Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe.,Journal of Medicinal Chemistry

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Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-03-16 , DOI: 10.1021/acs.jmedchem.9b02042
Sonia Kołt ₁ , Tomasz Janiszewski ₁ , Dion Kaiserman ₂ , Sylwia Modrzycka ₁ , Scott J Snipas ₃ , Guy Salvesen ₃ , Marcin Dra G _{1,

3} , Phillip I Bird ₂ , Paulina Kasperkiewicz ₁

Affiliation

Cytotoxic T-lymphocytes (CTLs) and natural killer cells (NKs) kill compromised cells to defend against tumor and viral infections. Both effector cell types use multiple strategies to induce target cell death including Fas/CD95 activation and the release of perforin and a group of lymphocyte granule serine proteases called granzymes. Granzymes have relatively broad and overlapping substrate specificities and may hydrolyze a wide range of peptidic epitopes; it is therefore challenging to identify their natural and synthetic substrates and to distinguish their localization and functions. Here, we present a specific and potent substrate, an inhibitor, and an activity-based probe of Granzyme A (GrA) that can be used to follow functional GrA in cells.

中文翻译：

基于荧光活性的探针检测NK92细胞中的活性颗粒酶A。

细胞毒性T淋巴细胞（CTL）和自然杀伤细胞（NK）杀死受损的细胞，以防御肿瘤和病毒感染。两种效应细胞类型均使用多种策略诱导靶细胞死亡，包括Fas / CD95活化和穿孔素的释放以及一组称为颗粒酶的淋巴细胞颗粒丝氨酸蛋白酶。颗粒酶具有相对广泛和重叠的底物特异性，并可以水解多种肽表位；因此，鉴定其天然和合成底物并区分其定位和功能是一项挑战。在这里，我们介绍了一种特定而有效的底物，一种抑制剂以及一种可用于追踪细胞中功能性GrA的颗粒酶A（GrA）的基于活性的探针。

更新日期：2020-03-19

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