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Is the adenosine A2B ‘biased’ receptor a valuable target for the treatment of pulmonary arterial hypertension?
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-05-07 , DOI: 10.1016/j.drudis.2018.05.005
Mafalda Bessa-Gonçalves , Bruno Bragança , Eduardo Martins-Dias , Paulo Correia-de-Sá , Ana Patrícia Fontes-Sousa

Pulmonary arterial hypertension (PAH) is a maladaptive disorder characterized by increased pulmonary vascular resistance leading to right ventricular failure and death. Adenosine released by injured tissues, such as the lung and heart, influences tissue remodeling through the activation of adenosine receptors. Evidence regarding activation of the low-affinity A2BAR by adenosine points towards pivotal roles of this receptor in processes associated with both acute and chronic lung diseases. Conflicting results exist concerning the beneficial or detrimental roles of the A2B ‘biased’ receptor in right ventricular failure secondary to PAH. In this review, we discuss the pros and cons of manipulating A2BARs as a putative therapeutic target in PAH.



中文翻译:

腺苷A 2B “偏倚”受体是否是治疗肺动脉高压的重要靶标?

肺动脉高压(PAH)是一种适应不良的疾病,其特征是肺血管阻力增加,导致右心室衰竭和死亡。受伤的组织(如肺和心脏)释放的腺苷会通过激活腺苷受体来影响组织重塑。关于腺苷激活低亲和力A 2B AR的证据表明,该受体在与急性和慢性肺部疾病相关的过程中起着关键作用。关于A 2B “偏向”受体在继发于PAH的右心衰竭中的有益或有害作用存在矛盾的结果。在这篇综述中,我们讨论了将A 2B ARs作为PAH中公认的治疗靶点的利弊。

更新日期:2018-05-07
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