G-Protein Coupled Receptor Flashcards

1
Q

BASIC STRUCTURE OF GPCRs
How many TM helices make up the GPCR?
What pattern do the connecting loops take?

A

7 alpha helices
alternating intracellular and extracellular loops

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2
Q

Where are the N and C-terminus located

A

N= extracellularly
C= Intracellularly

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3
Q

What are the main functions of the N and C-terminus

A

involved in ligand binding, receptor activation, and their interaction w/ downstream signalling molecules

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4
Q

Where is the G-protein binding site located

A

intracellularly

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5
Q

what are G-proteins crucial for

A

mediators of signal transduction
causing signalling cascades

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6
Q

what conformational change changes the a-subunit

A

GDP -> GTP
G-Protein activation

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7
Q

what purpose does a dissociated G(alpha)- GTP have on proteins

A

regulation of downstream effectors and enzymes

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8
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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9
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

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9
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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10
Q

what is G(alpha)i normal function

A

inhibits the activity of adenylyl cyclase
which converts ATP-> cAMP

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11
Q

when Gai is inactivated, what happens to the signalling pathway and the result of this

A

ATP will be converted into cAMP, with no end or stabilisation
this will lead to disease= whooping couch

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12
Q

physiological effects of inactivation of Gai

A

erosion of respiratory epithilium
large quantities of discharge, muscus containing fluid

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13
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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13
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

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13
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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13
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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13
Q

what receptor activates Phopholipidase C(beta)

A

Gq(alpha)

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13
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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13
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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13
Q

what receptor activates Phopholipidase C(beta)

A

Gq(alpha)

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13
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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13
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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13
Q

steps in the cAMP 2ndary messenger system

A
  1. ligand binding
  2. a-subunit binds to adenylate cyclase in membrane
  3. this activated enzyme catalyses formation of cAMP from ATP
  4. PKA phosphorylates protein (activates)
  5. initiates response in cell
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13
Q

In the Liver, when the Beta2 Adrenoceptor is activated what is the main goal of the receptor and signalling pathways

A

3 stages of alternating energy accumulation
GLYCOGENOLYSIS- breakdown of glycogen into glucose
GLUCONEOGENESIS- synthesis of glucose from non-carb sources (lactate etc)
LIPOLYSIS- breakdown of stored fats into fatty acids, used for energy production when in high demand

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13
Q

Energy mobilisation in the liver due to the Beta2 Adrenoceptor

A

activation in the liver helps to mobilise energy reserves to meet the increased energy demands

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13
Q

role of Glycogenolysis, vasodilation, enhanced muscle contraction, lipolysis and muscle glucose uptake in skeletal muscle when B2 Adrenoceptor is activated

A
  1. increase glucose stores in muscle
  2. increased blood flow to muscles= more oxygen and nutrients
  3. enhanced muscle contraction during physical activity
  4. production of fatty acids for energy production
  5. using glucose as an energy source
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14
Q

where can cGMP be found in the cell

A

receptor bound or ‘free’ in the cytoplasm

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15
Q

what enzyme will remove the cAMP and cGMP molecules/ recycle

A

Phosphodiesterase

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16
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

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17
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
  2. DAG, hydrophobic and will remain in the membrane
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18
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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18
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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18
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

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18
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

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18
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
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18
Q

role of lipid kinases

A

phosphorylate groups of lipids

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19
Q

activation of Phospholipase Cbeta to produce IP3- what will be released

A

Ca2+

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20
Q

Protein Kinase C (PKC) are activated by 2 molecules in 2 domains

A

DAG (in C1) and Ca2+ (in C2)

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21
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

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22
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

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23
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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23
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

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23
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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23
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

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23
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
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23
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

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23
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

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23
Q

help to regulate over-stimulation of GPCRs (2 proteins/ mechanisms)

A

GRK- stops G-protein binding

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24
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

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24
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
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24
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

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24
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

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24
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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25
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

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25
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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25
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

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26
Q

help to regulate over-stimulation of GPCRs (2 proteins/ mechanisms)

A

GRK- stops G-protein binding
Beta-arrestin= degrades/ recycle receptor

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27
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

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27
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

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27
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

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27
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

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27
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
How well did you know this?
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3
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27
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

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27
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

How well did you know this?
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2
3
4
5
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27
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

How well did you know this?
1
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2
3
4
5
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27
Q

help to regulate over-stimulation of GPCRs (2 proteins/ mechanisms)

A

GRK- stops G-protein binding
Beta-arrestin= degrades/ recycle receptor

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28
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

How well did you know this?
1
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2
3
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5
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28
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

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29
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

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29
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

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29
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

29
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

29
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
29
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

30
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

30
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

30
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

30
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

30
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

30
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

30
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
30
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

31
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

31
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

31
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

31
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
31
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

31
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

31
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

31
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

32
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

32
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

32
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

32
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

32
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

32
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

32
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

32
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
33
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

33
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
33
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

33
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

33
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

33
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

33
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

34
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

35
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

35
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

35
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

35
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
35
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

35
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

35
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

36
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

37
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

37
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

37
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
37
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

37
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

37
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

38
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

38
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

39
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

39
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
39
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

39
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

39
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

40
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

40
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

40
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

41
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

41
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

41
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

42
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

42
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

42
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

42
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
42
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

43
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

43
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

43
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

43
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

43
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

43
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

43
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
43
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

44
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

44
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

44
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
44
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

44
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

44
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

44
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

44
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

45
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

45
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

45
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
45
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

45
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

45
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

45
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

46
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

47
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

47
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

47
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

47
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

47
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

47
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

47
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
47
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis

48
Q

whooping cough- what g-protein is affected and the result to that protein

A

It is an inactivated Inhibitory G-Protein

48
Q

Uveal melanoma- and mutations of the Gq a-subunit
what is the result of this mutation?

A

blocking of GTP hydrolysis

48
Q

what receptor activates adenylyl cyclase

A

Gi(alpha)

48
Q

phospholipase Cbeta is an example of what?

A

Hydrophobic lipid in the membrane

48
Q

maintenance of Ca2+ levels is driven by what factor/ pump

A

ATP-driven Ca2+ pumps

48
Q

Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2

A
  1. IP3- water soluble, diffuse through the cytoplasm
49
Q

what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling

A

ACTIVATE or INHIBIT various signalling pathways, enzymes

49
Q

5 processes regulated by Ca2+ signalling

A

synaptic transmission
hormone secretion and synthesis
fertilisation
Muscle contraction
Cytokinesis