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Thioredoxin-dependent system. Application of inhibitors.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 362-371. - Publication Year :
- 2021
-
Abstract
- One of the systems responsible for maintaining cellular redox homeostasis is the thioredoxin-dependent system. An equally important function of this system is the regulation of the expression of many proteins by the transcription factor NF-κB or the apoptosis regulating kinase (ASK-1). Since it has been shown that the Trx-dependent system can contribute to both the enhancement of tumour angiogenesis and growth as well as apoptosis of neoplastic cells, the search for compounds that inhibit the level/activity of Trx and/or TrxR and thus modulate the course of the neoplastic process is ongoing. It has been shown that many naturally occurring polyphenolic compounds inactivate elements of the thioredoxin system. In addition, the effectiveness of Trx is inhibited by imidazole derivatives, while the activity of TrxR is reduced by transition metal ions complexes, dinitrohalobenzene derivatives, Michael acceptors, nitrosourea and ebselen. In addition, research is ongoing to identify new selective Trx/TrxR inhibitors.
- Subjects :
- Antineoplastic Agents chemical synthesis
Benzene Derivatives chemistry
Benzene Derivatives pharmacology
Enzyme Inhibitors chemical synthesis
Gene Expression Regulation, Neoplastic
Homeostasis drug effects
Homeostasis genetics
Humans
Imidazoles chemistry
Imidazoles pharmacology
Isoindoles chemistry
Isoindoles pharmacology
MAP Kinase Kinase Kinase 5 genetics
MAP Kinase Kinase Kinase 5 metabolism
NF-kappa B genetics
NF-kappa B metabolism
Neoplasms enzymology
Neoplasms genetics
Neoplasms pathology
Neovascularization, Pathologic enzymology
Neovascularization, Pathologic genetics
Neovascularization, Pathologic pathology
Nitrosourea Compounds chemistry
Nitrosourea Compounds pharmacology
Organoselenium Compounds chemistry
Organoselenium Compounds pharmacology
Oxidation-Reduction
Signal Transduction
Structure-Activity Relationship
Thioredoxin-Disulfide Reductase antagonists & inhibitors
Thioredoxin-Disulfide Reductase metabolism
Thioredoxins antagonists & inhibitors
Thioredoxins metabolism
Antineoplastic Agents therapeutic use
Enzyme Inhibitors therapeutic use
Neoplasms drug therapy
Neovascularization, Pathologic drug therapy
Thioredoxin-Disulfide Reductase genetics
Thioredoxins genetics
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 36
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 33356659
- Full Text :
- https://doi.org/10.1080/14756366.2020.1867121