Intracellular signalling Flashcards

lecture 13

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1
Q

What is signal transduction?

A

The process by which an extracellular signal activates a membrane receptor, which then alters intracellular molecules, activating a cellular response

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2
Q

What happens during signal transduction?

A

One form of signal is converted into another

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3
Q

Why are signal transduction pathways important?

A

They allow communication between cells of different tissues or organs.

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4
Q

What are the first and second messengers in signal transduction?

A

The first messenger is the extracellular signal molecule, while intracellular molecules form the second messenger system.

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5
Q

Name 4 examples of extracellular signalling molecules.

A

Amines (e.g., adrenaline)
Peptides/proteins (e.g, insulin)
Steroids (e.g., hormones)
Other small molecules (e.g, amino acids, gases)

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6
Q

How do small non-polar molecules like steroids signal?

A

They diffuse through the plasma membrane and bind to intracellular receptors, often acting as transcription factors for gene regulation (slow response).

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7
Q

How do large polar molecules signal?

A

They bind to cell surface receptors, activating intracellular pathways for a faster response.

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8
Q

What are the 4 main classes of receptors?

A
  1. Ligand-gated ion channels
  2. G-protein coupled receptors (GPCRs)
  3. Enzyme-linked receptors
  4. Nuclear receptors
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9
Q

What are ionotropic receptors?

A

Receptors that form an ion channel pore, such as nicotinic acetylcholine and GABA 𝐴 receptors

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10
Q

What are metabotropic receptors?

A

Receptors indirectly linked to ion channels through G protein-mediated signal transduction pathways, such as muscarinic acetylcholine and GABA 𝐵 receptors.

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11
Q

Compare ionotropic and metabotropic receptors.

A

Ionotropic receptors directly open ion channels, while metabotropic receptors activate signalling pathways to affect channels indirectly.

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12
Q

What are the components of GPCRs?

A

3 subunits:
alpha (α),
beta (β),
gamma (γ).

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13
Q

What is the common structure of GPCRs?

A

7 transmembrane domains encoded by over 800 genes.

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14
Q

What happens in the G protein cycle when adrenaline binds to a β-adrenoreceptor?

A

The receptor activates G protein interaction, GDP is exchanged for GTP, the α subunit activates adenylyl cyclase, and a cellular response occurs

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15
Q

How does cAMP activate Protein Kinase A (PKA)?

A

cAMP binds to PKA’s regulatory subunits, releasing the catalytic subunits to phosphorylate target proteins.

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16
Q

Give examples of cellular responses mediated by the cAMP/PKA pathway.

A

Kidney: Water retention by vasopressin
Cardiac muscle: Increased heart rate by adrenaline
Pancreas: Glucose release by glucagon

17
Q

How is signal transduction terminated?

A

Through signal or receptor removal/inactivation, dephosphorylation of proteins, or degradation of second messengers.

18
Q

What is the role of phosphodiesterase in signal termination?

A

PDE hydrolyses cAMP, rapidly decreasing its concentration to turn off the response.

19
Q

What happens during β-adrenoreceptor desensitisation?

A

Phosphorylation by β-ARK reduces receptor affinity for adrenaline, decreasing cellular response.

20
Q

Describe the structure of inactive PKA.

A

A tetramer with regulatory (R) and catalytic (C) subunits bound together, suppressing catalytic activity.

21
Q

How is PKA activated?

A

cAMP binding to R subunits releases active C subunits.

22
Q

What does active PKA do?

A

Phosphorylates serine/threonine residues on substrate proteins, affecting cellular functions.

23
Q

What does the nicotinic acetylcholine receptor do?

A

it forms an ion channel, allowing Na+ and Ca2+ entry upon acetylcholine binding, triggering electrical responses.

24
Q

What does the GABA 𝐴 receptor regulate?

A

It allows Cl- ion entry, serving as an inhibitory receptor important in the CNS.

25
Q

What does the muscarinic acetylcholine receptor regulate?

A

It activates signal transduction pathways via G proteins to affect ion channels indirectly.

26
Q

What is the role of protein phosphorylation in signalling?

A

Kinases transfer phosphate groups to proteins, altering their activity and triggering cellular responses.

27
Q

What is dephosphorylation, and what enzyme performs it?

A

Removal of phosphate groups by protein phosphatases, often deactivating the protein.

28
Q

How does caffeine affect signal termination?

A

Caffeine inhibits PDE, prolonging cAMP levels and cellular responses.

29
Q

Name a physiological response mediated by adrenaline through GPCRs.

A

Increased heart rate and relaxation of vascular smooth muscle.

30
Q

What is the role of CREB in the cAMP pathway?

A

Phosphorylated by PKA, CREb activates the transcription of target genes.

31
Q

What are the 3 main stages of signal transduction?

A
  1. Signal molecule binds receptor.
  2. Intracellular molecules relay the signal.
  3. Cellular response is activated.