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Small molecule inhibitors of mammalian thioredoxin reductase
Open accessAbstract
Mammalian thioredoxin reductases (TrxRs) are a family of NADPH-dependent flavoproteins with a penultimate selenocysteine residue at the carboxy-terminus. Besides their native substrate thioredoxins (Trx), the enzymes show a broad substrate specificity, at least partially, because of the C-terminal redox-active site that is easily accessible in the reduced form. TrxRs are ubiquitous in all kinds of cells and have a critical role in regulating intracellular redox signaling. In recent years, a wealth of evidence has revealed that overactivation/dysfunction of TrxRs is closely related to various diseases, especially in tumor development, and thus the past decades have witnessed an expanding interest in finding TrxRs inhibitors, which might be promising agents for cancer chemotherapy. Herein we reviewed the small molecule inhibitors of mammalian TrxRs, with an emphasis on those that have potential anticancer activity. This review includes the nonpatent references up to 2010 that deal with mammalian TrxR inhibitors.
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Cites
Thioredoxin Reductase Is Irreversibly Modified by Curcumin
Fang, J., Lu, J., & Holmgren, A. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m414645200 · Cited by 521
Self-citationLu, J., Papp, L. V., Fang, J., Rodriguez-Nieto, S., Zhivotovsky, B., & Holmgren, A. (2006) · Cancer Research · doi:10.1158/0008-5472.can-05-3310 · Cited by 326
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Cited by
Hanschmann, E.-M., Godoy, J. R., Berndt, C., Hudemann, C., & Lillig, C. H. (2013) · Antioxidants & Redox Signaling · doi:10.1089/ars.2012.4599 · Cited by 677
Targeting the Thioredoxin System for Cancer Therapy
Zhang, J., Li, X., Han, X., Liu, R., & Fang, J. (2017) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2017.06.001 · Cited by 460
Self-citationHighly Selective Off–On Fluorescent Probe for Imaging Thioredoxin Reductase in Living Cells
Zhang, L., Duan, D., Liu, Y., Ge, C., Cui, X., Sun, J., & Fang, J. (2014) · Journal of the American Chemical Society · doi:10.1021/ja408792k · Cited by 254
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Metadata
- Authors
- Cai, W., Zhang, L., Song, Y., Wang, B., Zhang, B., Cui, X., Hu, G., Liu, Y., Wu, J., & Fang, J.
- Venue
- Free Radical Biology and Medicine
- Publisher
- Elsevier BV
- Published
- 2012-01
- Volume
- 52
- Issue
- 2
- Pages
- 257-265
- ISSN
- 0891-5849 (ISSN-L)
- OpenAlex
- W2002462958
- Cited by
- 175
- References
- 2
- FWCI
- 3.64
- Type
- journal article
- Language
- en
- Open access
- green
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