Lecture 17: Signalling through GPCRs Flashcards

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1
Q

What causes GPCRs to become activated?

A

Extracellular ligands

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2
Q

What causes GPCRs to become inactivated?

A

Phosphorylation and internalisation

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3
Q

What causes the G protein complex to become activated?

A

When its bound to GTP

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4
Q

What is the name for the structure of the G protein complex?

A

Trimeric

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5
Q

What is the interaction of activated G proteins with ion channels?

A

They interact and cause them to open or close
This changes the cells behaviour

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6
Q

What is the interaction between membrane bound enzymes and G proteins?

A

Enzymes are activated
Production of intracellular signalling molecules called second messengers

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7
Q

What are second messengers?

A

Rapidly produced diffusible signalling molecules that activate effector proteins

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8
Q

What are the two stages of signal transduction?

A

Amplification and termination

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9
Q

What are the three different second messengers?

A

cAMP
DAG
IP3

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10
Q

What is the process of cAMP being produced in the cell?

A

Adenylyl cyclase converts ATP to cAMP
cAMP is inactivated by phosphodiesterase

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11
Q

What is the relationship between cAMP and PKA?

A

cAMP can activate PKA for it to be involved in gene transcription

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12
Q

What is the process of PKA being involved in gene transcription?

A
  1. PKA activated in cytosol
  2. Translocation to nucleus
  3. Phosphorylation of transcription factors
  4. Suppression or acceleration of target genes
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13
Q

How are IP3 and DAG produced?

A

Phospholipase C cleaves PIP2 into IP3 and DAG

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14
Q

What are phospholipases C?

A

Involved in cleavage of membrane phospholipids
Hydrolyse phosphorylated forms of PI 3 main groups

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15
Q

What are the three main groups of phospholipases C?

A

Activated by GPCRs
Activated by RTKs
Present in cytoplasm

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16
Q

What is the process of DAG and IP3 activating PKC?

A
  1. DAG recruits PKC to the membrane from cytosol
  2. IP3 opens Ca2+ channels
  3. Ca2+ bind to PKC and activate it
17
Q

What is in the regulatory domain of PKC?

A

C1
PS
C2

18
Q

What is in the catalytic domain of PKC?

A

C3
C4

19
Q

What is novel PKC?

A

Ca independent
PL sensitive
No C2
Group B

20
Q

What is atypical PKC?

A

Ca independent
PL insensitive
No C1 and part of C2
Group C

21
Q

What is the role of calmodulin and calcium?

A

Can bind together with target proteins
This alters the target proteins activity