1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. PCSK9

PCSK9 (前蛋白转化酶/枯草溶菌素9)

Proprotein convertase subtilisin/kexin type 9

前蛋白转化酶/枯草溶菌素 9 (PCSK9) 是由人类 1 号染色体上的 PCSK9 基因编码的酶它是蛋白转化酶家族的第 9 个成员,该家族的蛋白可以激活其他蛋白相似的基因(同源基因)在许多物种中被发现[1]。 PCSK9 一种肝脏合成的蛋白酶,它是肝细胞表面低密度脂蛋白受体 (LDLR) 水平的主要调节者,它可以抑制LDLR 循环途径。 PCSK9 通过与肝细胞表面 LDLR 结合,伴随 LDLR 到溶酶体进行降解,阻止 LDLR 再循环到细胞膜,并有效地上调了循环中的 LDL的水平。因此抑制 PCSK9 蛋白酶的活性,就可以下调循环中的 LDL 水平。PCSK9 与多种心血管疾病密切相关,尤其是高胆固醇血症和动脉粥样硬化症[2]

The protein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene located on human chromosome 1. It is the ninth member of the protein convertase family, a group of enzymes that can activate homologous genes found in many species[1]. PCSK9 is a liver-synthesized protease that plays a major role in regulating the levels of low-density lipoprotein receptors (LDLR) on the surface of liver cells and can inhibit the LDLR recycling pathway. PCSK9 binds to LDLR on the surface of liver cells, escorts LDLR to lysosomes for degradation, and prevents LDLR from recirculating to the cell membrane, effectively increasing the level of circulating LDL. Therefore, inhibiting the activity of the PCSK9 protease can down-regulate circulating LDL levels. PCSK9 is closely associated with various cardiovascular diseases, especially hypercholesterolemia and atherosclerosis[2].

PCSK9 相关产品 (82):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-158827A
    AZD8233 sodium
    AZD8233 sodium 是一种靶向肝脏的反义寡核苷酸,能抑制前蛋白转化酶/枯草溶菌素9(PCSK9)的蛋白合成。AZD8233 sodium 通过降低PCSK9水平增加可用的LDL受体,从而清除血液中的LDL并降低LDL-C水平。
    AZD8233 sodium
  • HY-155415
    PCSK9-IN-20 Inhibitor
    PCSK9-IN-20 (Compound 3i) 是一种 PCSK9 抑制剂,IC50 为 3.96 µM。PCSK9-IN-20 在体外降低 PCSK9 并增加 LDLR 蛋白表达。
    PCSK9-IN-20