drug targets Flashcards
(21 cards)
philosophies
empircal
rational
empirical drug discovery
screen —–> biological activity ——> optimised schedule
what is in optimised schedule
phase 1 - dose schedule
phase 2- activity
phase 3 - compare w standard
Target identification
area of interest in term of drug interaction
drug target and mechanism :
enzyme
reversible/irreversbile
drug target and mechanism :
receptor
agonists/antagonist
drug target and mechanism :
viral surface protein
block entry to cell
drug target and mechanism :
ion channel
block/open channel
drug target and mechanism :
transporter
block/promote transporter
drug target and mechanism :
nucleic acid
inhibit function/prevent gene expression
what is target validation
identify and asses whether molecular target merit drug development
tissue expression low
target protein expressed or active in desired organ
target expression medium
target mRNA expression altered in desired diseases tissue
target expression high
target protein expression is altered in desired disease
genetics low
small underpowdered
medium
replicated polygenic association with modest effects
genetics high
monogenic association
low clinical expierence
efficacy observed in small trial
medium clinical experience
efficacy observed with at least ligand with different mode of target modulation
high clinical expierence
at least ligand with analogous mode of action has approvable efficacy
pharmacology
low
medium
high
