PKCε Inhibitor Peptide, also called εV1-2, is a protein kinase C ε (PKCε)-derived peptide, act as a selective PKCε inhibitor, inhibits the translocation of PKCε [1]. PKCε Inhibitor Peptide is a peptide designed to compete with native nPKC ε to bind ε-Receptors for activated C Kinase (ε-RACK) and thereby inhibits nPKC ε catalytic activity due to decreased substrate accessibility.
PKCε Inhibitor Peptide, a selective PKCε inhibitor, the addition of PKCε Inhibitor Peptide interferes with the interaction between PKCε and its anchoring protein, and abolishes the cardioprotective effects of PKCε [2]. ADP-induced thromboxane generation in human platelets pretreated with PKCε Inhibitor Peptide was more compared to the platelets pretreated with control peptide [4].
PKCε Inhibitor Peptide were used to inhibit PKCε expression and activity. Apigenin-7-O-β-D-(-6"-p-coumaroyl)-glucopyranoside (APG) preconditioning-induced PKCε translocation to the mitochondria and anti-mitochondrial oxidative stress effects were attenuated by PKCε-targeted ε-V1-2 treatment in IR-injured hearts [3].
References:
[1]. M Yedovitzky, et al. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J Biol Chem. 1997 Jan 17;272(3):1417-20.
[2]. L. Tang, Y. Peng, T. Xu, X. Yi, Y. Liu, Y. Luo, D. Yin, M. He. The effects of quercetin protect cardiomyocytes from A/R injury is related to its capability to increasing expression and activity of PK C epsilon protein.Mol. Cell. Biochem., 382 (2013), pp. 145-152
[3]. Zhu Y, Di S, Hu W, et al.. A new flavonoid glycoside (APG) isolated from Clematis tangutica attenuates myocardial ischemia/reperfusion injury via activating PKCε signaling.Biochim Biophys Acta Mol Basis Dis. 2017; 1863:701-711. doi: 10.1016/j.bbadis.2016.12.013
[4]. Yamini Saraswathy Bynagari, B-Tech., Bela Nagy, M.D., et al. nPKC Epsilon Negatively Regulates Platelet Functional Responses 2008. Blood (2008) 112 (11): 2855.
PKCε Inhibitor Peptide,也称为 εV1-2,是一种蛋白激酶 C ε (PKCε) 衍生肽,作为选择性 PKCε 抑制剂,抑制 PKCε 的易位 [1]。 PKCε 抑制肽是一种肽,旨在与天然 nPKC ε 竞争结合激活 C 激酶 (ε-RACK) 的 ε-受体,从而由于底物可及性降低而抑制 nPKC ε 催化活性。
PKCε Inhibitor Peptide,一种选择性的PKCε抑制剂,PKCε Inhibitor Peptide的加入会干扰PKCε与其锚定蛋白的相互作用,从而消除PKCε的心脏保护作用[2]。与用对照肽预处理的血小板[4]相比,用 PKCε 抑制剂肽预处理的人血小板中 ADP 诱导的血栓素生成更多。
PKCε 抑制肽用于抑制 PKCε 的表达和活性。芹菜素-7-O-β-D-(-6\-p-coumaroyl)-glucopyranoside (APG) preconditioning-induced PKCε translocation to the mitochondria and anti-mitochondrial oxidative stress effects were attenuated by PKCε-targeted ε-V1-2en_zh_2022q2.mdtreatment in IR-injured hearts [3].