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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
In the Liver, when the Beta2 Adrenoceptor is activated what is the main goal of the receptor and signalling pathways
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
13
Energy mobilisation in the liver due to the Beta2 Adrenoceptor
activation in the liver helps to mobilise energy reserves to meet the increased energy demands
13
role of Glycogenolysis, vasodilation, enhanced muscle contraction, lipolysis and muscle glucose uptake in skeletal muscle when B2 Adrenoceptor is activated
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
14
where can cGMP be found in the cell
receptor bound or 'free' in the cytoplasm
15
what enzyme will remove the cAMP and cGMP molecules/ recycle
Phosphodiesterase
16
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
17
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm 2. DAG, hydrophobic and will remain in the membrane
18
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
18
what receptor activates adenylyl cyclase
Gi(alpha)
18
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
18
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
18
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
18
role of lipid kinases
phosphorylate groups of lipids
19
activation of Phospholipase Cbeta to produce IP3- what will be released
Ca2+
20
Protein Kinase C (PKC) are activated by 2 molecules in 2 domains
DAG (in C1) and Ca2+ (in C2)
21
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
22
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
23
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
23
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
23
what receptor activates adenylyl cyclase
Gi(alpha)
23
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
23
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
23
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
23
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
23
help to regulate over-stimulation of GPCRs (2 proteins/ mechanisms)
GRK- stops G-protein binding
24
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
24
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
24
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
24
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
24
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
25
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
25
what receptor activates adenylyl cyclase
Gi(alpha)
25
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
26
help to regulate over-stimulation of GPCRs (2 proteins/ mechanisms)
GRK- stops G-protein binding Beta-arrestin= degrades/ recycle receptor
27
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
27
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
27
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
27
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
27
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
27
what receptor activates adenylyl cyclase
Gi(alpha)
27
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
27
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
27
help to regulate over-stimulation of GPCRs (2 proteins/ mechanisms)
GRK- stops G-protein binding Beta-arrestin= degrades/ recycle receptor
28
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
28
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
29
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
29
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
29
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
29
what receptor activates adenylyl cyclase
Gi(alpha)
29
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
29
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
30
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
30
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
30
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
30
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
30
what receptor activates adenylyl cyclase
Gi(alpha)
30
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
30
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
30
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
31
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
31
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
31
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
31
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
31
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
31
what receptor activates adenylyl cyclase
Gi(alpha)
31
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
31
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
32
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
32
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
32
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
32
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
32
what receptor activates adenylyl cyclase
Gi(alpha)
32
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
32
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
32
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
33
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
33
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
33
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
33
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
33
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
33
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
33
what receptor activates adenylyl cyclase
Gi(alpha)
34
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
35
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
35
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
35
what receptor activates adenylyl cyclase
Gi(alpha)
35
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
35
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
35
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
35
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
36
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
37
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
37
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
37
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
37
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
37
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
37
what receptor activates adenylyl cyclase
Gi(alpha)
38
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
38
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
39
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
39
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
39
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
39
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
39
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
40
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
40
what receptor activates adenylyl cyclase
Gi(alpha)
40
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
41
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
41
what receptor activates adenylyl cyclase
Gi(alpha)
41
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
42
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
42
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
42
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
42
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
42
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
43
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
43
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
43
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
43
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
43
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
43
what receptor activates adenylyl cyclase
Gi(alpha)
43
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
43
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
44
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
44
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
44
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
44
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
44
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
44
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
44
what receptor activates adenylyl cyclase
Gi(alpha)
44
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
45
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
45
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
45
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
45
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
45
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
45
what receptor activates adenylyl cyclase
Gi(alpha)
45
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
46
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
47
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
47
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
47
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
47
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
47
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
47
what receptor activates adenylyl cyclase
Gi(alpha)
47
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
47
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis
48
whooping cough- what g-protein is affected and the result to that protein
It is an inactivated Inhibitory G-Protein
48
Uveal melanoma- and mutations of the Gq a-subunit what is the result of this mutation?
blocking of GTP hydrolysis
48
what receptor activates adenylyl cyclase
Gi(alpha)
48
phospholipase Cbeta is an example of what?
Hydrophobic lipid in the membrane
48
maintenance of Ca2+ levels is driven by what factor/ pump
ATP-driven Ca2+ pumps
48
Lipases will target membrane lipids in order to generate 2 kinds of 2nd messengers, name the main 2
1. IP3- water soluble, diffuse through the cytoplasm
49
what does the G(beta-gamma) complex do after dissociation, in terms of proteins and signalling
ACTIVATE or INHIBIT various signalling pathways, enzymes
49
5 processes regulated by Ca2+ signalling
synaptic transmission hormone secretion and synthesis fertilisation Muscle contraction Cytokinesis

Advanced Mol Cell (11 decks)

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