Pineal gland hormone melatonin binds and activates an orphan of the nuclear receptor superfamily - PubMed (original) (raw)

. 1994 Nov 18;269(46):28531-4.

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• PMID: 7961794

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Pineal gland hormone melatonin binds and activates an orphan of the nuclear receptor superfamily

M Becker-André et al. J Biol Chem. 1994.

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• J Biol Chem 1997 Jun 27;272(26):16707

Abstract

Nuclear orpan receptors are members of the superfamily of structurally related, ligand-inducible transcription factors for which no ligand has yet been identified. Over the past few years many nuclear orphan receptors have been cloned, but only for the retinoid X receptor (RXR) has a natural ligand (9-cis-retinoic acid) been found. Here we report the identification of melatonin as a ligand for the recently cloned orphan receptor retinoid Z receptor beta (RZR beta). We found RZR beta expression in the rat brain nearly coincident with binding sites for the pineal gland hormone melatonin (5-methoxy-N-acetyltryptamine). We show here binding and activation of RZR beta by melatonin with Kd and EC50 values in the low nanomolar range. A nuclear signaling pathway for melatonin may contribute to some of the diverse and profound effects of this hormone, for example, in the context of circadian rhythmicity.

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