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

Intro to Receptors Flashcards

1
Q

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

A

pocket into which a small molecule can bind

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2
Q

What is the druggable genome

A

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

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3
Q

What are the majority of drugs

A

small molecules that target proteins

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4
Q

What is main protein target for drugs

A

receptors

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5
Q

How come receptors are good targets for drugs

A

recognise specific chemical signals

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6
Q

What happens if a drugs concentration is too high

A

drug binds to other types of proteins

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7
Q

What does malfunction or loss of receptors lead to

A

disease

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8
Q

What are the two ways agonists affect receptors

A

directly or indirectly via transduction mechanisms

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9
Q

What is the effect of direct agonist action on a receptor

A

ion channel opening or closing

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10
Q

What are the effects of agonists that affect receptors transduction mechanisms

A

Enzyme activation/inhibition, Ion channel modulation, DNA transcription

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11
Q

Where do antagonists bind on receptors

A

bind in the same place as the agonist

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12
Q

Describe the mechanism of antagonist action on receptors

A

Stabilise the receptor, prevents activation and signalling

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13
Q

What do antagonists block when binding to receptors

A

endogenous mediator action

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14
Q

True or False - receptors cant activate themselves

A

False

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15
Q

How can receptors activate themselves

A

float around the cell membrane, change into an active shape

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16
Q

Name drug targets

A

receptors, channels, enzymes, transporters, microtubules

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17
Q

What is the effect of ion channel blockers

A

prevent the channel from opening or block the pore

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18
Q

What proteins do modulators target

A

channels

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19
Q

What do modulators affect

A

the gating mechanism of channels

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20
Q

What is the effect of modulators affecting gating mechanism

A

increase or decrease opening probability

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21
Q

Where are enzymes normally found

A

inside cells

22
Q

What are the two types of drugs that target ion channels

A

blockers, modulators

23
Q

What are the types of drugs that target enzymes

A

inhibitors, false substrate, prodrug

24
Q

What is the effect of inhibitor drugs on enzymes

A

inhibit normal reaction and function of enzyme

25
Q

What is the effect of false substrate drugs on enzymes

A

enzyme makes an abnormal metabolite

26
Q

How do pro drugs work

A

metabolised by the enzyme to create an active drug

27
Q

What types of drug target transporters

A

inhibitors, false substrates

28
Q

What do transporters require to function

A

concentration gradient or energy

29
Q

How do inhibitors affect transporters

A

bind into transporter pocket and prevent function

30
Q

How do false substrates affect transporters

A

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

31
Q

Name two drugs that target microtubules

A

colchine, paclitaxel

32
Q

What does colchine treat

A

gout

33
Q

What is gout

A

inflammatory disease

34
Q

How does colchine treat gout

A

interferes with inflammatory response and microtubule stability

35
Q

What is paclitaxel

A

chemo therapeutic drug

36
Q

How does paclitaxel work

A

stabilises the microtubule, preventing cell division

37
Q

What are the different types of receptor

A

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

38
Q

What are the two features of ligand gated ion channel structure

A

built in ligand binding site, sequence of AAs with pore

39
Q

What are the two structural features of GPCRs

A

identifiable ligand binding sites, 7 transmembrane spanning domains

40
Q

What do GPCRs require to signal

A

GTP binding protein

41
Q

Describe the structure of kinase linked receptors

A

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

42
Q

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

A

kinase signalling cascade

43
Q

Describe the structure of nuclear receptors

A

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

44
Q

How do nuclear receptors exert their actions

A

DNA binding domain

45
Q

What are the four families of ligand gated ion channels

A

Cys loop, glutamate, P2X, and calcium release

46
Q

How many transmembrane spanning domains do the Cys loop family have

A

4

47
Q

How many transmembrane domains does the glutamate family have

A

3

48
Q

What part of the glutamate ion channel is the pore

A

re-enterant loop

49
Q

What is the ligand for the P2X receptor

A

ATP

50
Q

Where are calcium release type ion channels found

A

intracellular membranes, endoplasmic reticulum

BMS 242 Core Physiology and Pharmacology (13 decks)

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