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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Antipain Y, a new antipain analog that inhibits neurotransmitter release from rat dorsal root ganglion neurons.
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Antipain Y, a new antipain analog that inhibits neurotransmitter release from rat dorsal root ganglion neurons.

机译：抗抛光Y，一种抑制来自大鼠背根神经节神经元的神经递质释放的新的抗抛光剂。

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摘要

Protease-activated receptors (PARs) are a unique class of G protein-coupled receptors activated by proteolytic cleavage of the receptor N terminus. The exposed new N terminus acts as a tethered ligand that interacts with extracellular loop 2 of its receptor, resulting in the initiation of intracellular signaling. To date, four PAR subtypes (PAR1-4) have been reported; these are expressed in a variety of organs and have important functions both physiologically and pathologically.1,2 Activation of PARs is initiated by several serine proteases. PAR1 is activated by thrombin and PAR2 is activated by several serine proteases, including trypsin and mast cell tryptase. Recently, it was reported that PAR activation closely relates to sensory neuron-associated disorders, such as inflammation, pain and pruritus. Consequently, inhibitors of PAR signaling, including protease inhibitors, antagonists and intracellular signaling inhibitor, are expected to be therapeutic candidates for these disorders and biological tools.
机译：蛋白酶活化受体（PARS）是由受体N末端的蛋白水解切割激活的独特G蛋白偶联受体。暴露的新N末端用作束缚配体，其与其受体的细胞外环2相互作用，导致细胞内信号传导。迄今为止，报告了四个PAR亚型（PAR1-4）;这些在各种器官中表达，并且在生理学和病理学上具有重要的功能.1,2通过几种丝氨酸蛋白酶引发解析的激活。 PAR1由凝血酶和PAR2激活，由几种丝氨酸蛋白酶激活，包括胰蛋白酶和肥大细胞胰蛋白酶。最近，据报道，PRAR激活与感官神经元相关疾病密切相关，例如炎症，疼痛和瘙痒。因此，预期对这些疾病和生物工具的蛋白酶抑制剂，拮抗剂和细胞内信号传导抑制剂包括蛋白酶抑制剂，拮抗剂和细胞内信号传导抑制剂的抑制剂。

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