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Prorenin receptor blockers: effects on cardiovascular complications of diabetes and hypertension

机译:肾上腺素受体阻滞剂:对糖尿病和高血压的心血管并发症的影响

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摘要

When the 'handle region' of the prorenin prosegment interacts with the (pro)renin receptor, the prorenin molecule partially changes the conformation to an enzymatically active state. On the other hand, the receptor triggers its own intracellular signalling pathways independent of the renin-angiotensin system (RAS). The 'handle region' peptide competitively binds to the receptor as a decoy peptide and inhibits both the non-proteo-lytic activation of prorenin and the RAS-independent intracellular signals. Therefore, prorenin receptor blockers including the decoy peptide may have superior benefits on end-organ damage in diabetes and hypertension compared with conventional RAS inhibitors.
机译:当prorenin prosegment的“句柄区域”与(pro)renenin受体相互作用时,prorenin分子将构象部分改变为酶促活性状态。另一方面,该受体触发其自身的细胞内信号传导途径,而与肾素-血管紧张素系统(RAS)无关。 “手柄区域”肽作为诱饵肽竞争性地与受体结合,并抑制蛋白原的非蛋白水解激活和不依赖RAS的细胞内信号。因此,与常规RAS抑制剂相比,包括诱饵肽在内的prorenin受体阻滞剂对糖尿病和高血压患者的终末器官损害具有更好的益处。

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