Vincenzi Fabrizio, Pasquini Silvia, Contri Chiara, Cappello Martina, Nigro Manuela, Travagli Alessia, Merighi Stefania, Gessi Stefania, Borea Pier Andrea, Varani Katia
Department of Translational Medicine, University of Ferrara, 44121 Ferrara, Italy.
Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, 44121 Ferrara, Italy.
Biomolecules. 2023 Sep 14;13(9):1387. doi: 10.3390/biom13091387.
Adenosine receptors (ARs) are widely acknowledged pharmacological targets yet are still underutilized in clinical practice. Their ubiquitous distribution in almost all cells and tissues of the body makes them, on the one hand, excellent candidates for numerous diseases, and on the other hand, intrinsically challenging to exploit selectively and in a site-specific manner. This review endeavors to comprehensively depict the substantial advancements witnessed in recent years concerning the development of drugs that modulate ARs. Through preclinical and clinical research, it has become evident that the modulation of ARs holds promise for the treatment of numerous diseases, including central nervous system disorders, cardiovascular and metabolic conditions, inflammatory and autoimmune diseases, and cancer. The latest studies discussed herein shed light on novel mechanisms through which ARs exert control over pathophysiological states. They also introduce new ligands and innovative strategies for receptor activation, presenting compelling evidence of efficacy along with the implicated signaling pathways. Collectively, these emerging insights underscore a promising trajectory toward harnessing the therapeutic potential of these multifaceted targets.
腺苷受体（ARs）是广泛认可的药理学靶点，但在临床实践中仍未得到充分利用。它们在人体几乎所有细胞和组织中的广泛分布，一方面使其成为众多疾病的理想靶点，另一方面，要以选择性和位点特异性的方式开发利用它们，本质上具有挑战性。本综述致力于全面描述近年来在调节ARs药物开发方面取得的重大进展。通过临床前和临床研究，已明显看出调节ARs有望治疗多种疾病，包括中枢神经系统疾病、心血管和代谢疾病、炎症和自身免疫性疾病以及癌症。本文讨论的最新研究揭示了ARs控制病理生理状态的新机制。它们还介绍了新的配体和受体激活的创新策略，并展示了令人信服的疗效证据以及相关的信号通路。总体而言，这些新见解突显了利用这些多面靶点治疗潜力的充满希望的轨迹。
