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AssigneeSRX Cardio, LLC
InventorsThomas E. Barta, Jonathan W. Bourne, Kyle D. Monroe, Michael M. Muehlemann
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This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol, High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
A method, comprising binding an allosteric small molecule compound to a PCSK9 protein to modulate the uptake of low-density lipoprotein by a plurality of hepatocytes.
A commercial package comprising a pharmaceutical composition of a PCSK9 allosteric small molecule compound and instructions for the use of said compound for modulating the biological activity of PCSK9 to treat hypercholesterolemia.
A method of administering a PCSK9 allosteric small molecule compound to a subject, wherein said subject has at least one symptom of hypercholesterolemia such that said at least one symptom of hypercholesterolemia is reduced.
Dependencies are inferred from the claim text.