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    Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) Allosteric Binding Ligands To Modulate Serum Low Density Lipoprotein (LDL) Levels
    2.
    发明申请
    Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) Allosteric Binding Ligands To Modulate Serum Low Density Lipoprotein (LDL) Levels 审中-公开
    前蛋白转氨酶枯草杆菌蛋白酶Kexin 9型（PCSK9）变构结合配体调节血清低密度脂蛋白（LDL）水平

    公开(公告)号：US20160083425A1

    公开(公告)日：2016-03-24

    申请号：US14825700

    申请日：2015-08-13

    申请人： SRX Cardio, LLC

    发明人： Michael M. Muehlemann ,  Thomas E. Barta ,  Kyle D. Monroe ,  Jonathan William Bourne ,  Margaret Thompson Reece ,  Vesa Nevalainen ,  Eric T. Baldwin

    IPC分类号： C07K7/06 ,  C07K5/097 ,  C12N5/071

    CPC分类号： C07K7/06 ,  C07K5/06078 ,  C07K5/06156 ,  C07K5/0812 ,  C07K5/0817 ,  C07K5/0821 ,  C07K5/101 ,  C07K5/1016

    摘要： This invention is related to the field of hypercholesterolemia. In particular, the invention provides compositions and methods to modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9 using synthetic ligands and/or synthetic ligand derivative sequences of 3-8 amino acids ranging between 350-2,000 Da. Altering the conformation of PCSK9 affects 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 ligands which can raise LDL levels.

    摘要翻译： 本发明涉及高胆固醇血症的领域。 特别地，本发明提供了通过使用范围在350-2,000Da之间的3-8个氨基酸的合成配体和/或合成配体衍生物序列改变蛋白质PCSK9的构象来调节低密度脂蛋白的循环水平的组合物和方法。 改变PCSK9的构象影响PCSK9与内源性低密度脂蛋白受体之间的相互作用，并且可导致循环低密度脂蛋白胆固醇水平降低或增加。 高LDL胆固醇水平与心脏病风险增加有关。 低脂低胆固醇水平可能在其他病症如肝功能障碍中有问题; 因此，也可以提高可以提高LDL水平的配体。

    COMPOSITION AND METHODS OF USE OF TETRAHYDROISOQUINOLINE SMALL MOLECULES TO BIND AND MODULATE PCSK9 PROTEIN ACTIVITY
    7.
    发明申请
    COMPOSITION AND METHODS OF USE OF TETRAHYDROISOQUINOLINE SMALL MOLECULES TO BIND AND MODULATE PCSK9 PROTEIN ACTIVITY 有权

    公开(公告)号：US20210309613A1

    公开(公告)日：2021-10-07

    申请号：US17098184

    申请日：2020-11-13

    申请人： SRX Cardio, LLC

    发明人： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

    IPC分类号： C07D217/24 ,  C07D217/02

    摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound 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 dysfunctions; thus, there is also utility for small organic compound ligands and can raise LDL levels.