European Journal of Pharmacology ( IF 4.2 ) Pub Date : 2023-08-22 , DOI: 10.1016/j.ejphar.2023.175999
João Carlos Martins Mafra 1 , Nubia Boechat 2 , Guilherme Pegas Teixeira 3 , Robson Xavier Faria 3
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Stimulation of the P2X7 receptor by extracellular adenosine 5'-triphosphate induces a series of responses in the organism, exceptionally protein cascades related to the proinflammatory process. This has made P2X7 a target for research on inflammatory diseases such as rheumatoid arthritis. Thus, the incessant search for new prototypes that aim to antagonize the action of P2X7 has been remarkable in recent decades, a factor that has already led to numerous clinical studies in humans. In this review, we present the key molecules developed over the years with potential inhibition of P2X7 and inflammation. In addition, an update with newly developed chemical classes with promising activity and results in clinical studies for human pathologies focusing on P2X7 inhibition.
中文翻译:

作为 P2X7 受体拮抗剂的合成分子:聚焦炎症性疾病治疗的药物化学更新
细胞外 5'-三磷酸腺苷对 P2X7 受体的刺激会在生物体中诱导一系列反应,特别是与促炎过程相关的蛋白质级联反应。这使得P2X7成为类风湿性关节炎等炎症性疾病的研究目标。因此,近几十年来,对旨在拮抗 P2X7 作用的新原型的不断探索是引人注目的,这一因素已经导致了大量的人类临床研究。在这篇综述中,我们介绍了多年来开发的具有 P2X7 和炎症潜在抑制作用的关键分子。此外,新开发的化学类别的更新具有良好的活性,并在针对 P2X7 抑制的人类病理学临床研究中取得了成果。