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幽门螺杆菌 CAs 抑制。

Helicobacter pylori CAs inhibition.

机构信息

Department of Pharmacy, University of Pisa, Pisa, Italy.

Department of Pharmacy, G. d'Annunzio University of Chieti-Pescara, Chieti, Italy.

出版信息

Enzymes. 2024;55:213-241. doi: 10.1016/bs.enz.2024.05.013. Epub 2024 Jun 8.

Abstract

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.

摘要

幽门螺杆菌(Hp)感染正在危及全球公共卫生安全,因为它与发生严重疾病(如消化性溃疡、胃癌、糖尿病和心血管疾病)的高风险相关。由于(多)耐药表型的出现,当前的治疗方法变得越来越不有效,因此迫切需要具有创新作用机制的新型抗菌药物。在最有前途的药理学靶标中,幽门螺杆菌的碳酸酐酶(EC:4.2.1.1),即 HpαCA 和 HpβCA,因其高可成药性和在病原体在宿主中生存中的关键作用而受到关注。因此,在过去几十年中,这两种同工酶被分离和表征,从而有机会对其动力学进行分析并测试不同系列的抑制剂。

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