L-JNKI-1是一种针对JNK的细胞渗透性多肽抑制剂。
L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.
L-JNKI-1 has been shown to effectively inhibit JNK activity in in vivo studies. It is shown that Ang II induces a dose-dependent pressor response, which was significantly attenuated by JNK inhibition[1]. It is also found that 10 μM L-JNKI-1 decreases phosphorylated c-Jun by 98% and phosphorylated Elk-1 by 100%. L-JNKI-1 is able to across the blood-brain barrier and penetrate neurons of adult mice and P5 rats within 1 h after an intraperitoneal injection[2].
[1]. Zhou MS, et al. Role of c-Jun N-terminal kinase in the regulation of vascular tone. J Cardiovasc Pharmacol Ther. 2010 Mar;15(1):78-83. [2]. Borsello T, et al. A peptide inhibitor of c-Jun N-terminal kinase protects against excitotoxicity and cerebral ischemia. Nat Med. 2003 Sep;9(9):1180-6.
Animal experiment: | Rats[1]Six-week-old male SD rats are used. The rats are injected with a bolus of JNK peptide inhibitor L-JNKI-1 (5 mg/kg) followed by infusion of JNKI 1 (5 mg/kg per hour) until the completion of the experiment. After a 30-minute infusion of JNK inhibitor, the pressor response to Ang II at the 3 doses described above is determined at 30-minute intervals[1]. |
参考文献: [1]. Zhou MS, et al. Role of c-Jun N-terminal kinase in the regulation of vascular tone. J Cardiovasc Pharmacol Ther. 2010 Mar;15(1):78-83. | |
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