Term
Ligand activated transcription factors
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Definition
a.can’t bind DNA in the absence of bound ligand or
b.can’t activate transcription in the absence of bound ligand
c.Some steroid hormone receptors become repressors when ligand binds (example: some thyroid hormone receptors)
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Term
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Definition
pass through cell membranes to meet their receptors inside the cell
•Hydrophobic (move through blood on carrier proteins)
• pass across the cell membrane
•directly regulates the receptors.
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Term
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Definition
1) induces conformational change
-kicks off inhibitiory proteins
-causes receptor to dimerize
[image] |
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Term
Retinoic Androgen Receptor |
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Definition
•RAR and RXR
Ligands (derivatives of vitamin A)
•All-trans retinoic acid
•9-cis retinoic acid
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Jobs
•Retinoids play an important role in development,
differentiation, and homeostasis
-major role in normal blood development |
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Term
Unliganded retinoid receptors
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Definition
•bind retinoic acid response elements (RARE; Cis elements on DNA)
•recruit histone deacetylase machinery (HDAC)
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Term
Ligand Bound retinoid Receptors
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Definition
•Retinoid binding leads to release of HDAC
•recruits of transcriptional co-activators
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Term
Treatment strategy of APL |
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Definition
-High-dose all-trans Retinoic Acid (RA)
Mechanism: High doses of RA release histone deacetylase activity
from PML–RAR
-trigger myeloid maturation (undergo complete remission)
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Term
1. What type of androgen receptor mutations, cause androgen insensitivity syndromes?
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Definition
- Mutations that interfere with direct contact of Ligand
- Mutations that abolish binding to general transcription factors or chromatin remodeling factors
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Term
What are the mechanisms by which gene regulatory proteins can be regulated?
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Definition
- Protein synthesis
- Ligand Binding
- Covalent modification
- Addition of second subunit
- Unmasking
- Stimulation of nuclear entry
- Release from membrane
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