BIOL1025 - Hydrophilic signalling - G-protein linked receptor Flashcards

1
Q

orphan receptor

A

unknown

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2
Q

G-protein receptor

A

superfamily of around 800 protein in human genome

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3
Q

structure of G-protein

A

has 7 pass structure - start N-terminus out of cell and end C terminus

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4
Q

roles

A

senses
neurotransmission
hormone secretion
chemotaxis etc

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5
Q

trimetric G-protein - large protein

A

a, b, y

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6
Q

a

A

has GTP and GDP binding and GTPase activity - GTP to GDP

GTP bind active signalling forming complex GDP - inactive

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7
Q

larges G protein

A

link to inner membrane associated with receptor

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8
Q

signal transduction by G-protein (inactive state)

A

GPCR bound to G-protein - if GTP -outer subunit then signal stops
ligand binds at extracellular of GPCR causing conformational change in receptor transmitted to Ga subunit to release GDP exchanging for GTP
which dissociates from Gby dimer and receptor - both active complex

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9
Q

when active

A

Ga and Gby causes signalling effects

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10
Q

no. of Ga

A

20
depends on form = different signalling events
Gas, Gai, Gaq

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11
Q

no. Gb

A

5

some can interact with ion channels

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12
Q

no. Gy

A

13

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13
Q

when active there are differences in … due to specificity to signals

A

expression pattern
receptor binding
effects produced in cells

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14
Q

target of activated Gas-subunit

A

activate GPCR by noradrenaline bind to receptor activates adenylyl cyclase
converting ATP to cAMP activating PkA by binding of cAMP to regulatory subunit of PkA by release catalytic subunit

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15
Q

PkA

A

protein kinase A - phosphorylating function

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16
Q

GPCR

A

G-protein coupled receptor

17
Q

cAMP

A

cyclic AMP

18
Q

formation of cAMP from ATP

A

by adenylyl cyclase - removing 2 phosphate groups = cyclic reaction between O and C3 and C5r = cAMP

19
Q

cAMP phosphodiesterase function

A

break down = inactive monophosphate (5’ AMP)

20
Q

example of Gas-subunit

A

beta adrenergic receptor

for signalling for neurotransmitter adrenaline

21
Q

B adrenergic receptor activated PkA

A

fast or slow

22
Q

fast activated PkA

A

phosphorylate and activate other enzymes

23
Q

slow activated PkA

A

bind to DNA regulating enzyme and transcription

24
Q

some prostaglandin receptors

A

a of activated GP inactivates adenylyl cyclase
receptor binds to GP
Gai binds to adenylyl cyclase and deactivates it decreasing in cAMP
PkA inactivates

25
Q

Gaq subunit

A

activated Gaq released - move around and activate phospholipase C
targets PIP2 cleaves = IP3 + DAG

26
Q

example of Gaq

A

Antidiuretic hormone

27
Q

PIP2

A

phosphatidylinositol-4,5-bisphosphate

28
Q

PC

A

phospholipase C

29
Q

PkC

A

Protein kinase C

30
Q

acetylcholine can activate 2 signalling pathways activating PC

A

IP3

Ca2+

31
Q

IP3

A

inositol 1,4,5 triphosphate
binds to Ca2+ in ER
increasing cytoplasmic [Ca2+] from 0.1 to 10 um

32
Q

IP3 - activating PkC

A

activates no. protein targets including transcription

terminated by conversion to inactive metabolite

33
Q

Ca2+ pathway

A

intracellular messenger
no. cellular process produced by Ca2+ increases and binds to calmodulin = conformational changes - bind protein
act as a switch

34
Q

termination of Ca2+

A

by ER pump - pumps Ca2+ back into ER

35
Q

example of calmodulin

A

CaM - kinase - calmodulin dependent kinase