Lecture notes
Nuclear Receptor
- Module
- Pharmacology
- Institution
- University Of Sunderland (UoS)
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exam qua :Nuclear Receptor
f
Describe
Key
* features/characteristics of nuclear receptor superfamily
Super
↳ family of intracellular
VA-binding
BI transcription factor selectively bind
small molecule Lipophilic Ligandand transduce their signal into specific in
gene
expression
↳ located intracellularly (in cytosol or nucleus) & translocate to nucleus
upon ligand binding ->
recognize
& bind specific DNA element sequence regulatory region of
in of
target gene >
- control
transcription of target gene
↳ human NR
superfamily consist of 48 members includes receptor for steroid hormones , thyroid hormone,
vitamin A
,
vitamin D , fatty did cholesterol metabolites Oxystest
↳ NR are
=
monomeric protein that share a common structural architecture consisting of 5 main
domains :
· N-terminal (A/B) domain (NTD) -
harbours a
ligand-independent transcriptional
activation function-1 site
·
DNA-binding (C) domain (BD) -
mediates DNA recognition & Receptor binding
motifs each
comprises 2 "Zind
Finger"coordinating
-
containing
a zinc ion
fetrahedrally 4 cysteine residues .
Hinge (D) highly flexible link DBA to LBD
play role in receptor
·
region -
, ,
dimerization
harbours
ligand-binding(E) domain (LBD) ligand-binding site
·
-
a
or
pocket & a
Ligand dependent
-
transcriptional activation function-2 site
C-terminal
· (F) domain That modulates co-activator $
co-repressor binding
↳ harbours motifs with nuclear localisation signals
& binding sites for accessory heat
shock & other proteins.
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