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利用化学文库筛选鉴定组蛋白去乙酰化酶抑制剂作为斑马鱼中性粒细胞募集调节剂。

Identification of histone deacetylase inhibitors as neutrophil recruitment modulators in zebrafish using a chemical library screen.

机构信息

Laboratory of Developmental Biology, Department of Cell Biology and Genetics, School of Basic Medical Sciences, Chongqing Medical University, Chongqing 400016, China.

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE) and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, China.

出版信息

Dis Model Mech. 2023 Oct 1;16(10). doi: 10.1242/dmm.050056. Epub 2023 Oct 13.

Abstract

Tissue injury-induced neutrophil recruitment is a prerequisite for the initiation and amplification of inflammatory responses. Although multiple proteases and enzymes involved in post-translational modification (PTM) of proteins regulate leukocyte recruitment, an unbiased functional screen of enzymes regulating inflammatory leukocyte recruitment has yet to be undertaken. Here, using a zebrafish tail fin amputation (TFA) model to screen a chemical library consisting of 295 compounds that target proteases and PTM enzymes, we identified multiple histone deacetylase (HDAC) inhibitors that modulate inflammatory neutrophil recruitment. AR-42, a pan-HDAC inhibitor, was shown to inhibit neutrophil recruitment in three different zebrafish sterile tissue injury models: a TFA model, a copper-induced neuromast damage and mechanical otic vesicle injury (MOVI) model, and a sterile murine peritonitis model. RNA sequencing analysis of AR-42-treated fish embryos revealed downregulation of neutrophil-associated cytokines/chemokines, and exogenous supplementation with recombinant human IL-1β and CXCL8 partially restored the defective neutrophil recruitment in AR-42-treated MOVI model fish embryos. We thus demonstrate that AR-42 non-cell-autonomously modulates neutrophil recruitment by suppressing transcriptional expression of cytokines/chemokines, thereby identifying AR-42 as a promising anti-inflammatory drug for treating sterile tissue injury-associated diseases.

摘要

组织损伤诱导的中性粒细胞募集是炎症反应启动和放大的前提。尽管涉及蛋白质翻译后修饰 (PTM) 的多种蛋白酶和酶调节白细胞募集,但尚未对调节炎症性白细胞募集的酶进行无偏见的功能筛选。在这里,我们使用斑马鱼尾鳍截肢 (TFA) 模型筛选了一个包含 295 种靶向蛋白酶和 PTM 酶的化合物的化学文库,鉴定出多种组蛋白去乙酰化酶 (HDAC) 抑制剂可调节炎症性中性粒细胞募集。pan-HDAC 抑制剂 AR-42 被证明可抑制三种不同的斑马鱼无菌组织损伤模型中的中性粒细胞募集:TFA 模型、铜诱导的毛细胞损伤和机械耳囊损伤 (MOVI) 模型以及无菌鼠腹膜炎模型。用 AR-42 处理的鱼胚胎的 RNA 测序分析显示,中性粒细胞相关细胞因子/趋化因子的表达下调,外源性补充重组人 IL-1β 和 CXCL8 部分恢复了 AR-42 处理的 MOVI 模型鱼胚胎中缺陷的中性粒细胞募集。因此,我们证明 AR-42 通过抑制细胞因子/趋化因子的转录表达非细胞自主地调节中性粒细胞募集,从而鉴定出 AR-42 是治疗无菌组织损伤相关疾病的有前途的抗炎药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/64e9/10621070/7795a6643072/dmm-16-050056-g1.jpg

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