首页|High-throughput fluorescent screening of thioredoxin reductase inhibitors to inhibit Mycobacterium tuberculosis

High-throughput fluorescent screening of thioredoxin reductase inhibitors to inhibit Mycobacterium tuberculosis

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Tuberculosis(TB)is a chronic infectious disease,which is caused by the pathogen Mycobacterium tubercu-losis(Mtb)and reemerged as a global health risk with a significant proportion of multi-drug resistant and extensively drug resistant TB cases.It is very urgent to find some novel high-confidence drug targets in Mtb for discovering the effective anti-TB agents.Thioredoxin reductase(TrxR)has been identified to be a highly viable target for anti-TB drugs for its important role in protecting the pathogen from thiol-specific oxidizing stress,regulating intracellular dithiol/disulfide homeostasis and DNA replication and repair.In the present work,a near-infrared(NIR)fluorescent probe DDAT was developed for the detection of TrxR activity and used to high-throughput screen the TrxR inhibitors from natural products.Two screened TrxR inhibitors from Sappan Lignum and microbial metabolites that were further used to inhibit Mycobacterium tuberculosis.All the results indicate that DDAT is a practical fluorescent molecular tool for the discovery of potential anti-TB drugs.

Thioredoxin reductaseNIR fluorescent probeFluorescence imagingHigh-throughput screening inhibitorsInhibit Mycobacterium tuberculosis

Fei Yan、Xin Zhao、Ruibo Li、Xiuyan Han、Qiulong Yan、Lei Feng、Xiulan Xin、Jingnan Cui、Xiaochi Ma

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Second Affiliated Hospital,Dalian Medical University,Dalian 116044,China

State Key Laboratory of Fine Chemicals,Dalian University of Technology,Dalian 116024,China

Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy,Xuzhou Medical University,Xuzhou 221004,China

School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang 453007,China

College of Bioengineering,Beijing Polytechnic,Beijing 100029,China

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国家自然科学基金国家自然科学基金Open Research Fund of the School of Chemistry and Chemical Engineering,Henan Normal University for supportResearch on National Reference Material and Product Development of Natural ProductsResearch on National Reference Material and Product Development of Natural Products

81930112822250482021YB07SG030801Beijing Polytechnic

2024

10.1016/j.cclet.2023.108504

中国化学快报(英文版)
中国化学会

中国化学快报(英文版)

CSTPCD
影响因子：0.771
ISSN：1001-8417
年,卷(期)：2024.35(3)
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