Baqi Younis
Department of Chemistry, Faculty of Science, Sultan Qaboos University, PO Box 36, Postal Code 123, Muscat, Oman.
Mini Rev Med Chem. 2015;15(1):21-33. doi: 10.2174/1389557515666150219115141.
Ecto-nucleotidases are nucleotide metabolizing enzymes that are divided into four different families; nucleoside triphosphate diphosphohydrolases (NTPDases), ecto-5'-nucleotidase (ecto-5'-NT), nucleotide pyrophosphatase/phosphodiesterases (NPPs), and alkaline phosphatases (APs). These enzymes are responsible for the hydrolysis of nucleotidases (nucleoside 5'-triphosphates, 5'-diphosphates and 5'-monophosphates). Ecto-nucleotidases modulate P1- and P2-receptor-mediated signaling. Alterations in extracellular nucleotide and adenosine level can increase or decrease P1 and P2 activity. Potent and selective ligands for certain ectonucleotidase are important as pharmacological tools to investigate the (patho)physiological roles of these enzymes. Furthermore, such ligands are required to study their potential as novel drugs, e.g., as immunomodulatory agents, for the treatment of cancer, cardiovascular or central nervous system disorders. Hence, this review aims to provide an overview of ecto-nucleotidases inhibitors developed so far.
外核苷酸酶是核苷酸代谢酶，分为四个不同的家族：核苷三磷酸二磷酸水解酶（NTPDases）、外5'-核苷酸酶（ecto-5'-NT）、核苷酸焦磷酸酶/磷酸二酯酶（NPPs）和碱性磷酸酶（APs）。这些酶负责核苷酸（核苷5'-三磷酸、5'-二磷酸和5'-单磷酸）的水解。外核苷酸酶调节P1和P2受体介导的信号传导。细胞外核苷酸和腺苷水平的改变可增加或降低P1和P2活性。某些外核苷酸酶的强效和选择性配体作为研究这些酶的（病理）生理作用的药理学工具很重要。此外，需要此类配体来研究它们作为新型药物的潜力，例如作为免疫调节剂，用于治疗癌症、心血管或中枢神经系统疾病。因此，本综述旨在概述迄今为止开发的外核苷酸酶抑制剂。
