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Nuclear Receptor

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  • April 5, 2024
  • 5
  • 2023/2024
  • Class notes
  • Boachie-ansah
  • All classes
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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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