抑制 APC/C 的蛋白酶解活性对于纺锤体检查点组件介导的有丝分裂后期启动是必需的
中文名称
通路描述
有丝分裂检查点的靶标是 Anaphase Promoting Complex/Cyclosome (APC/C)，它是一种 E3 泛素连接酶，负责降解对有丝分裂退出至关重要的蛋白质。目前，抑制 APC/C 的机制有两种：一是通过 Mitotic Checkpoint Complex (MCC) 直接结合，二是通过 sequestration 其激活因子 Cdc20。
英文描述
Ribavirin ADME Ribavirin (RBV) is a synthetic nucleoside analog structurally related to guanine. It is given orally as part of the treatment of HCV infection, and by inhalation for the treatment of RSV infection. According to the WHO, ribavirin can also be used for the treatment of viral hemorrhagic fevers (WHO 2015).
RBV is administered orally in doses of 400 to 600 mg. It is highly soluble in water and a typical dose is dissolved completely over a wide range of acidities. RBV is rapidly absorbed into the circulation. After the oral administration of 600 mg radiolabeled ribavirin, approximately 61% of the drug was detected in the urine and 12% was detected in the feces. 17% of an administered dose was in unchanged form. RBV accumulates in human erythrocytes and remains in the body for weeks, with a halflife of >100 hours (Goodarzi et al, 2016). A consequence of the accumulation in erythrocytes is the well-known side effect of hemolytic anemia, which is reversible by cessation of administration (FDA label Rebetol, 2013).
Ribavirin is a prodrug. It is metabolized through two different paths: phosphorylation, yielding the active triphosphate (RBV-TP), and degradation via de-ribosylation and hydrolysis of the amide group. The GI tract, and not the liver, appears to be the major site of first-pass elimination (Dixit and Perelson, 2006).
RBV is administered orally in doses of 400 to 600 mg. It is highly soluble in water and a typical dose is dissolved completely over a wide range of acidities. RBV is rapidly absorbed into the circulation. After the oral administration of 600 mg radiolabeled ribavirin, approximately 61% of the drug was detected in the urine and 12% was detected in the feces. 17% of an administered dose was in unchanged form. RBV accumulates in human erythrocytes and remains in the body for weeks, with a halflife of >100 hours (Goodarzi et al, 2016). A consequence of the accumulation in erythrocytes is the well-known side effect of hemolytic anemia, which is reversible by cessation of administration (FDA label Rebetol, 2013).
Ribavirin is a prodrug. It is metabolized through two different paths: phosphorylation, yielding the active triphosphate (RBV-TP), and degradation via de-ribosylation and hydrolysis of the amide group. The GI tract, and not the liver, appears to be the major site of first-pass elimination (Dixit and Perelson, 2006).
所含基因
11 个基因