receptor families Flashcards
classification is done in
order of potency
adrenergic agonists
distict potency what is the order for alpha receptors and the response
constricting response
a>nor>isoprenaline
adrenergic agonists
distict potency what is the order for beta receptors and the response
dilating response
iso>adr>nor
response curve
the lower the potency of blocking needed the
less antagonist needed
different potency of adrenaline in the receptor we can get
sub classes
classification through gene cloning
how is it done
4 points
identify and sequence cDNA for the receptor
predict AA sequence for receptor
repeat for all receptor subtypes compare AA to give molecular classification
which identifies distinct subtypes by pharmacological classification
molecular method that opens up diversity in receptor families
how do we use cDNA to find family types
4 points
find code for receptor using cDNA
look for sequence via oligonucleotide screening
compare sequence to find similar ones
we can change the similarities so that not so similar ones can be found
expressed sequence tags ESTs and data mining
what do they do
cDNA gets a EST attached
this sequence is complementary to identical but also homologous receptor subtypes
gene sequencing using a computer
it will artificially splice and build a diversity of receptor families from the sequence
building post genomic receptor families
G proteins predicted by cDNA what do they contain
7 membrane domains
coupled to g protein
5 families from superfamily of g protein
which are organised with structural similarities
receptor types
g protein
tyrosine kinase
ion channel
steroid
G coupled receptors
primary
secondary
tertiary
- multifaced family made up of related subfamilies
- all receptors predicted to be 7 MD
- rhodopsin supports 7 MD model
ligand gated ion channel
subunits facts about them
4 points
number of related genes encoding subunits
for each receptor type which come together in a mix and match
each subunit exhibits a common transmembrane topology
tertiary structure supported by 3D arrangement of AA sequence
ligand gated ion channels
subunits what are they
5 subunits
can be homo-oligomer
hetero-oligomer
ions with water bound around what can channels do to remove the water
the water ligands are substituted for protein ligands
this also helps to restrict larger ions from entering the cell