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Inhibition of the newly discovered β‑carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with inorganic anions and small molecules
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2020-10-07 , DOI: 10.1016/j.jinorgbio.2020.111274
Linda J Urbański 1 , Andrea Angeli 2 , Vesa P Hytönen 3 , Anna Di Fiore 4 , Seppo Parkkila 3 , Giuseppina De Simone 4 , Claudiu T Supuran 2
Affiliation  

The protozoan pathogen Trichomonas vaginalis encodes two carbonic anhydrases (CAs, EC 4.2.1.1) belonging to the β-class. One of these enzymes, T. vaginalis carbonic anhydrase 1 (TvaCA1), was recently cloned and characterized by our group, and its X-ray crystal structure reported. No inhibitors of this enzyme were reported up until now. Here we investigated the inhibition of TvaCA1 with inorganic anions and small molecules and observed that thiocyanate, cyanide, selenite, selenocyanate and divanadate are sub-millimolar inhibitors, whereas sulfamide, sulfate, phenylboronic acid and phenylarsonic acid are micromolar inhibitors. Finding effective TvaCA1 inhibitors may be useful for developing new antiprotozoan drugs.



中文翻译:

无机阴离子和小分子抑制原生动物病原体阴道毛滴虫中新发现的β-碳酸酐酶

原生动物病原体阴道毛滴虫编码两个属于β-类的碳酸酐酶(CAs,EC 4.2.1.1)。这些酶之一,即阴道锥虫碳酸酐酶1(TvaCA1),最近被我们的研究小组克隆和鉴定,并报道了其X射线晶体结构。迄今为止,尚未报道该酶的抑制剂。在这里,我们研究了无机阴离子和小分子对TvaCA1的抑制作用,并观察到硫氰酸盐,氰化物,亚硒酸盐,硒氰酸盐和分明酸盐是亚毫摩尔级抑制剂,而磺酰胺,硫酸盐,苯基硼酸和苯基ar磺酸是微摩尔抑制剂。寻找有效的TvaCA1抑制剂可能对开发新的抗原生动物药物有用。

更新日期:2020-10-15
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