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首页> 外文期刊>Expert opinion on therapeutic targets >Bradykinin receptors as a therapeutic target.
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Bradykinin receptors as a therapeutic target.

机译：缓激肽受体作为治疗靶标。

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摘要

Biologically-active kinins, including bradykinin (BK) and Lys(0)-BK (kallidin), are short-lived peptide mediators predominantly generated by the enzymatic action of kallikreins on kininogen precursors. A diverse spectrum of physiological and pathological actions attributed to local kinin production is a consequence of the activation of G-protein-coupled receptors (GPCRs). Currently, two major subtypes of kinin receptor, designated B(1) and B(2), are recognised, although there is much evidence for pharmacological heterogeneity, particularly within the B(2) receptors. Considering these facts and the widespread distribution of kinin receptors in many human tissues, it is no surprise that the therapeutic potential of kinins and kinin receptor antagonists remains the focus of numerous investigations. Studies in animals and animal tissues, instrumental in elucidating the biological roles of kinins, are well-documented in numerous excellent reviews. Unfortunately, and despite the enormous potential illustrated by animal studies, attempts to develop kinin analogues as therapeutic agents to combat human disease have largely proven disappointing. Consequently, this review selectively focuses upon studies that are directly relevant to the targeting of human BK receptors as a therapeutic intervention. In addition to providing a succinct review of well-documented pathological conditions to which kinin receptors contribute, the authors have also included more recent data that illustrate new avenues for the therapeutic application of kinin analogues.
机译：具有生物活性的激肽，包括缓激肽（BK）和Lys（0）-BK（激肽），是短暂的肽介体，主要由激肽释放酶对激肽原的前体的酶促作用产生。 G蛋白偶联受体（GPCR）活化的结果是归因于局部激肽产生的多种生理和病理作用。目前，虽然有很多药理学异质性的证据，特别是在B（2）受体内，但公认有激肽受体的两种主要亚型，分别为B（1）和B（2）。考虑到这些事实以及激肽受体在许多人体组织中的广泛分布，激肽和激肽受体拮抗剂的治疗潜力仍然是众多研究的重点也就不足为奇了。在动物和动物组织中的研究，阐明了激肽的生物学作用，在许多出色的评论中都有详细记录。不幸的是，尽管动物研究显示出巨大的潜力，但开发激肽类似物作为对抗人类疾病的治疗剂的尝试在很大程度上令人失望。因此，本综述选择性地关注与将人BK受体作为治疗干预目标直接相关的研究。除了简要回顾激肽受体所致的病理状况外，作者还提供了更多近期数据，这些数据说明了激肽类似物的治疗性应用的新途径。

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