Technology ID
TAB-2559
Stapled Peptides for Treatment of Cardiovascular Diseases and Inflammation
E-Numbers
E-126-2011-0
Lead Inventor
Remaley, Alan (Clinical Center (CC))
Co-Inventors
Amar, Marcelo (NHLBI)
Ikpot, Imoh (NHLBI)
Sviridov, Denis (NHLBI)
Osei-Hwedieh, David (NHLBI)
Applications
Therapeutics
Research Materials
Diagnostics
Therapeutic Areas
Cardiology
Development Status
- Pre-clinical
- In vitro data available
- In vivo data available (animal)
Lead IC
CC
ICs
NHLBI
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.
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.
Commercial Applications
- Treatment of inflammation and cardiovascular diseases, including hyperlipidemia, atherosclerosis, restenosis, and acute coronary syndrome.
- Inclusion in oral, intravenous or transdermal peptide formulations.
Competitive 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.
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