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背景说明：Epsilon-V1-2 (ε-V1-2) 是一种 PKCε 衍生肽，是一种选择性 PKCε 抑制剂。Epsilon-V1-2 抑制 PKCε 的转运，但不抑制 α-，β-和 δPKC 的转运。Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
In Vivo：Epsilon-V1-2 (20 mg/kg/day; osmotic pumps; daily; for 4 weeks) treatment significantly improves the beating score in a murine heterotopic transplantation model. Epsilon-V1-2 reduces infiltration of macrophages and T cells into the cardiac grafts, and decreases parenchymal fibrosis. Epsilon-V1-2 treatment almost abolishes the rise in pro-fibrotic cytokine, TGF-β and monocyte recruiting chemokine MCP-1 levels.
In Vitro：Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide containing the site for its specific receptor for activated C kinase (RACK), inhibits translocation of PKCε and reduces insulin response to glucose.
Epsilon-V1-2 (ε-V1-2; 1 μM, 24 hours) treatment significantly inhibits Oleic acid (OA)-induced connexin 43 (Cx43) Ser368 phosphorylation and prevents OA-induced gap junction disassembly in cardiomyocytes.
参考文献：[1] Lamy, C. et al. Tetrahedron Lett 46, 6177 (2007);
[2] Brandman, R. et al. J. Biol. Chem. 282, 4113 (2007).
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