Intracellular Signalling Pathway Flashcards

1
Q

Why are most receptors on the cell surface?

A

As most extracellular signalling molecules can not pass the plasma membrane

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2
Q

What is transduction?

A

Extracellular queue that causes a response

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3
Q

What are the 3 superfamilies of cell surface receptors?

A

G protein-coupled receptors
Ligand gated ion channels
Receptors with intrinsic enzymatic activity

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4
Q

How is a receptor activated?

A

When its complementary ligand binds

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5
Q

What do agonists do?

A

Bind to a receptors and activate it (stimulates)

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6
Q

What do antagonists do?

A

Bind to a receptor but do not activate it (blocks)

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7
Q

What are some examples of agonists?

A

Salbutamol (anti asthma)

Morphine (analgesia)

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8
Q

What are some examples of antagonists?

A

Propranolol (cardiovascular- hypertension)

Haloperidol (neuroleptics- anti-schizophrenic)

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9
Q

What do sensory GPCRs sense?

A

Light, odours and taste

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10
Q

What do GPCRs respond to?

A

Ions
Neurotransmitters
Peptide and non-peptide hormones
Large glycoproteins

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11
Q

What is the common basic structure of GPCR’s

A

Single polypeptide chain, 7 transmembrane regions, extracellular N terminal and intracellular C terminal

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12
Q

What areas of the GPCR can be responsible for ligand binding?

A

2-3 of the transmembrane domains

Or the N terminal region

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13
Q

What happens when a ligand binds to a GPCR?

A

Changes the conformational shape of the receptor
changes shape of GPCR
interacts with a G protein
G protein activated causing GTP to exchange for GDP on the alpha subunit
G protein dissociates into Alpha and GDP and also beta and gamma these then interact with effector
GTP reforms to GDP and subunits reform

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14
Q

How many G proteins does GPCR activate?

A

A single or small population of G proteins

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15
Q

How many different G proteins are there?

A

1000s

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16
Q

What does QISS QIQ mean?

A
Q -Alpha 1 - Phospholipase C
I- Alpha 2 - Inhibits Adenyl cyclase 
S- Beta 1 - Stimulates Adenyl Cyclase
S- Beta 2- Stimulates Adenyl cyclase 
Q- M1- Phospholipase C
I- M2- Inhibits Adenyl cyclase 
Q- M3- Phospholipase C
17
Q

How do Cholera and Pertussis toxin work?

A

Binds to the cell and enzyme is injected into the cell

18
Q

What does PTx do?

A

Stops GTP- GDP

19
Q

What does CTx do?

A

Stops GTPase

20
Q

Where is most of calcium found intracellular or extracellular?

A

extracellular

21
Q

How are increases in the cytoplasmic ca concentrations mediated?

A

Movement of Ca across the plasma membrane and release Ca from the ER

22
Q

How are increases in the cytoplasmic ca concentrations opposed?

A

Relative impermeability of the plasma membrane to Ca
Pumps and transporters that of ca out of the cytoplasm
Ca buffer proteins

23
Q

What is the PMCA?

A

Plasma membrane Ca- ATPase

Moves Ca out of the cell

24
Q

What is SERCA?

A

SR/ER Ca-ATPase

Move Ca into the SR/ER

25
Q

What is the NCX?

A

Na Ca exchanger

Moves Ca out of the cell and Na in- can be reversed

26
Q

What is VOCC?

A

Voltage operated Ca Channel

Moves Ca into cytoplasm

27
Q

What is LGIC?

A

Ligand gated ion channel

Moves Ca into cytoplasm

28
Q

What is CICR?

A

Calcium induced calcium release

29
Q

What is the IP3R?

A

Inositol 1,4,5- triphosphate receptors

Moves Ca out of ER into cytoplasm

30
Q

What does phospholipase C do?

A

catalyses the cleavage of the membrane phospholipid PIP2 into IP3 and DAG (second messengers)

31
Q

What is signal amplification?

A

A few molecules of binding to a cell surface ay cause a massive cellular response e.g. adenylyl cyclase- cyclic AMP to PKA

32
Q

What hormones increase the force of contraction in the heart?

A

Adrenaline and Noradrenaline by binding to ventricular B1 adrenoreceptors

33
Q

What hormone can cause vasoconstriction?

A

Noradrenaline by binding to a1 adrenoreceptors of vascular smooth muscle

34
Q

What hormone can cause bronchoconstriction?

A

Acetylcholine by binding to M3 muscarinic receptors of bronchiole smooth muscle

35
Q

What modulates neurotransmitter release?

A

presynaptic G protein coupled receptors

36
Q

What can G proteins inhibit?

A

specific types of voltage operated Ca2+ channels (VOCCs) reducing Ca influx and neurotransmitter release

37
Q

What is the summary of GCPRs?

A

Diversity, Specificity, Amplification