P110 能够抑制Drp1酶活性,并在体外和培养的神经元中阻断 Drp1/Fis1(动力相关蛋白 1/分裂蛋白 1)的相互作用,但对 Drp1 与其他线粒体适配体的相互作用没有影响。在帕金森病模型中,P110具有神经保护作用,通过抑制线粒体分裂和活性氧(ROS)的生成,进而改善线粒体膜电位和线粒体完整性。P110 可通过减少细胞凋亡和自噬性细胞死亡来提高神经元细胞的存活率,并减少原代多巴胺能神经元的神经突损失。
P110 inhibits Drp1 enzyme activity and blocks the Drp1/Fis1 (Dynamin related protein 1/fission 1) interaction in vitro and in cultured neurons, but has no effect on the interaction between Drp1 and other mitochondrial adaptors. In Parkinson's disease models P110 is neuroprotective by inhibiting mitochondrial fragmentation and reactive oxygen species (ROS) production and subsequently improving mitochondrial membrane potential and mitochondrial integrity. P110 increases neuronal cell viability by reducing apoptosis and autophagic cell death, and reduces neurite loss of primary dopaminergic neurons.
单字母 H2N-YGRKKRRQRRRGGDLLPRGS-NH2
多字母 H2N-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Gly-Asp-Leu-Leu-Pro-Arg-Gly-Ser-NH2
氨基酸个数 20
分子式 C100H179N45O25
平均分子量(MW) 2411.78
精确分子量(Exact Mass)(MW) 2410.41
等电点(PI) 13.29
pH=7.0时的净电荷数 9.97
GRAVY -2.18
亲水残基比例 0.05
消光系数 1490
溶解建议 亲水
参考文献:
Qi et al (2013) A novel Drp1 inhibitor diminishes aberrant mitochondrial fission and neurotoxicity. J.Cell Sci. 126 789 PMID: 23239023
Joshi et al (2018) Drp1/Fis1 interaction mediates mitochondrial dysfunction, bioenergetic failure and cognitive decline in Alzheimer's disease. Oncotarget 9 6128 PMID: 29464060
Iqbal et al (2018) A synthetic peptide rescues rat cortical neurons from anesthetic-induced cell death, perturbation of growth and synaptic assembly. Sci Rep 11 4567 PMID: 33633281