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

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.

Citation

M Becker-André, I Wiesenberg, N Schaeren-Wiemers, E André, M Missbach, J H Saurat, C Carlberg. Pineal gland hormone melatonin binds and activates an orphan of the nuclear receptor superfamily. The Journal of biological chemistry. 1994 Nov 18;269(46):28531-4

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PMID: 7961794

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