PHIL 2015 Lecture Notes - Lecture 59: Farnesoid X Receptor, Pregnane X Receptor, Constitutive Androstane Receptor
Document Summary
Notes for dr. cummins" section of the course. Nuclear receptors are important for fasting, feeding and reproduction. They are involved in pathology (ie breast cancer with the estrogen receptor, and prostate cancer with the androgen receptor) They are important targets for therapeutics: excessively targeted ( overrepresented ): anti-androgen, anti-estrogen blockers for prostate cancer and breast cancer, respectively. Targeted for hormone replacement-ie thyroid hormone replacement with hypothyroidism. Transcription factors can be activated by small molecules at the level of dna. We can span different classes (ie. cholesterol agents, hormones, diabetes therapy etc) Nuclear receptors are also important in adapting to the environment and development. Other: thyroid hormone, vitamin d, retinoic acid (derivative of vitamin a) Already in the nucleus in the absence of ligand. Thyroid receptor, peroxisome proliferator-activated receptors, liver x receptor, estrogen receptor. Receptors are bound to one another to the hormone response element with the corepressor-actively repress transcription. Once the ligand comes in and corepressor is transferred for coactivator.