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Design, synthesis, and evaluation of a novel TRAIL-activated HDAC6 inhibitor for the treatment of pulmonary fibrosis

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文献详情

资源类型：
Pubmed体系：
作者：
Gao Ying[1] * ; Wang Pengfeng[2] * ; Hu Zan[3] ; Cui Hao[2,4] ; Chen Xuxi[1] ; Wang Liqun[1] ; Zhao Manyu[5] ; Qian Rui[1] ; Zhang Ling[1] ; Ye Tinghong[3] ; Zhu Yong[2] ; Yao Yuqin[1,3,*1] ;
机构： [1]West China Institute of Preventive and Medical Integration for Major Diseases, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China [2]School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China [3]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China [4]School of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei 230032, China [5]Department of Pulmonary and Critical Care Medicine, Precision Medicine Center, Frontiers Science Center for Disease-Related Molecular Network and West China Hospital, Sichuan University, Chengdu 610041, China
出处：
DOI： 10.1016/j.bmc.2024.117924
ISSN：

关键词： HDAC6 TRAIL Tumour Pulmonary fibrosis silicosis

摘要：
Pulmonary fibrosis (PF) is a common, severe, chronic, and progressive pulmonary interstitial disease characterized by rapid disease progression and high mortality. Despite the Food and Drug Administration (FDA)'s approval of two antifibrotic drugs, nintedanib and pirfenidone, effectively halting the progression of pulmonary fibrosis remains challenging. Histone deacetylase (HDAC) inhibitors have indeed emerged as an important class of antitumour drugs. However, their application in the treatment of fibrotic diseases is still relatively limited. Tumour necrosis factor-related apoptosis-inducing ligand (TRAIL) has the potential to inhibit fibrotic processes by inducing fibroblast apoptosis. In this study, we designed and synthesized a series of histone deacetylase 6 (HDAC6) inhibitors that activate TRAIL, among which compound 7e exhibited potent inhibitory activity against HDAC6, with an IC50 of 42.90 ± 4.96 nM and superior antiproliferative effects on fibroblasts. Therefore, we further investigated its anti-pulmonary fibrosis effect in mouse models of both idiopathic pulmonary fibrosis (IPF) and silicosis. Our results suggest that compound 7e is a promising candidate for the treatment of pulmonary fibrosis.Copyright © 2024 Elsevier Ltd. All rights reserved.

基金：
his study was supported by the National Natural Science Foundation of China (Program Nos. 82373548, U23A20495, U22A20359), the Science & Technology Department of Sichuan Province, China (Nos. 2023NSFSC0647, 2023NSFSC0649, 2023NSFSC0723) and the Postdoctoral Fellowship Program of CPSF (No. GZB20240471)
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2024]版：
无
最新[2023]版：
大类 | 3 区 医学
小类 | 2 区 有机化学 3 区 生化与分子生物学 3 区 药物化学
第一作者：
第一作者机构： [1]West China Institute of Preventive and Medical Integration for Major Diseases, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China
共同第一作者：
通讯作者：
通讯机构： [1]West China Institute of Preventive and Medical Integration for Major Diseases, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China [3]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China [*1]West China Institute of Preventive and Medical Integration for Major Diseases, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China
推荐引用方式(GB/T 7714)：
Gao Ying,Wang Pengfeng,Hu Zan,et al.Design, synthesis, and evaluation of a novel TRAIL-activated HDAC6 inhibitor for the treatment of pulmonary fibrosis[J].Bioorganic & Medicinal Chemistry.2024,113:117924.doi:10.1016/j.bmc.2024.117924.
APA：
Gao Ying,Wang Pengfeng,Hu Zan,Cui Hao,Chen Xuxi...&Yao Yuqin.(2024).Design, synthesis, and evaluation of a novel TRAIL-activated HDAC6 inhibitor for the treatment of pulmonary fibrosis.Bioorganic & Medicinal Chemistry,113,
MLA：
Gao Ying,et al."Design, synthesis, and evaluation of a novel TRAIL-activated HDAC6 inhibitor for the treatment of pulmonary fibrosis".Bioorganic & Medicinal Chemistry 113.(2024):117924

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