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Targeting the 'Janus face' of the B2-bradykinin receptor

机译：靶向B2-缓激肽受体的“剑齿面”

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Introduction: Kinins are main active mediators of the kallikrein-kinin system (KKS) via bradykinin type 1 inducible (B1R) and type 2 constitutive (B2R) receptors. B2R mediates most physiological bradykinin (BK) responses, including vasodilation, natriuresis, NO, prostaglandins release. Areas covered: The article summarizes knowledge on kinins, B2R signaling and biological functions; highlights crosstalks between B2R and renin-angiotensin system (RAS). The double role (Janus face) in physiopathology, namely the beneficial protection of the endothelium, which forms the basis for the therapeutical utilization of B2 receptor agonists, on the one side, and the involvement of B2R in inflammation or infection diseases and in pain mechanisms, which justifies the use of B2R antagonists, on the other side, is extensively analyzed. Expert opinion: For decades, the B2R has been unconsciously activated during angiotensin-converting enzyme inhibitor (ACEI) or angiotensin receptor blocker (ARB) treatments. Whether direct B2R targeting with stable agonists could bring additional therapeutic benefit to RAS inhibition should be investigated. Efficacy, established in experimental models, should be confirmed by translational studies in cardiovascular pathologies, glaucoma, Duchenne cardiopathy and during brain cancer therapy. The other face of B2R is targeted by antagonists already approved to treat hereditary angioedema. The use of antagonists could be extended to other angioedema and efficacy tested against acute pain and inflammatory diseases.
机译：简介：激肽是激肽释放酶激肽系统（KKS）的主要活性介质，通过1型缓激肽诱导型（B1R）和2型组成型（B2R）受体发生。 B2R介导大多数生理缓激肽（BK）反应，包括血管舒张，钠尿，NO，前列腺素释放。涵盖的领域：本文总结了有关激肽，B2R信号传导和生物学功能的知识;突出显示了B2R与肾素-血管紧张素系统（RAS）之间的串扰。生理病理学中的双重作用（Janus脸），即对内皮的有益保护，一方面形成了B2受体激动剂的治疗利用基础，另一方面B2R参与了炎症或感染性疾病以及疼痛机制的形成另一方面，对使用B2R拮抗剂的合理性进行了广泛分析。专家意见：几十年来，在血管紧张素转换酶抑制剂（ACEI）或血管紧张素受体阻滞剂（ARB）治疗期间，B2R一直在不知不觉中被激活。应该研究用稳定激动剂直接靶向B2R是否可以为RAS抑制带来其他治疗益处。在实验模型中确定的功效，应通过对心血管疾病，青光眼，杜兴氏心脏病和脑癌治疗期间的转化研究加以证实。 B2R的另一面是已被批准用于治疗遗传性血管性水肿的拮抗剂的靶标。拮抗剂的使用可以扩展到其他血管性水肿，并可以针对急性疼痛和炎性疾病进行功效测试。

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