptide.  The inventors have dissected this interaction and identified a specific protein derived from antigen I/II that binds to Mfa and inhibits biofilm development.  Site specific mutagenesis studies have identified a structural motif that is essential for bioactivity of this peptide.  However, this region alone is not sufficient for biofilm inhibition.  To this effect, a second necessary motif comprised of five amino acids was identified.  A peptide (or molecular mimic) containing both motifs is highly active, preventing the initial formation of biofilms and disrupting pre-existing biofilms.  This novel therapeutic could be used both to treat and prevent periodontal disease.

    

Intellectual Property

    
U.S. patent 8142764 (peptides);  WO/2013/016206 (small molecule peptidomimetic compounds)   

Publications

    

Infect Immun. 2008 Jul;76(7):3273-80.

Peptides. 2010 Dec;31(12):2173-8.

Infect Immun. 2011 Jan;79(1):67-74.

    

Preparation of azidoaryl- and azidoalkyloxazoles for click chemistry.  Tetrahedron Letters.  epub 14 August 2012 http://www.sciencedirect.com/science/article/pii/S0040403912013895?v=s5

    

CONTACT 

    
For more information, please contact University of Louisville's Office of Technology Transfer:
Telephone:  (502)852-2965
Email:  thinker@louisville.edu
Website:  http://louisville.edu/thinker
Reference Disclosure No. 08044

Keywords: Dental, dentistry, biofilm, dental biofilm, gingivalis, gingivitis, oral health,

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