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天然来源的人中性粒细胞弹性蛋白酶抑制剂肽:概述。

Peptide Human Neutrophil Elastase Inhibitors from Natural Sources: An Overview.

机构信息

Department of Pharmacy, "G. d'Annunzio" University of Chieti-Pescara, 66100 Chieti, Italy.

Department of Biology, Science Faculty, Selcuk University, Konya 42130, Turkey.

出版信息

Int J Mol Sci. 2022 Mar 8;23(6):2924. doi: 10.3390/ijms23062924.

Abstract

Elastases are a broad group of enzymes involved in the lysis of elastin, the main component of elastic fibres. They are produced and released in the human body, mainly by neutrophils and the pancreas. The imbalance between elastase activity and its endogenous inhibitors can cause different illnesses due to their excessive activity. The main aim of this review is to provide an overview of the latest advancements on the identification, structures and mechanisms of action of peptide human neutrophil elastase inhibitors isolated from natural sources, such as plants, animals, fungi, bacteria and sponges. The discovery of new elastase inhibitors could have a great impact on the pharmaceutical development of novel drugs through the optimization of the natural . Bacteria produce mainly cyclic peptides, while animals provide for long and linear amino acid sequences. Despite their diverse natural sources, these elastase inhibitors show remarkable IC values in a range from nM to μM values, thus representing an interesting starting point for the further development of potent bioactive compounds on human elastase enzymes.

摘要

弹性蛋白酶是一组广泛的酶,参与弹性蛋白的裂解,弹性蛋白是弹性纤维的主要成分。它们在人体内产生和释放,主要由中性粒细胞和胰腺产生。弹性酶活性与其内源性抑制剂之间的失衡可能由于其过度活性而导致不同的疾病。本综述的主要目的是提供对从天然来源(如植物、动物、真菌、细菌和海绵)中分离出的人中性粒细胞弹性蛋白酶抑制剂的鉴定、结构和作用机制的最新进展的概述。通过对天然抑制剂的优化,发现新的弹性酶抑制剂可能会对新药的药物开发产生重大影响。细菌主要产生环状肽,而动物则提供长而线性的氨基酸序列。尽管它们的天然来源多种多样,但这些弹性酶抑制剂在纳摩尔到微摩尔范围内表现出显著的 IC 值,因此为进一步开发针对人弹性酶的有效生物活性化合物提供了一个有趣的起点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5051/8954713/c0fa7b891208/ijms-23-02924-g001.jpg

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