Intro to Receptors

Question 1

What are the requirements for a protein to be targeted by drugs

Answer 1

pocket into which a small molecule can bind

Question 2

What is the druggable genome

Answer 2

set of genes encoding proteins that can be modulated using experimental small molecule compounds

Question 3

What are the majority of drugs

Answer 3

small molecules that target proteins

Question 4

What is main protein target for drugs

Answer 4

receptors

Question 5

How come receptors are good targets for drugs

Answer 5

recognise specific chemical signals

Question 6

What happens if a drugs concentration is too high

Answer 6

drug binds to other types of proteins

Question 7

What does malfunction or loss of receptors lead to

Answer 7

disease

Question 8

What are the two ways agonists affect receptors

Answer 8

directly or indirectly via transduction mechanisms

Question 9

What is the effect of direct agonist action on a receptor

Answer 9

ion channel opening or closing

Question 10

What are the effects of agonists that affect receptors transduction mechanisms

Answer 10

Enzyme activation/inhibition, Ion channel modulation, DNA transcription

Question 11

Where do antagonists bind on receptors

Answer 11

bind in the same place as the agonist

Question 12

Describe the mechanism of antagonist action on receptors

Answer 12

Stabilise the receptor, prevents activation and signalling

Question 13

What do antagonists block when binding to receptors

Answer 13

endogenous mediator action

Question 14

True or False - receptors cant activate themselves

Answer 14

False

Question 15

How can receptors activate themselves

Answer 15

float around the cell membrane, change into an active shape

Question 16

Name drug targets

Answer 16

receptors, channels, enzymes, transporters, microtubules

Question 17

What is the effect of ion channel blockers

Answer 17

prevent the channel from opening or block the pore

Question 18

What proteins do modulators target

Answer 18

channels

Question 19

What do modulators affect

Answer 19

the gating mechanism of channels

Question 20

What is the effect of modulators affecting gating mechanism

Answer 20

increase or decrease opening probability

Question 21

Where are enzymes normally found

Answer 21

inside cells

Question 22

What are the two types of drugs that target ion channels

Answer 22

blockers, modulators

Question 23

What are the types of drugs that target enzymes

Answer 23

inhibitors, false substrate, prodrug

Question 24

What is the effect of inhibitor drugs on enzymes

Answer 24

inhibit normal reaction and function of enzyme

Question 25

What is the effect of false substrate drugs on enzymes

Answer 25

enzyme makes an abnormal metabolite

Question 26

How do pro drugs work

Answer 26

metabolised by the enzyme to create an active drug

Question 27

What types of drug target transporters

Answer 27

inhibitors, false substrates

Question 28

What do transporters require to function

Answer 28

concentration gradient or energy

Question 29

How do inhibitors affect transporters

Answer 29

bind into transporter pocket and prevent function

Question 30

How do false substrates affect transporters

Answer 30

use transporter to get across the CM, abnormal compounds build up

Question 31

Name two drugs that target microtubules

Answer 31

colchine, paclitaxel

Question 32

What does colchine treat

Answer 32

gout

Question 33

What is gout

Answer 33

inflammatory disease

Question 34

How does colchine treat gout

Answer 34

interferes with inflammatory response and microtubule stability

Question 35

What is paclitaxel

Answer 35

chemo therapeutic drug

Question 36

How does paclitaxel work

Answer 36

stabilises the microtubule, preventing cell division

Question 37

What are the different types of receptor

Answer 37

ligand gated ion channels, GPCRs, kinase linked receptor, nuclear receptors

Question 38

What are the two features of ligand gated ion channel structure

Answer 38

built in ligand binding site, sequence of AAs with pore

Question 39

What are the two structural features of GPCRs

Answer 39

identifiable ligand binding sites, 7 transmembrane spanning domains

Question 40

What do GPCRs require to signal

Answer 40

GTP binding protein

Question 41

Describe the structure of kinase linked receptors

Answer 41

single transmembrane domain, ligand binding site sticks out of the cell

Question 42

What is the signal that binds to kinase linked receptors dependant on

Answer 42

kinase signalling cascade

Question 43

Describe the structure of nuclear receptors

Answer 43

lack transmembrane domains, not anchored to CM, DNA binding domain

Question 44

How do nuclear receptors exert their actions

Answer 44

DNA binding domain

Question 45

What are the four families of ligand gated ion channels

Answer 45

Cys loop, glutamate, P2X, and calcium release

Question 46

How many transmembrane spanning domains do the Cys loop family have

Answer 46

4

Question 47

How many transmembrane domains does the glutamate family have

Answer 47

3

Question 48

What part of the glutamate ion channel is the pore

Answer 48

re-enterant loop

Question 49

What is the ligand for the P2X receptor

Answer 49

ATP

Question 50

Where are calcium release type ion channels found

Answer 50

intracellular membranes, endoplasmic reticulum