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碳酸酐酶抑制剂作为新型抗寄生虫药物的研究进展。

Advances in the Development of Carbonic Anhydrase Inhibitors as New Antiprotozoal Agents.

机构信息

Laboratorio de Biotecnología Farmacéutica, Centro de Biotecnología Genómica, Instituto Politécnico Nacional, Reynosa 88710, Tamaulipas, México.

Departamento de Biotecnología Farmacéutica, Facultad de Medicina Veterinaria y Zootecnia, Universidad Autónoma de Nuevo León, Gral. Escobedo, 66050, México.

出版信息

Curr Med Chem. 2024;31(41):6735-6759. doi: 10.2174/0109298673249553231018070920.

Abstract

BACKGROUND

Parasitic diseases are a public health problem despite the existence of drugs for their treatment. These treatments have variable efficacy and, in some cases, serious adverse effects. There has been interest in the enzyme carbonic anhydrase (CA) in the last two decades since it is essential in the life cycle of various parasites due to its important participation in processes such as pyrimidine synthesis, HCO - transport across cell membranes, and the maintenance of intracellular pH and ion transport (Na, K, and H), among others.

OBJECTIVE

In this review, CA was analyzed as a pharmacological target in etiological agents of malaria, American trypanosomiasis, leishmaniasis, amoebiasis, and trichomoniasis. The CA inhibitors´ design, binding mode, and structure-activity relationship are also discussed.

CONCLUSION

According to this review, advances in discovering compounds with potent inhibitory activity suggest that CA is a candidate for developing new antiprotozoal agents.

摘要

背景

寄生虫病是一个公共卫生问题,尽管已有治疗药物。这些治疗方法的疗效各不相同,在某些情况下还会产生严重的不良反应。在过去的二十年中,人们对酶碳酸酐酶(CA)产生了兴趣,因为它在各种寄生虫的生命周期中是必不可少的,因为它在嘧啶合成、HCO3-跨细胞膜运输以及细胞内 pH 值和离子运输(Na、K 和 H)等过程中发挥着重要作用。

目的

本综述分析了 CA 作为疟疾、美洲锥虫病、利什曼病、阿米巴病和滴虫病等病因药物的药理学靶点。还讨论了 CA 抑制剂的设计、结合模式和结构-活性关系。

结论

根据本综述,在发现具有强抑制活性的化合物方面的进展表明,CA 是开发新型抗原生动物药物的候选药物。

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