Flashcards in Intro to Receptors Deck (50)
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1
What are the requirements for a protein to be targeted by drugs
pocket into which a small molecule can bind
2
What is the druggable genome
set of genes encoding proteins that can be modulated using experimental small molecule compounds
3
What are the majority of drugs
small molecules that target proteins
4
What is main protein target for drugs
receptors
5
How come receptors are good targets for drugs
recognise specific chemical signals
6
What happens if a drugs concentration is too high
drug binds to other types of proteins
7
What does malfunction or loss of receptors lead to
disease
8
What are the two ways agonists affect receptors
directly or indirectly via transduction mechanisms
9
What is the effect of direct agonist action on a receptor
ion channel opening or closing
10
What are the effects of agonists that affect receptors transduction mechanisms
Enzyme activation/inhibition, Ion channel modulation, DNA transcription
11
Where do antagonists bind on receptors
bind in the same place as the agonist
12
Describe the mechanism of antagonist action on receptors
Stabilise the receptor, prevents activation and signalling
13
What do antagonists block when binding to receptors
endogenous mediator action
14
True or False - receptors cant activate themselves
False
15
How can receptors activate themselves
float around the cell membrane, change into an active shape
16
Name drug targets
receptors, channels, enzymes, transporters, microtubules
17
What is the effect of ion channel blockers
prevent the channel from opening or block the pore
18
What proteins do modulators target
channels
19
What do modulators affect
the gating mechanism of channels
20
What is the effect of modulators affecting gating mechanism
increase or decrease opening probability
21
Where are enzymes normally found
inside cells
22
What are the two types of drugs that target ion channels
blockers, modulators
23
What are the types of drugs that target enzymes
inhibitors, false substrate, prodrug
24
What is the effect of inhibitor drugs on enzymes
inhibit normal reaction and function of enzyme
25
What is the effect of false substrate drugs on enzymes
enzyme makes an abnormal metabolite
26
How do pro drugs work
metabolised by the enzyme to create an active drug
27
What types of drug target transporters
inhibitors, false substrates
28
What do transporters require to function
concentration gradient or energy
29
How do inhibitors affect transporters
bind into transporter pocket and prevent function
30
