Cited by 460Redox biology and oxidative stressGenomics, phytochemicals, and oxidative stressGlutathione Transferases and Polymorphisms

Targeting the Thioredoxin System for Cancer Therapy

Zhang, Junmin, Li, Xinming, Han, Xiao, Liu, Ruijuan, Fang, Jianguo·2017·Trends in Pharmacological Sciences

Abstract

Thioredoxin (Trx) and thioredoxin reductase (TrxR) are essential components of the Trx system which plays pivotal roles in regulating multiple cellular redox signaling pathways. In recent years TrxR/Trx have been increasingly recognized as an important modulator of tumor development, and hence targeting TrxR/Trx is a promising strategy for cancer treatment. In this review we first discuss the structural details of TrxR, the functions of the Trx system, and the rational of targeting TrxR/Trx for cancer treatment. We also highlight small-molecule TrxR/Trx inhibitors that have potential anticancer activity and review their mechanisms of action. Finally, we examine the challenges of developing TrxR/Trx inhibitors as anticancer agents and perspectives for selectively targeting TrxR/Trx.

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Crossref · 10.1016/j.tips.2017.06.001

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Authors
Zhang, J., Li, X., Han, X., Liu, R., & Fang, J.
Affiliations
State Key Laboratory of Applied Organic Chemistry (CN)
Corresponding author
Fang, Jianguo
Venue
Trends in Pharmacological Sciences
Publisher
Elsevier BV
Published
2017-09
Volume
38
Issue
9
Pages
794-808
ISSN
0165-6147 (ISSN-L)
OpenAlex
W2709224048
Cited by
460
References
120
Citations by year
2026: 38 · 2025: 55 · 2024: 55 · 2023: 66 · 2022: 61 · 2021: 61 · 2020: 45 · 2019: 47 · 2018: 28 · 2017: 3
FWCI
3.22
Type
journal article
Language
en
Open access
closed
Locations
  • Trends in Pharmacological Sciences (publishedVersion)
  • PubMed (publishedVersion)
  • Lanzhou University Institutional Repository (submittedVersion)
Funders
  • Natural Science Foundation (21572093)
  • Fundamental Research Funds (lzujbky-2016-49)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Redox biology and oxidative stress
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics, phytochemicals, and oxidative stress
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Glutathione Transferases and Polymorphisms
Keywords
thioredoxin, thioredoxin reductase, redox signaling, cancer therapy, small molecule inhibitors, anticancer agents, carcinogenesis, selective targeting
MeSH terms
Animals, Antineoplastic Agents, Enzyme Inhibitors, Humans, Neoplasms, Oxidation-Reduction, Structure-Activity Relationship, Thioredoxins, Thioredoxin-Disulfide Reductase, Small Molecule Libraries, Molecular Targeted Therapy

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