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Stapled Peptides for Treatment of Cardiovascular Diseases and Inflammation

Posted May 06 2013 8:00pm

Description of Invention:
The invention is directed to small molecule mimetics of apolipoproteins that have an inter-helical hydrocarbon bond, which stabilizes helix formation.

Apolipoproteins facilitate the transport of lipids and cholesterol in the body. Mimetics of apolipoproteins have been used to treat cholesterol-related disorders. However, these mimetics are susceptible to degradation in biological fluids and as a result, their ability to bind cholesterol becomes diminished over time.

Scientists at NHLBI have devised methods to stabilize and improve the performance of apolipoprotein mimetic peptides, using a modified hydrocarbon chain (“stapled apolipoproteins”). These stapled apolipoproteins are superior to singular apolipoproteins in that they are more resistant to enzymatic degradation and efflux a greater amount of cellular cholesterol.

Stapled apolipoproteins can be used in the treatment of cardiovascular diseases, particularly for treatment of atherosclerosis.

Applications:
  • Treatment of inflammation and cardiovascular diseases, including hyperlipidemia, atherosclerosis, restenosis, and acute coronary syndrome.
  • Inclusion in oral, intravenous or transdermal peptide formulations.


Advantages:
  • Stapled apolipoproteins are more resistant to proteolysis and display enhanced bioavailability.
  • Stapled apolipoproteins are amenable to oral delivery and have increased permeability to the blood brain barrier.


Development Status:
  • Pre-clinical
  • In vitro data available
  • In vivo data available (animal)


Inventors:
Alan T Remaley (CC)
Marcelo A Amar (NHLBI)
Imoh Z Ikpot (NHLBI)
Denis O Sviridov (NHLBI)
David O Osei-Hwedieh (NHLBI)


Patent Status:
HHS, Reference No. E-126-2011/0
PCT, Application No. PCT/US1235870 filed 30 Apr 2012


Relevant Publication:
  1. Osei-Hwedieh DO, et al. [ PMID 21172387 ]


Collaborative Research Opportunity:
The NHLBI Lipoprotein Metabolism Section is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize Hydrocarbon-stapled Apolipoprotein Peptide Mimetics for the Treatment of Cardiovascular Diseases and Inflammation. For collaboration opportunities, please contact Denise Crooks, Ph.D. at crooksd@nhlbi.nih.gov .


For Licensing Information Please Contact:
Lauren Nguyen-Antczak Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: nguyenantczakla@mail.nih.gov
Phone: 301-496-7057
Fax: 301-402-0220


Ref No: 2559

Updated: 05/2013

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