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| Receptors on cell surface, often transmembrane proteins that activate intracellular signaling proteins in response to binding |
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| Protein found inside the cell that respond to the presence of hormones or other molecules and effect the expression genes; ofton developmental, homeostatic and metabolic |
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Regulate expression of genes neededfor dev of repro organs and second sex traits and reproduction
ex. Estrogen, progesterone and androgen receptors |
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| Adrenal steroid receptors |
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Definition
| regulate genes for glucose, fat and protein metabolism along with immuno-suppression (glucocorticoid) and for salt balance (aldosterone) |
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Regulate gene expression for calcium metabolism, important to bone development and homeostasis
- Vitamin D is derived from Cholesterol |
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Regulates genes that set metabolic rate of all tissues, important in growth and development of many tissues (including brain)
- Thyroxine derived from tyrosine |
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Regulate many aspects of dev
- RA is derived from Vitamin A and has Cis and Trans forms
- RAR refers to trans RA
- RXR refers to cis RA |
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| Peroxisome proliferator-activated receptors, regulate lipid metab, glucose homeostasis and adipocyte differentiation |
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act as cholesterol sensors and activate genes that govern cholesterol catabolism and elimination
- Oxysterols |
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Bile Acid sensor and activate genes necessary to regulate bile acid levels
- Bile Acods |
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| Nuclear Receptors bind to... |
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Definition
| Response elements often in the promoter |
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| Derived from steroids, form homodimers, found in cytoplasm complexed with HSPs, binding of hormone triggers conformation changes causing dissociation from HSP, formation of homodimer, and entrance to nucleus |
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| Examples of Type 1 Receptors |
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Definition
| Progesterone, Extrogen, Androgen/T, Glucocorticoid and Mineralcorticoid receptors |
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| Examples of Type II Receptors |
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Definition
| Vitamin D, Thyroid Hormone, RA, Peroxisome Proliferator activated receptors, Liver X, Farnesoid X |
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| Mostly heterodimers with RXR (cis) except RXR whch functions with itself as homodimer. Already in the nucleus and often already bound to resp element of target gene and represses transcription by recruiting co-repressors. Binding of ligand causes release of co-rep + HDAC and association of co-activators + HATs leading to transcription of target gene. |
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Must have its specific hormone to function
ex. RXR-TR/VDR |
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Response to one element requires that the other receptor be bound too.
ex. RXR-RAR only responds to cisRA if alltrans RA is also bound |
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Either ligand can activate and both often are synergistic when bound together.
Ex RXR-PPAR/LXR/FXR |
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| The amino terminal domain... |
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Definition
| functions in transcriptional activation |
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Definition
| functions (i) in binding specific DNA sequences and (ii) contributes to receptor dimerization |
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| The carboxy terminal domain |
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Definition
| has 3 functions; ligand binding, receptor dimerization, and transcriptional activation, some receptors have an additional activation domain at the very carboxy terminus |
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| Response elements are contacted by |
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Definition
| specific helices in the DNA binding domain |
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| Recognizes specific response elements in promoter |
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| Functions in dimerization of steroid hormone receptors and contributes to the recognition of spacing between half sites |
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| Portion of DNA resp element that binds to one monomer of the receptor |
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Definition
| Complex of receptor and ligand trigger expression and production of proteins |
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| Delayed Secondary Response |
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Definition
| Primary response protein shut off primary response gene then trigger secondary response gene and production of secondary response proteins |
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Definition
| Design driven by getting more and more detailed information of structure, especially by modifying co-activator sensitivity to allow for target specificity |
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| Estrogen and Test Receptor Disease |
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Definition
| Testicular Fem Syndrome, genetic male but doesnt respond to T because of faulty receptor at either ligand bidning or DNA binding |
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