42 results about "Steroids Receptors" patented technology

The present invention includes novel methods and compositions for inhibiting or reducing steroid-dependent gene activation including the administration of at least two compounds that act different steps within a steroid receptor gene activation pathway. Preferred methods may include administering a first compound able to induce degradation of a steroid receptor and administering a second compound able to inhibit gene activation at a different step of the steroid receptor pathway. Steroid-dependent gene activation may be reduced or inhibited, modulated or controlled greater when the at least two of the compounds are administered in combination or together.

The present invention provides in vitro test kits, assays and methods useful for screening a test sample for the presence of a ligand which is characterized by its ability to form a complex with a steroid hormone receptor and elicit a genomic response when in a cell. Advantageously, the activity-based assays which form the basis of the test kits and methods described herein, are particularly useful in detecting the presence of a ligand of unknown structure, for example, a designer drug used by equine, canine and human athletes in sports doping. Different assay prototypes are disclosed in whichactivation of the hormone receptor by a ligand binding interaction may be detected, for example, though activation of a reporter molecule. In certain examples, the present invention provides test kits, assays and methods involving aptame: fluorophore reporter constructs for detection of a ligand from (e.g.) a sample taken trackside from an athlete.

The present invention relates to the detection of ligands that bind to and activate a steroid hormone receptor. In particular, the present invention provides test kits and assays for selectively identifying steroid hormone receptor ligands from a test sample. Importantly, the test kits and assays described herein are cell-free and enzyme-free and do not require the production of expensive nuclear extracts to enable the performance of the test kits and assays. In contrast, the test kits and assays described herein employ a reporter construct that includes a hormone response element that, when bound by a ligand-activated steroid hormone receptor, changes physical, mechanical, optical, photochemical, or electrochemical properties of the reporter construct. Thus, the presence of a target ligand in a sample under study can be determined using measured changes in physical, mechanical, optical, photochemical, or electrochemical properties (e.g., fluorescent readings) of the reporter construct.

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.

The present invention is concerned with the detection of ligands which bind to and activate steroid hormone receptors. Specifically, the present invention provides test kits and assay methods for the selective identification of steroid hormone receptor ligands from a test sample. Importantly, the test kits and assay methods described herein are cell-free and enzyme-free, and do not require expensive-to-manufacture nuclear extracts for their performance. Instead, the test kits and assay methods described herein employ reporter constructs comprising hormone response elements, which when bound by a ligand-activated steroid hormone receptor force a change in a physical property, a mechanical property, an optical property, a photochemical property or an electrochemical property of the reporter construct. Accordingly, a measured change in a physical, mechanical, optical, photochemical or electrochemical property of the reporter construct (e.g. fluorescence read-out) may be used to determine the presence of a target ligand in a sample under investigation.