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Glutathione reductase regenerates the cell's main antioxidant; the nitrosourea carmustine inhibits it as a side action to its DNA cross-linking, which adds to the drug's toxicity as well as its effect.
Glutathione reductase converts oxidised glutathione back to its reduced form, maintaining the cell's largest pool of antioxidant. Carmustine (BCNU), the nitrosourea used in glioma and in high-dose conditioning for lymphoma, carbamoylates the enzyme and inactivates it, so cells treated with the drug face oxidative stress as well as DNA cross-links; the effect is thought to contribute to carmustine's lung toxicity. Because tumours with high glutathione levels resist alkylating agents and platinum drugs, the glutathione system as a whole is a target for chemosensitisation.
In plain words · Glutathione reductase regenerates the cell's main antioxidant; the nitrosourea carmustine inhibits it as a side action to its DNA cross-linking, which adds to the drug's toxicity as well as its effect.
Glutathione reductase regenerates the cell's main antioxidant; the nitrosourea carmustine inhibits it as a side action to its DNA cross-linking, which adds to the drug's toxicity as well as its effect.
A dimeric flavoenzyme using NADPH to reduce glutathione disulphide; part of the pentose phosphate and antioxidant network in every cell.
No product in this corpus aims at Glutathione reductase yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
Broadly expressed or essential: HPA finds the RNA at low tissue specificity; the 1 medicine aimed at it (Carmustine) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA GSR: RNA low tissue specificity; high antibody staining in 2 normal tissues; highest cancer staining carcinoid (2 of 4 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Brain and spinal cord tumours (all types), Lymphoma); Open Targets associates it with 4 specific cancer types at or above 0.5 (glioblastoma, plasma cell myeloma, Hodgkins lymphoma, non-Hodgkin lymphoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas GSR tissue; Open Targets ENSG00000104687 associations
First described 1977. Earliest sequence paper UniProt cites for the protein: Krohne-Ehrich et al, Eur. J. Biochem, 1977, "Glutathione reductase from human erythrocytes. Isolation of the enzyme and sequence analysis of the redox-active peptide". Source.
A dimeric flavoenzyme using NADPH to reduce glutathione disulphide; part of the pentose phosphate and antioxidant network in every cell.
RNA: low tissue specificity, detected in all normal tissues.
Medium: Adrenal gland, Appendix, Breast, Bronchus, Cervix, Colon, Duodenum, Endometrium.
Medium only: glioma, head and neck cancer, melanoma, ovarian cancer.
HPA GSR tissue · HPA GSR pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Metastatic cancer | all% | Housekeeping enzyme present in every dividing cell (antioxidant recycling); not a selection marker, which is why these drugs are given by cancer type rather than by test. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"Glutathione reductase" OR ABSTRACT:"Glutathione reductase" OR TITLE:"GSR" OR ABSTRACT:"GSR") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Glutathione reductase, not a curated reading list.
Shares Carmustine, Glioma & glioblastoma.
Shares Carmustine, Glioma & glioblastoma.
Shares Carmustine, Diffuse large B-cell lymphoma.