Glutathione reductase
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
A dimeric flavoenzyme using NADPH to reduce glutathione disulphide; part of the pentose phosphate and antioxidant network in every cell.
- 3 · How drugs use it
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.
External identifiers
Biology
A dimeric flavoenzyme using NADPH to reduce glutathione disulphide; part of the pentose phosphate and antioxidant network in every cell.
- All cells, high in liver and red blood cells
- Gliomas and lymphomas treated with carmustine
Latest papers
topQuery 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.