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发现抑制甲酰甘氨酸生成酶活性的五肽及其对……的潜在抗菌作用。

The discovery of penta-peptides inhibiting the activity of the formylglycine-generating enzyme and their potential antibacterial effects against .

作者信息

Asiimwe Nicholas, Al Mazid Mohammad Faysal, Jeong Yong Taek, Lee Juyong, Lee Jun-Seok

机构信息

Bio-Med Program, KIST-School UST South Korea.

Department of Pharmacology, Korea University College of Medicine South Korea

出版信息

RSC Adv. 2022 Jun 29;12(29):18884-18888. doi: 10.1039/d2ra03379h. eCollection 2022 Jun 22.

DOI:10.1039/d2ra03379h
PMID:35873338
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9241360/
Abstract

The formylglycine-generating enzyme is a key regulator that converts sulfatase into an active form. Despite its key role in many diseases, enzyme activity inhibitors have not yet been reported. In this study, we investigated penta-peptide ligands for FGE activity inhibition and discovered two hit peptides. In addition, the lead peptides also showed potential antibacterial effects in a model.

摘要

甲酰甘氨酸生成酶是一种关键调节因子，可将硫酸酯酶转化为活性形式。尽管其在许多疾病中起关键作用，但尚未有酶活性抑制剂的报道。在本研究中，我们研究了用于抑制FGE活性的五肽配体，并发现了两种有活性的肽。此外，先导肽在模型中也显示出潜在的抗菌作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/57a9502547c3/d2ra03379h-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/8e062ed869ff/d2ra03379h-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/9734a158a33a/d2ra03379h-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/4a922537f13a/d2ra03379h-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/57a9502547c3/d2ra03379h-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/8e062ed869ff/d2ra03379h-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/9734a158a33a/d2ra03379h-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/4a922537f13a/d2ra03379h-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dfde/9241360/57a9502547c3/d2ra03379h-f4.jpg

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JIMD Rep. 2020 Dec 8;58(1):80-88. doi: 10.1002/jmd2.12189. eCollection 2021 Mar.
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