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来自蓝藻(KUCC C2)的 Aeruginosin 525(AER525):一种新型丝氨酸蛋白酶抑制剂。

Aeruginosin 525 (AER525) from Cyanobacterium Sp. (KUCC C2): A New Serine Proteases Inhibitor.

机构信息

Marine Research Institute, Klaipėda University, Universiteto av. 17, LT-92294 Klaipėda, Lithuania.

Institute of Oceanology, Polish Academy of Sciences, Powstańców Warszawy 55, PL-81712 Sopot, Poland.

出版信息

Mar Drugs. 2024 Nov 8;22(11):506. doi: 10.3390/md22110506.

Abstract

Aeruginosins (AERs) are one of the most common classes of cyanobacterial peptides synthesised through a hybrid non-ribosomal peptide synthase/polyketide synthase pathway. They have been found in , , /, and The presence of AER in isolated from the Curonian Lagoon was reported for the first time in our previous work. Here, the structure of aeruginosin 525 (AER525), isolated from sp. KUCC C2, was characterised based on high-resolution mass spectrometry. This new AER variant shows potent activity against thrombin. It also inhibits trypsin and carboxypeptidase A but has no effect on elastase and chymotrypsin. In terms of the -terminal residue and biological activity, AER525 displaces some similarity to dysinosins, which belongs to the most potent inhibitors of thrombin among AERs. The findings underline the potential of AER525 as a new anticoagulant agent.

摘要

苍蓝素(AERs)是通过杂合非核糖体肽合酶/聚酮合酶途径合成的最常见的一类蓝藻肽之一。它们存在于 、 、 、 中。我们之前的工作首次报道了在从库尔斯沙嘴泻湖分离出的 中存在苍蓝素。在这里,我们基于高分辨率质谱法对从 sp. KUCC C2 中分离出的苍蓝素 525(AER525)的结构进行了表征。这种新的 AER 变体对凝血酶表现出很强的活性。它还抑制胰蛋白酶和羧肽酶 A,但对弹性蛋白酶和糜蛋白酶没有影响。就 -末端残基和生物活性而言,AER525 与 dysinosins 有一些相似之处,dysinosins 是 AERs 中凝血酶最强抑制剂之一。这些发现强调了 AER525 作为新型抗凝剂的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a61/11595689/33da86da077f/marinedrugs-22-00506-g001.jpg

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