Intro to Receptors Flashcards Preview

BMS 242 Core Physiology and Pharmacology > Intro to Receptors > Flashcards

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

How do false substrates affect transporters

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

31

Name two drugs that target microtubules

colchine, paclitaxel

32

What does colchine treat

gout

33

What is gout

inflammatory disease

34

How does colchine treat gout

interferes with inflammatory response and microtubule stability

35

What is paclitaxel

chemo therapeutic drug

36

How does paclitaxel work

stabilises the microtubule, preventing cell division

37

What are the different types of receptor

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

38

What are the two features of ligand gated ion channel structure

built in ligand binding site, sequence of AAs with pore

39

What are the two structural features of GPCRs

identifiable ligand binding sites, 7 transmembrane spanning domains

40

What do GPCRs require to signal

GTP binding protein

41

Describe the structure of kinase linked receptors

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

42

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

kinase signalling cascade

43

Describe the structure of nuclear receptors

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

44

How do nuclear receptors exert their actions

DNA binding domain

45

What are the four families of ligand gated ion channels

Cys loop, glutamate, P2X, and calcium release

46

How many transmembrane spanning domains do the Cys loop family have

4

47

How many transmembrane domains does the glutamate family have

3

48

What part of the glutamate ion channel is the pore

re-enterant loop

49

What is the ligand for the P2X receptor

ATP

50

Where are calcium release type ion channels found

intracellular membranes, endoplasmic reticulum