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Nuclear Receptors

Creative Animodel has extraordinary experience in drug discovery targeting nuclear receptors. With years of expertise in this field, Creative Animodel is dedicated to providing high-quality services and reliable outcomes of nuclear receptor screening and profiling. We are confident in accelerating your experimental progress and achieving ideal research goals with the most competitive price.

What Are Nuclear Receptors?

Nuclear receptors (NRs) are a large superfamily within cells that are responsible for sensing thyroid hormones, steroid hormone, vitamin D, fatty acid, sterol oxide and certain other molecules. Nuclear receptors have two subtypes, steroid and non-steroid. When a ligand is present, activated nuclear receptors can directly bind to DNA and regulate the expression of specific genes to control the metabolism and development of organisms. Therefore, nuclear receptors can play a role in the pathology of cancer, inflammation, cardiovascular diseases, and reproduction. The unique characteristic of nuclear receptors differing from other receptors is their ability to up-regulate or down-regulate gene expression. This ability makes nuclear receptors involve therapeutic targets of various diseases.

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Figure 1. A mechanism of nuclear receptors regulating gene transcription. Hormone binding to the NR triggers dissociation of heat shock proteins (HSP), dimerization, and translocation to the nucleus, where the dimer binds to a hormone response element (HRE). The nuclear receptor DNA complex then recruits proteins that are responsible for transcription of downstream DNA, which is eventually translated into protein and results in a change in cell function.

Nuclear receptors regulate gene transcription through three basic mechanisms of action: (a) the dimer of the nuclear receptor and its partner transcription factor is activated by lipophilic ligand, then binds to target DNA and regulates transcription (Figure 1); (b) the dimer is activated by the ligands and recruits other transcription factors to regulate transcription; (c) the dimer is activated by surface receptors or CDK (cyclin-dependent kinases) and binds to the target sequence to regulate transcription.

Nuclear Receptor Assays at Creative Animodel

Creative Animodel offers a comprehensive service of cellular and biochemical nuclear receptor assays to profile your compounds. We have carried out a broad range of nuclear receptor binding and profiling assays, such as glucocorticoid receptor, progesterone receptor, androgen receptor, mineralocorticoid receptor, estrogen receptor, and retinoic acid receptor. Our nuclear receptor services include but are not limited to:
• Ligand binding activity
• Nuclear receptor translocation
• Nuclear receptor coregulator interaction
• High throughput screening
• IC50 determination and selectivity

Other than assays mentioned above, Creative Animodel has also developed customized assays for our clients. Our nuclear receptor experts can provide high-quality experimental design to evaluate the efficacy, potency, and selectivity of your compounds.

Creative Animodel provides a wide range of in vitro pharmacology services to help achieve your goals of drug research and development. All our services are conducted under GLP compliant. If you have any special needs in nuclear receptor assays, please don’t hesitate to contact us. We look forward to working together with you in the near future.

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