The RXR heterodimers and orphan receptors

Article Abstract:

The formation of a heterodimer of the retinoid X receptor (RXR) with nonsteroid receptors is necessary for the binding of the nonsteroid receptors to DNA hormone response elements (HREs). The heterodimer formation occurs by the binding of RXR DNA binding domain (DBD) with the ligand binding domain (LBD) of the nonsteroid receptors. The DBDs of the heterodimer then bind to the HREs. Orphan receptors are nuclear receptors which may form heterodimers with RXR or bind to DNA as homodimers or monomers. The fourth type of orphan receptors have no DBD or LBD.

Analysis, Molecular structure, DNA-ligand interactions, DNA binding

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Structural determinants of allosteric ligand activation in RXR heterodimers

Article Abstract:

A network of energetically coupled residues that link the functional surfaces of nuclear receptor ligand binding domains is examined by using a sequence-based method known as statistical coupling analysis (SCA). The results reveal a structural network required for RXR heterodimer allosteric communication and suggest that the specificity of ligand response and permissivity coevolved to enable signal discrimination.

Ligand binding (Biochemistry), Allosteric enzymes

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Identification of ligands for DAF-12 that govern dauer formation and reproduction in C. elegans

Article Abstract:

Two distinct 3-keto-cholestenoic acid metabolites of DAF-9, a cytochrome P450 involved in hormone production, that function as ligands for DAF-12 is identified. The results define the first steroid hormones in nematodes as ligands for an invertebrate orphan nuclear receptor and demonstrate that steroidal regulation of reproduction, from biology to molecular mechanism, is conserved from worms to humans.

United States, Medicinal and Botanical Manufacturing, Medicinals and botanicals, Steroids, Physiological aspects, Inflammation, Caenorhabditis elegans, Steroid hormones

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