Term
| Where is the AF-1 region of the NR? |
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Definition
| Near the N-terminal in the A/B region |
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Term
|
Definition
| Activating Factor-1: ligand-independent transactivation |
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Term
| Are Type-1 receptors steroid or non-steroid? |
|
Definition
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|
Term
| Are type-II receptors steroid or non-steroid? |
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Definition
|
|
Term
| Where are type I receptors located? |
|
Definition
|
|
Term
| where are type II receptors located? |
|
Definition
|
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Term
| What are type II receptors bound to most of the time? |
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Definition
|
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Term
| Type I receptors bind as heterodimers or homodimers to DNA? |
|
Definition
|
|
Term
| Type II receptors bind as heterodimers or homodimers to DNA? |
|
Definition
|
|
Term
| Describe Ligand activation of NR |
|
Definition
1) ligand binding repositions which exposes a hydrophobic surface of NR
2) Co-activators can now bind and form the pre-initiation complex |
|
|
Term
| How are type II nuclear receptors found in cell i.e. are they active/inactive/inhibiting |
|
Definition
| inactive and/or actively inhibiting |
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Term
| What happens when ligand binds a actively repressing type II nuclear receptor? |
|
Definition
1) Ligand binding causes the release of co-repressors (HDAC) which opens up the chromatin structure
2) co-activators are recruited to help in promoter exposure (HATs: acetylates Lys residue of Histone's N-terminal tails)
3) TRAP binds to complex which forms link with mediator complex and initiates transcription. |
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Term
| In actively supressing type II NR's, what co-repressors are bound to unliganded NR? What do they do? |
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Definition
| 1) HDAC's (Histone De-acetylases)form non-premissive structure for transcriptions |
|
|
Term
| how many nucleotides are in between the DR of Vitamin D receptors half-site recognition? |
|
Definition
|
|
Term
| how many nucleotides are in between the DR of Thyroid Receptor-Beta half-site recognition? |
|
Definition
|
|
Term
| how many nucleotides are in between the DR of RAR half-sites recognition? |
|
Definition
|
|
Term
| What is the half-site sequence for estrogen? |
|
Definition
|
|
Term
| What is the half-site for all the other type I receptors besides estrogen? |
|
Definition
|
|
Term
| What is the half-site configuration (IR, DR, ER) for type-I NR? |
|
Definition
|
|
Term
| What is the halfsite configuration (ER,IR, DR) for type-II NR? |
|
Definition
|
|
Term
| What does Tamoxifen do? What is it? |
|
Definition
| It is a SERM, ER antagonist in breast tissue, ER agonist in bone and uterine tissue |
|
|
Term
| What does Raloxifin do? What is it? |
|
Definition
| It is a SERM, ER antagonist is breast tissue and bone, but not in uterine |
|
|
Term
| What area of the Nuclear receptors do co-activators bind? (AF-1 or AF-2) |
|
Definition
|
|
Term
|
Definition
HATs
Chromatin modifying machines
TRAP/DRIP |
|
|
Term
|
Definition
| acytylates the lys residue to open up nucleosome structure |
|
|
Term
| How to Chromatin Modifying Machines work? |
|
Definition
| Contain intrinsic ATPase activity, and the complex perturbs core histone structure |
|
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Term
|
Definition
|
|
Term
| what does NCoR stand for? |
|
Definition
|
|
Term
| What does SMRT stand for? |
|
Definition
| Silencing Mediator for Retinoid and thyroid hormone receptor |
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