Details

Project TitleBioreversible Boronates Improve Drug Delivery
Track CodeP150009US02
Websitehttp://www.warf.org/technologies/summary/P150009US02.cmsx
Short DescriptionThe utility of many biologic drugs is limited by inefficient delivery into cells. Strategies to overcome this limitation have included enhancing the attraction between positively charged drug agents and the negatively charged cell surface. Other efforts have focused on natural ligands to target and bind agents to specific receptors on the cell surface.

Such methods have been used to deliver pharmaceuticals, proteins, peptides, nucleic acids and other particles into cells. While this has yielded some success, there remains a need for additional delivery strategies. In particular, the ability to bioreversibly modify molecules (i.e., enhance cellular uptake without effecting stability, function or immunogenicity) is highly desirable.\r\n\r\nA UW–Madison researcher has developed methods and reagents for enhancing cellular uptake in vivo or in vitro by attaching to any desired molecule one or more phenylboronic acid groups. The method is bioreversible; the boronate compound is cleaved from the molecule by intracellular enzymes, leaving its ‘cargo’ unaltered.

Advantageously, boronic acids readily form esters within the dense forest of polysaccharides, known as the glycocalyx, found on the surface of many cells. Targeting therapeutic agents to the glycocalyx has been shown to enhance cellular delivery. In addition, boronate groups are compatible with human physiology, appearing in chemotherapeutic agents and other remedies.
AbstractThe Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing improved methods of boronating cargo molecules to enhance their uptake in cells.
 
Tagsbiotechnology, pharmaceutical, Drug delivery
 
Posted DateJun 8, 2017 9:25 PM

Advantages

KEY BENEFITS
  • Bioreversible
  • Demonstrated to enhance cellular uptake
  • Delivery can take place in vivo or in vitro.

Potential Applications

  • Boronate-mediated delivery of drugs, proteins, nucleic acids and other molecules

Additional Information

Andersen K.A., Smith T.P. and Raines R.T. 2016. Boronic Acid for the Traceless Delivery of Proteins into Cells. ACS Chem. Biol. 11, 319-323.

Andersen K.A., Smith T.P. and Raines R.T. 2016. Boronic Acid for the Traceless Delivery of Proteins into Cells. ACS Chem. Biol. 11, 319-323.



WARF reference number P150031US02 describes the researcher’s bioreversible method of fluorenylating proteins and drugs to enhance their uptake in cells.

http://www.warf.org/technologies/summary/P150031US02.cmsx

Contact Information

TTO Home Page: http://www.warf.org



Name : Jennifer Gottwald

Title : Director of Licensing

Department : Licensing

Email : jennifer@warf.org

Phone : 608-960-9854

Address : 614 Walnut Street, 13th floor, Madison, WI 53726

Principal Investigator

Name : Ronald Raines

Department : Biochemistry



Name : Thomas Smith

Department : Biochemistry

Intellectual Property

Patent Number : 9,732,101

Patent Title : BIOREVERSIBLE BORONATES FOR DELIVERY OF MOLECULES INTO CELLS

Patent Application Date : Jul 27, 2015

Patent Publication Date : Jan 28, 2016

Patent Issue Date : Aug 15, 2017

Patent Link : http://www.warf.org/documents/ipstatus/P150009US02.PDF