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吡喹酮:一种神秘而有效的药物。

Praziquantel: An Enigmatic, Yet Effective, Drug.

机构信息

School of Pharmacy and Biomolecular Sciences, University of Brighton, Brighton, UK.

出版信息

Methods Mol Biol. 2020;2151:1-8. doi: 10.1007/978-1-0716-0635-3_1.

Abstract

Praziquantel is a remarkably effective drug for the treatment of schistosomiasis. It has few side effects, some of which have been attributed to its inactive enantiomer. Few, if any, verified cases of drug resistance have been reported in a clinical setting. The preponderance of scientific evidence suggests that the drug works by dysregulating calcium homeostasis in the worm. Voltage-gated calcium channels have been proposed as the main pharmacological target of praziquantel, although no direct evidence of interaction with this protein is available. Here, the biochemical pharmacology of praziquantel is briefly reviewed and a hypothesis for its mechanism proposed. This hypothesis suggests that the drug works, in part, by disrupting an interaction between a voltage-gated calcium channel (SmCav1B) and an accessory protein, SmTAL1.

摘要

吡喹酮是一种治疗血吸虫病的非常有效的药物。它的副作用很少,其中一些副作用归因于其非活性对映异构体。在临床环境中,很少有(如果有的话)已证实的耐药病例报告。大量科学证据表明,该药物通过扰乱蠕虫体内的钙稳态而起作用。电压门控钙通道已被提议为吡喹酮的主要药理靶点,尽管没有与该蛋白相互作用的直接证据。在这里,简要回顾了吡喹酮的生化药理学,并提出了其作用机制的假设。该假设表明,该药物的作用部分是通过破坏电压门控钙通道(SmCav1B)和辅助蛋白 SmTAL1 之间的相互作用来实现的。

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