Old and new inhibitors of quinone reductase 2.

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Ferry G, Hecht S, Berger S, Moulharat N, Coge F, Guillaumet G, Leclerc V, Yous S, Delagrange P, Boutin JA

Old and new inhibitors of quinone reductase 2.

Chem Biol Interact. 2010 Jul 30;186(2):103-9. doi: 10.1016/j.cbi.2010.04.006. Epub 2010 May 4.

PubMed ID

20399199 [ View in PubMed

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Abstract

Quinone reductase 2 is a cytosolic enzyme which catalyses the reduction of quinones, such as menadione and coenzymes Q. Despite a relatively close sequence-based resemblance to NAD(P)H:quinone oxidoreductase 1 (QR1), it has many different features. QR2 is the third melatonin binding site (MT3). It is inhibited in the micromolar range by melatonin, and does not accept conventional phosphorylated nicotinamides as hydride donors. QR2 has a powerful capacity to activate quinones leading to unexpected toxicity situations. In the present paper, we report the characterization of three QR2 modulators: melatonin, resveratrol and S29434. The latter compound inhibits QR2 activity with an IC(50) in the low nanomolar range. The potency of the modulators ranged as follows, from the least to the most potent: melatonin

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Resveratrol	Melatonin receptor type 1A	Protein	Humans	Unknown	Not Available	Details
Resveratrol	Melatonin receptor type 1B	Protein	Humans	Unknown	Not Available	Details