H-ARG-ARG-ARG-PRO-ARG-PRO-PRO-TYR-LEU-PRO-ARG-PRO-ARG-PRO-PRO-PRO-PHE-PHE-PRO-PRO-ARG-LEU-PRO-PRO-ARG-ILE-PRO-PRO-GLY-PHE-PRO-PRO-ARG-PHE-PRO-PRO-ARG-PHE-PRO-NH2
- CAS号:139637-11-9
- 英文名:PR 39 (PORCINE)
- 中文名:H-ARG-ARG-ARG-PRO-ARG-PRO-PRO-TYR-LEU-PRO-ARG-PRO-ARG-PRO-PRO-PRO-PHE-PHE-PRO-PRO-ARG-LEU-PRO-PRO-ARG-ILE-PRO-PRO-GLY-PHE-PRO-PRO-ARG-PHE-PRO-PRO-ARG-PHE-PRO-NH2
- CBNumber:CB8101390
- 分子式:C229H345N69O41
- 分子量:4720.6273
- MOL File:139637-11-9.mol
- 储存条件 :Desiccate at -20°C
- 溶解度 :Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
- 形态 :Powder
H-ARG-ARG-ARG-PRO-ARG-PRO-PRO-TYR-LEU-PRO-ARG-PRO-ARG-PRO-PRO-PRO-PHE-PHE-PRO-PRO-ARG-LEU-PRO-PRO-ARG-ILE-PRO-PRO-GLY-PHE-PRO-PRO-ARG-PHE-PRO-PRO-ARG-PHE-PRO-NH2性质、用途与生产工艺
- 生物活性 PR-39 是富含脯氨酸和精氨酸的天然抗菌肽，是一种非竞争性，可逆和变构的蛋白酶体 (proteasome) 抑制剂。PR-39 可逆地结合到蛋白酶体的 α7 亚基上，并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。PR-39 刺激小鼠的血管生成，抑制炎症反应并显着减小心肌梗死面积。
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体外研究
PR-39, shown to selectively affect proteasomemediated protein degradation in vivo, alters the shape of the 20S and 26S cylinder and affects the binding of 19S caps in a reversible manner. PR-39 specifically blocks degradation of IκBα and HIF-1α by the proteasome.
PR-39 (100 nM) blocks TNF-α-induced (1 ng/mL; for 20 minutes) activation of VCAM-1 (2 hours) and ICAM-1 (8 hours) expression in human umbilical vein endothelial cells (HUVEC).
PR-39 (10 μM) does not affect the ability to proliferate of ECV304 cell. PR39 is able to inhibit IκBα degradation without significantly affecting overall protein degradation in cells.
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体内研究
PR-39 (10 mg/kg, intravenously; 1 hour before Caerulein of 50μg/kg, ip) blocks IκBα degradation and NF-κB-dependent transcription in the mouse pancreas after induction of acute pancreatitis.
PR-39 (1 μg/kg/day; 7-day intraperitoneal infusion) demonstrates significantly small infarct in C57BL/6 mice.
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