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编 号:F760045
分子式:C22H38O5
分子量:382.53
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生物活性:
JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases.

体外研究:
Munc13-1 是二酰甘油第二信使途径的靶标,在胞吐作用期间的囊泡成熟中发挥作用。通过在囊泡融合之前作用于突触囊泡启动来参与神经递质释放,并参与易释放囊泡池 (RRP) 的活性依赖性再填充。
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