Bianca Laura Bernardoni, Concettina La Motta, Simone Carradori, Ilaria D'Agostino
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引用次数: 0
摘要
幽门螺旋杆菌(Hp)感染危及全球公共卫生安全,因为它极易引发严重疾病,如消化性溃疡、胃癌、糖尿病和心血管疾病。由于(多重)耐药性表型的增加,目前的疗法越来越不奏效,因此迫切需要具有创新作用机制的新型抗菌剂。在最有希望的药理靶点中,来自 Hp 的碳酸酐酶(EC:4.2.1.1),即 HpαCA 和 HpβCA,因其高可药性和在病原体在宿主体内生存的关键作用而崭露头角。因此,在过去的几十年中,这两种同工酶被分离出来并进行了表征,为研究它们的动力学和测试不同系列的抑制剂提供了机会。
Infections from Helicobacter pylori (Hp) are endangering Public Health safety worldwide, due to the associated high risk of developing severe diseases, such as peptic ulcer, gastric cancer, diabetes, and cardiovascular diseases. Current therapies are becoming less effective due to the rise of (multi)drug-resistant phenotypes and an urgent need for new antibacterial agents with innovative mechanisms of action is pressing. Among the most promising pharmacological targets, Carbonic Anhydrases (EC: 4.2.1.1) from Hp, namely HpαCA and HpβCA, emerged for their high druggability and crucial role in the survival of the pathogen in the host. Thereby, in the last decades, the two isoenzymes were isolated and characterized offering the opportunity to profile their kinetics and test different series of inhibitors.