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BMS242 Cell & Molecular > L9 - GPCRs > Flashcards

L9 - GPCRs Flashcards

1
Q

Which is the largest receptor family

A

GPCRs

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2
Q

Structural features of GPCRs

A

7 transmembrane spanning domains

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3
Q

Alpha helix 3 in GPCRs

A

always orientated towards centre of structure

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4
Q

Function of alpha helix 3 in GPCRs

A

contributes to binding site

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5
Q

What connects TM domains

A

Intracellular and extracellular loops

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6
Q

N terminus location GPCRs

A

Points out of the cell - extracellular

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7
Q

C terminus function in GPCRs

A

regulation of receptor function

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8
Q

What do receptor families share

A

one or more homologous domains

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9
Q

States of GPCRs

A

resting and active

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10
Q

Which regions open up the GPCR

A

TM5 and TM6

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11
Q

TM3 function in GPCR

A

central location, crucial for transduction of ligand binding

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12
Q

What domains does TM3 send the transduction to

A

TM5 and TM6

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13
Q

What else can contribute to ligand binding

A

Extracellular N terminus

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14
Q

PAR receptor

A

GPCR for thrombin

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15
Q

What activates PAR receptors

A

proteinases

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16
Q

PAR receptor function

A

blood clotting and wound healing

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17
Q

Thrombin

A

protease (enzyme)

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18
Q

Thrombin function

A

cleaves amino terminus of receptor

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19
Q

Effect of cleaving amino terminus of PAR receptor

A

activates receptor

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20
Q

What two receptors are involved in blood clotting

A

thrombin receptor and ADP

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21
Q

Blood thinners interfere with which receptors

A

thrombin receptor and ADP

22
Q

Which patients require blood thinners

A

patients at risk of stroke or clotting

23
Q

ADP receptor type

A

purinergic

24
Q

Allosteric modulator

A

molecules that act away from ligand binding site

25
Q

Impact of allosteric modulator

A

may impact receptor function

26
Q

Describe the resting GPCR

A

three inactive components

27
Q

How is the resting GPCR activated

A

ligand binding and exchange of GDP for GTP

28
Q

End result of active GPCR

A

three separate active components

29
Q

inactive alpha subunit Gprotein characteristics

A

alpha subunit has high affinity for GDP

30
Q

GEF

A

guanine exchange factor

31
Q

GEF function

A

causes GDP to fall off and GTP to come on

32
Q

RGS

A

regulators of G protein signalling

33
Q

How is receptor signalling system adapted

A

feedback

34
Q

Olfactory receptors activation

A

transduced through same trimeric G protein

35
Q

What do RGS proteins stimulate

A

GTPase activity

36
Q

What is duration of signalled by activated trimeric G protein regulated by

A

rate of GDP hydrolysis by Ga

37
Q

What do G proteins control production of

A

second messengers, and ion channels

38
Q

What are effectors of trimeric G proteins

A

enzymes

39
Q

What do G proteins effectors (enzymes) control levels of

A

second messengers

40
Q

What is local concentration fo 2nd messengers determined by

A

rate of production, rate of diffusion and rate of removal

41
Q

What regulates cAMP production

A

adenylyl cyclase

42
Q

What removes cAMP

A

phosphodiesterase

43
Q

What does activated adenylyl cyclase catalyse

A

ATP into cAMP

44
Q

How many isoforms of adenylate cyclase are there

A

10

45
Q

What activates adenylate cyclase

A

Gas

46
Q

What inhibits adenylyl cyclase

A

Gai

47
Q

What does B2 adreno-receptor regulate

A

metabolism in liver and skeletal muscle

48
Q

What does stimulation of cAMP and adenylate cyclase activate

A

PKA

49
Q

PKA function in metabolism

A

sets up signalling cascade that phosphorylates enzymes controlling glycogen metabolism

50
Q

What is the effect of a stimulus on cell function determined by

A

receptor and signalling molecules expressed in that cell

BMS242 Cell & Molecular (14 decks)

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