1: Proteins as drug targets Flashcards
which 4 drugs dont target proteins
antacids
osmotic diuretics
DNA modifying drugs
Membrane lipid targeting drugs
what is the main extracellular target protein
enzymes
main intracellular target proteins
nuclear hormone receptors
and
enzymes
what is binding domain
usually a acavity lined with amino acids that make up the protein
small part of the protein, so must ensure the binding energy that comes from the drug binding to it, has a conformational effect on the receptor
what are families and superfamilies based on
AA sequence similarity
what superfamily is the Estrogen like family part of
Nuclear hormone receptor superfamily
name the 4 subunits of estrogen receptors
androgen receptors
progesterone receptors
glucocorticoid receptors
mineralcorticoid receptors
general mechanism of NHR superfamily
bind lipohillic agonist
then regulate transcripstion of DNA
which causes changes in protein mexpression
what is an advantage of having multiple proteins that are tissue specific
the individual types ar especialised for each tissue
and if a disorder affects one protein, there’s only some functions that are affected instead of everything going to poo
also they can compensate for each other
where are corticosteroids produced
adrenal cortex
what are the natural steroids that bind to glucocorticoid (and mineralcorticoid undesireably)
hydrocortisone
corticosterone
what are 4 key receptors
Ligand-gated ion channel
Receptor tyrosine kinase
G protein-coupled receptors
nuclear hormone receptor
example of receptor tyronsine kinase
insulin receptor
what do RTKs bind
big molecules
peptide hormones
growth factors
cytokines
how do RTKs operate
recognise specfic AAs in target proteins
and phosphroyalte tyrosine residues in these target protein