F6 Receptors and signalling Flashcards

(52 cards)

1
Q

examples of chemical messengers

A
  • hormones
  • growth factors
  • neurotransmitters
  • paracrine agents
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

simply describe hormones. site of secretion and effects

A
  • secreted from site of synthesis in circulating blood (for long range communication)
  • has short and long term effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

effect of growth factors

A

long term control of cell growth and differentiation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

effect of neurotransmitters

A

fast chemical transmission at neuronal synapses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

effect of paracrine agents

A

local control of cell behaviour in the immediate environment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

explain relationship between adrenaline and noradrenaline

A
  • adrenaline is a hormone and noradrenaline is neurotransmitter
  • they work on the same set of adrenoceptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

common characteristics of receptors

A
  • selective binding site for native hormone / transmitter
  • act as molecular switches (inactive and active states)
  • signal is amplified
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

common types of signal amplification

A
  • second messenger (many molecules produced eg. cAMP)
  • enzyme activity (catalytic: many molecules of substrate converted)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what are the 4 superfamilies of receptors?

A
  • ligand-gated ion channels
  • G protein coupled receptors
  • catalytic receptors
  • nuclear receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

order the 4 types of receptors from fast to slow

A
  • ligand-gated ion channels
  • G protein coupled receptors
  • catalytic receptors
  • nuclear receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what are ligand-gated ion channels primarily responsible for?

A
  • fast synaptic transmission
  • eg. nicotinic receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

describe signal amplification in terms of ligand-gated ion channels

A
  • opening a single ion channel lets thousands of ions flow through
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

describe amplification in terms of G protein coupled receptors

A
  • 1 receptor can activate many G proteins
  • activated ‘effector’ proteins are often enzymes or ion channels
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

describe catalytic receptors and what happens when activated. give an example
- what are they activated by and what do they cause?

A
  • activated by hormone binding
  • causes enzyme activity
  • Tyrosine Kinase receptors for growth factors eg. EGF
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

give an example of a nuclear receptor

A
  • transcription factors
  • eg. steroid hormones (oestrogen receptor (ER))
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

describe the process of transcription factor action

A
  • ligands diffuse across membranes to intracellular receptors
  • when receptors (transcription factors) are activated, they can translocate to the nucleus and bind to DNA to promote transcription
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

why can ligands diffuse across membranes to activate transcription factors?

A

they are lipophilic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

how does the G protein coupled receptor system cause amplification?

A
  • one receptor can activate many G proteins
  • activated ‘effector’ proteins are often enzymes or ion channels
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

why does the G protein coupled receptor system have flexibility?

A

it’s a 3 stage system that offers variety in messengers recognised and cellular responses generated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what do GPCRs look like?

A
  • 7 transmembrane domain helices
  • 7 transmembrane receptors
  • extracellular N terminus
  • intercellular C terminus
  • 3 extracellular loops (ECL), 3 intracellular loops (ICL)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

how do GPCRs exhibit a wide diversity?

A
  • 800 different GPCR proteins
  • 7 transmembrane domain ‘template’ allows many types of binding site (receptors can be adapted for different binding sites)
22
Q

NA action on arterioles in GIT (binding site and result)

A
  • bind to alpha 1 adrenoceptor
  • cause contraction
23
Q

NA action on arterioles in skeletal muscle

A
  • bind to beta 2 adrenoceptor
  • cause relaxation
24
Q

NA action on airway smooth muscle in bronchioles (binding site and result)

A
  • bind to beta 2 adrenoceptor
  • cause relaxation
25
what are the 3 main types of G protein?
Gs, Gi, Gq (a particular receptor will normally activate just one type of G protein)
26
name 2 effectors of G proteins
- adenylyl cyclase - phospholipase C (PL C)
27
what G proteins are adenylyl cyclase regulated by?
- regulated by Gs, Gi - catalyses production of cAMP
28
what can phospholipase C be activated by?
- Gq receptor
29
what subunits are there of G proteins?
G alpha and G beta
30
what do the G alpha subunits bind to?
- binds guanine nucleotides (GDP/GTP) - part of the activation process
31
what is cAMP synthesised by?
adenylyl cyclase
32
what does cAMP trigger and how?
- cellular responses - bind and activate protein kinase A (PK A)
33
after being triggered by cAMP, what does PK A do?
- phosphorylates target proteins to change their function
34
what is a 'kinase'?
phosphorylates proteins to change their function
35
what do Gs-coupled receptors do to adenylyl cyclase? describe the events that this allows for afterwards
- stimulate adenylyl cyclase - adenylyl cyclase can then make cAMP from ATP - cAMP activates PK A which activates target protein
36
what do Gi-coupled receptors do to adenylyl cyclase? describe the events afterwards
- inhibit adenylyl cyclase - cAMP levels and PK A activity decreases
37
what do Gq-coupled receptors do?
- activate a membrane enzyme (phospholipase C / PL C)
38
after activation by Gq-coupled receptors, what does phospholipase C (PL C) do?
- hydrolyses a plasma membrane lipid (PIP2) - 2 intracellular messengers are produced (IP3 and DAG)
39
after hydrolysis of PIP2, what does one of the products, IP3, do?
- activates ion channels and calcium ions influx into the cytoplasm resulting in smooth muscle contraction
40
describe the alpha 1 adrenoceptor in terms of G protein coupling and its effects
- Gq coupled - increases intracellular calcium ions
41
describe the alpha 2 adrenoceptor in terms of G protein coupling and its effects
- Gi coupled - decreases intracellular cAMP
42
describe the beta adrenoceptors in terms of G protein coupling and their effects
- Gs coupled - increases intracellular cAMP
43
effect of noradrenaline on the arterioles in the GIT in terms of the receptor (type of GPCR and result) and response of smooth muscle
- alpha 1 adrenoceptor - Gq coupled - increases intracellular calcium ions - contraction
44
effect of noradrenaline on the arterioles in the skeletal muscle in terms of the receptor and response in smooth muscle
- beta 2 adrenoceptor - Gs coupled - increases intracellular cAMP - relaxation
45
effect of noradrenaline on the airway in terms of the receptor and response in smooth muscle
- beta 2 adrenoceptor - Gs coupled - increases intracellular cAMP - relaxation
46
second messengers of Gq-coupled GPCR
- increased IP3 - DAG - intracellular calcium ions
47
second messengers of Gs-coupled GPCR
- increased cAMP
48
second messengers of Gi-coupled GPCR
decreased cAMP
49
effect of Gq-coupled receptors on neurons, smooth muscle, epithelial cells and endocrine cells
- neurons: increased NT release - smooth muscle: contraction - epithelial cells: increased fluid secretion - endocrine cells: increased hormone secretion
50
effect of Gs-coupled receptors on neurons, smooth muscle, epithelial cells and endocrine cells
- neurons: increased NT release - smooth muscle: relaxation - epithelial cells: increased fluid secretion - endocrine cells: increased hormone secretion
51
effect of Gi-coupled receptors on neurons, smooth muscle, epithelial cells and endocrine cells
- neurons: decreased NT release - smooth muscle: contraction - epithelial cells: decreased fluid secretion - secretory cells: decreased hormone secretion
52
what are the 4 main receptor superfamilies?
- ligand-gated ion channels - GPCRs - catalytic receptors - nuclear receptors