Glutathione peroxidase (EC1.11.1.9, GPx) is an enzyme related with anti-oxidation in mammal bodies.1) The enzyme consists of four sub-units and contains a selenium atom per subunit.2) The selenium atom exists in the enzyme as selenocysteine residue (Sec45*) and it is proposed that the residue forms the active center of the enzyme.3) The selenocysteine residue forms a catalytic triad with two other amino acid residues, Gln79* and Trp153*.3) Based on the knowledge, small organic molecules containing selenium have been designed as a mimic of the enzyme.3) Ebselen (1) is one of such seleno-molecules and possesses GPx like activity.4,5) Therefore, 1 works as an anti-oxidant.6)
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Selenium-containing Antioxidant
No.169(April 2016)
As shown in Table, 1 possesses interesting biological activities including anti-inflammatory activity, immuno-modulation, neuroprotective activity, etc. 1 also inhibits several enzymes such as NADPH oxidase, nitric oxide synthases, and 5- and 15-LOXs.
*The residue numbers are according to the sequence alignment of human enzyme (Human pGSHPx) reported by Ren et al.7)
References
- 1)Selenium: Biochemical role as a component of glutathione peroxidase
- 2)Glutathione peroxidase: A selenoenzyme
- 3)Functional mimics of glutathione peroxidase: Bioinspired synthetic antioxidants
- 4)A novel biologically active seleno-organic compound-I, glutathione peroxidase-like activity in vitro and antioxidant capacity of PZ 51 (Ebselen)
- 5)The early research and development of ebselen
- 6)Ebselen, a glutathione peroxidase mimetic seleno-organic compound, as a multifunctional antioxidant
- 7)The crystal structure of seleno-glutathione peroxidase from human plasma at 2.9 Å resolution
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