Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(PCSK9) protein activity
US10307433B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 25, 2018 |
| Grant date | Jun 4, 2019 |
| Priority date | — |
| Expiry date | May 25, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/06078
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.