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首页> 外文期刊>Journal of Medicinal Chemistry >Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from malassezia globosa, a potential antidandruff target
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Molecular cloning, characterization, and inhibition studies of a β-carbonic anhydrase from malassezia globosa, a potential antidandruff target

机译:潜在的去头皮屑目标马拉色小球藻β-碳酸酐酶的分子克隆,表征和抑制研究

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摘要

A β-carbonic anhydrase (CA, EC 4.2.1.1) from the fungal pathogen Malassezia globosa has been cloned, characterized, and studied for its inhibition with sulfonamides. This enzyme, designated MG-CA, has significant catalytic activity in the CO _2 hydration reaction and was inhibited by sulfonamides, sulfamates, and sulfamides with K _I in the nanomolar to micromolar range. Several sulfonamides have also been investigated for the inhibition of growth of M. globosa, M. dermatis, M. pachydermatic, and M. furfur in cultures, whereas a mouse model of dandruff showed that treatment with sulfonamides led to fragmented fungal hyphae, as for the treatment with ketoconazole, a clinically used antifungal agent. These data prompt us to propose MG-CA as a new antidandruff drug target.
机译:已经从真菌病原体球形小球藻(Malassezia globosa)的β-碳酸酐酶(CA,EC 4.2.1.1)进行了克隆,鉴定和研究,以研究其对磺酰胺的抑制作用。该酶称为MG-CA,在CO _2水合反应中具有显着的催化活性,并被纳摩尔至微摩尔范围内的K _I的磺酰胺,氨基磺酸盐和磺酰胺所抑制。还研究了几种磺胺类药物对培养物中球藻分枝杆菌,皮炎分枝杆菌,厚皮分枝杆菌和糠fur分枝杆菌的生长的抑制作用,而对头皮屑的小鼠模型显示,用磺酰胺处理可导致真菌菌丝断裂。用酮康唑(一种临床上使用的抗真菌剂)进行治疗。这些数据促使我们提出MG-CA作为新的去头皮屑药物靶标。

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