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AssigneeN.V. Organon
InventorsChristine J. C. Boersma, Paulus Theodorus Maria Van Der Saag, Sacha Wissink, Bart Van Der Burg
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Interaction of Rel proteins and steroid receptors is known to result in repression of target genes. Here we describe the discovery of a new mechanism in which Rel proteins and steroid receptors act synergistically to activate a regulatory element. This mechanism is shown to influence the expression of the brain-specific 5HT1A receptor wherein the estrogen receptor acts synergistically with the Nuclear Factor kappa B to enhance the activity of the promoter for the 5HT1A receptor gene. In addition, synergistic effects of Rel proteins with the mineralocorticoid receptor were observed, showing that synergism with Rel proteins may be expected for other steroid receptors as well. The synergism between Rel proteins and estrogen receptor or mineralocorticoid receptor provides a tool for the development of compounds that interact with the estrogen or mineralocorticoid receptor in such a way that only the synergistic effect is modulated whereas other effects are left intact. Such compounds would be invaluable for the development of medicaments for the treatment of diseases of the central nervous or cardiovascular system and other disorders in which Rel proteins play a role.
A method for the identification of compounds capable of modulating a synergistic effect of a steroid receptor and a Rel protein on regulatory elements, comprising the steps of:
A cell transfected with a nucleic acid comprising a promoter for the 5-HT1A receptor gene and a reporter gene capable of signaling the activation of the promoter for the 5-HT1A reporter gene, said cell further comprising:
Dependencies are inferred from the claim text.