Finding New Targets Flashcards
(7 cards)
Druggable classes
- TTM GPCRs
- proteases
- kinases
- nuclear receptors
- ion channels
- integrins
Good drug targets
- functional rather than structural proteins
- can be modulated
- can set up an assay
- chemical tractibility
- strong rationale for disease link
- ability to separate desirable vs undesirable effects
- demonstrate efficacy in clinical setting
- market for drug
Susceptibility genes
Natural polymorphisms can increase the likelihood of certain diseases
Act in combination with other susceptibility genes
Animal models (e.g. ADHD)
Animal models used to test new targets; must recapitulate aspects of human disease
e.g. ADHD
- spontaneously hypertensive rat as a model
- main symptoms of impaired attention and hyperactivity
- human ritalin treatment also works in SHR
Known drugs
Known drugs can act as guides for new drugs
e.g. original antipsychotics have motor side effects so new antipsychotics have reduced D2 affinity but increased activity at other sites (e.g. 5-HTRs) to combat other symptoms
Disease pathway targeting in asthma
- avoid allergen exposure
- vasodilators
- steroids
- chemotaxic receptor blockers
- novel anti-inflammatoriees
Methods of finding new targets
- disease genetics + susceptibility genes
- disease pathways
- druggable protein classes
- animal models
- known drugs