epsilon-v1-2

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membranes, blocking activation.[2] PKC inhibitor peptide is commonly used in cells to evaluate the role of PKC in various cellular responses.[3],[4],[5]

Epsilon-V1-2, Cys-conjugated 是 εPKC 特异性抑制剂，通过阻断 εPKC 与 εRACK 锚定蛋白之间的相互作用，抑制 εPKC 易位及 MARCKS 磷酸化，从而表现生物活性。该肽将半胱氨酸残基接到 C 末端，以形成与载体蛋白的 SS 键。当序列 N 末端为谷氨酰胺 (Q) 或谷氨酸 (E) 时，肽可自发生成焦谷氨酰 (pGlu)。Q或E到pGlu的转化属于自然过程，并且pGlu的疏水性γ-内酰胺环对提高肽对胃肠道蛋白酶的稳定性起关键作用。在 HPLC 分析中，焦谷氨酰肽作为肽纯度的一部分进行检测，视为这类肽的典型子集。