Ac-Tyr-Trp-Gly-OH

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Ac-Tyr-Trp-Gly-OH
• 英文别名: 2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetic acid
• 化学式: C₂₄H₂₆N₄O₆
• 分子量: 466.5
• InChiKey: REPIUJDWPUWNET-SFTDATJTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  34
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  161
• 氢给体数：
  6
• 氢受体数：
  6

文献信息

• Proprotein convertase subtilisin kexin type 9 (PCSK9) allosteric binding ligands to modulate serum low density lipoprotein (LDL) levels
  申请人：SRX Cardio, LLC

  公开号：US10287317B2

  公开（公告）日：2019-05-14

  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.

  本发明涉及高胆固醇血症领域。特别是，本发明提供了通过使用合成配体和/或 350-2,000 Da 之间的 3-8 个氨基酸的合成配体衍生物序列改变蛋白质 PCSK9 的构象来调节循环中低密度脂蛋白水平的组合物和方法。改变 PCSK9 的构象会影响 PCSK9 与内源性低密度脂蛋白受体之间的相互作用，从而导致循环中低密度脂蛋白胆固醇水平的降低或升高。低密度脂蛋白胆固醇水平高与心脏病风险增加有关。低密度脂蛋白胆固醇水平过低可能会对肝功能障碍等其他疾病造成困扰；因此，能提高低密度脂蛋白水平的配体也很有用。
• Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) Allosteric Binding Ligands To Modulate Serum Low Density Lipoprotein (LDL) Levels
  申请人：SRX Cardio, LLC

  公开号：US20160083425A1

  公开（公告）日：2016-03-24

  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.
• [EN] PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) ALLOSTERIC BINDING LIGANDS TO MUDULATE SERUM LOW DENSITY LIPOPROTEIN (LDL) LEVELS<br/>[FR] LIGANDS DE LIAISON ALLOSTÉRIQUES DE LA PROPROTÉINE CONVERTASE SUBTILISINE/KEXINE DE TYPE 9 (PCSK9) UTILISABLES EN VUE DE LA MODULATION DES NIVEAUX SÉRIQUES DE LIPOPROTÉINES DE BASSE DENSITÉ (LDL)
  申请人：SRX CARDIO LLC

  公开号：WO2014127316A2

  公开（公告）日：2014-08-21

  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.