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The aldosterone receptor - new insights?

机译:醛固酮受体-新见解?

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Aldosterone,or mineralocorticoid,excess plays an important role in the patho-physiology of cardiac disease.This response is mediated through the mineralocorticoid receptor (MR).Although blockade of the MR has been shown to reduce mortality in cardiac failure,therapy may be limited by the hyperkalae-mia that results from blockade of the renal MR.It is now well established for a number of steroid receptors that tissue-specific antagonism and agonism can be achieved by the so-called selective receptor modulators.Recently,three groups have crystallised the ligand-binding pocket of the MR,and each reveal a structure that is similar to that of the other steroid receptors.This raises the possibility that cardiac-specific antagonists of the MR may be developed that avoid the potassium retention seen with blockade of the renal MR.
机译:醛固酮或盐皮质激素的过量在心脏疾病的病理生理中起着重要作用。这种反应是通过盐皮质激素受体(MR)介导的。尽管已证实对MR的阻断可降低心力衰竭的死亡率,但治疗可能受到限制由肾MR阻滞引起的高钾血症引起的。现在已经对许多类固醇受体充分证实了可以通过所谓的选择性受体调节剂实现组织特异性拮抗和激动作用。最近,三个基团已经结晶MR的配体结合口袋,每个都显示出与其他类固醇受体相似的结构。这增加了开发MR的心脏特异性拮抗剂的可能性,从而避免了钾的滞留(由于钾离子的阻滞)肾MR。

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