Flashcards in Lecture 8: Hormone Receptors Deck (81)
What are the 7 domains of a nuclear hormone receptor?
1. Hormone binding
2. DNA binding
3. Nuclear localization
4. Dimerization/Modulation/Phosphorylation domains
5. Transducing domain
What are the 6 domains of a membrane hormone receptor? Which ones are in the cell and which ones are out?
1. Hormone binding (out)
2. Transmembrane (within)
3. Dimerization (out)
4. Modulation (in)
5. Phosphorylation (in)
6. Transducing domain (in)
What are the 4 ways for a membrane hormone receptor to trigger a second messenger system?
3. Phosphorylation domains
4. Enzymatic activity
What method is used by membrane receptors to induce a conformational change leading to transduction of response/second messenger cascade?
Which is inside the cell: N or C terminus of membrane hormone receptor?
Where is the hormone-binding domain of nuclear hormone receptors? What is particular about it?
At the C-terminal
LARGE: ~250 AAs
What is the function of the nuclear localization domain of the nuclear hormone receptor?
Allows receptor to localize the nucleus of the cell
When does the nuclear hormone receptor enter the nucleus?
Could have always been there or upon binding to the hormone in the cytosol
What is the transducing domain of the nuclear hormone receptor?
Could be considered the entire hormone receptor
What is an agonist?
Molecule that binds to the hormone receptor and brings about a response
What is an antagonist?
Molecule that binds to the hormone receptor and inhibits the agonist responses
What is the role of the transducing domain of the membrane hormone receptor? What part of the receptor is it?
To induce second messengers
Cytoplasmic side of the receptor
What is the role of the transducing domain of the nuclear hormone receptor?
Which bind better: agonists or antigonists?
How can one determine if the binding domain of a hormone receptor binds the hormone reversibly?
Binding assay: scatchard plots
Which type of receptors can be glycosylated?
Which type of membrane receptors can have enzymatic activity??
What is an example of a partial/weak antagonist?
Ru486: works to inhibit progesterone receptor but partially inhibits the glucocorticoid receptor
What can an antagonist's properties depend on? Example?
The tissue it is in!
Eg: tamoxifen inhibits estradiol receptors well in breasts and poorly in bone
What does hGR stand for?
What does hMR stand for?
What does hAR stand for?
What does hPR stand for?
What does hERalpha and B stand for?
Alpha and beta estrogen receptors
What does hTR stand for?
What are the 2 main types of hTRs?
Alpha 1 and beta 1
What does hRAR stand for?
Retinoic acid receptor
What are the 3 types of hRARs?
Alpha, beta, gamma
What does hRXR stand for?
Retinoic acid X receptor