Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe

被引：17

作者：

Kolt, Sonia ^{[1
]}

Janiszewski, Tomasz ^{[1
]}

Kaiserman, Dion ^{[2
]}

Modrzycka, Sylwia ^{[1
]}

Snipas, Scott J. ^{[3
]}

Salvesen, Guy ^{[3
]}

Drag, Marcin ^{[1
,3
]}

Bird, Phillip, I ^{[2
]}

Kasperkiewicz, Paulina ^{[1
]}

机构：

[1] Wroclaw Univ Sci & Technol, Dept Chem Biol & Bioimaging, PL-50370 Wroclaw, Poland

[2] Monash Univ, Monash Biomed Discovery Inst, Dept Biochem & Mol Biol, Clayton, Vic 3800, Australia

[3] NCI, Designated Canc Ctr, Sanford Burnham Prebys Med Discovery Inst, La Jolla, CA 92037 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2020年 / 63卷 / 06期

关键词：

LYMPHOCYTE PROTEASE GRANZYME; MEDIATED APOPTOSIS; SUBSTRATE LIBRARY; SERINE PROTEASES; MOUSE GRANZYME; TARGET; DEATH; SET; INHIBITORS; GRANULES;

D O I：

10.1021/acs.jmedchem.9b02042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：3359 / 3369

页数：11

共 35 条

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