W1: Hormone-Receptor Interaction & Signalling Mechanisms Flashcards

1
Q

intracellular vs intercellular signalling

A

com w/in a cell

com btwn diff cells (I.e. extracellular signalling)​ -
Endocrine, autocrine, paracrine, neuroendocrine, NT​

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2
Q

ligand (key)

A

any molecule that binds to a specific site on a protein or other molecule e.g. hormone that binds to a receptor

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3
Q

receptor (lock)

A

a molecule that recognises & binds to a ligand w/ high specificity

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4
Q

affinity

A

Some hormones can bind to multiple diff receptors, but w/ diff affinities​

Some ligands don’t fit exactly into the receptor, but do work w/ a bit of adjustment

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5
Q

what molecules can a ligand be?

A

protein, lipid or carbohydrate

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6
Q

ligands - agonist vs antagonist

A

molecules that bind to a receptor & trigger a signalling pathway
molecules that bind to a receptor but do NOT trigger signalling (block the signal)

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7
Q

ligands - precursor form

A

e.g pro-hormones

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8
Q

ligands - binding partner

A

if ligand not soluble in blood, needs something to carry it around blood system

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9
Q

characteristics of protein & peptide hormones

A

Small or large​

Often pro-hormone (prod as AA chain, then processed)​

Hydrophilic​

Soluble (free) in blood, so shorter half-life (bc don’t always need carrier protein, so get degraded faster)​

Degraded by proteolytic enzymes​

Extracellular receptor (bc ligand can’t easily cross cell mem)​

Stored & rapid release (bc can’t get out of cell easily, able to make it inside cell then store it)

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10
Q

characteristics of steroid hormones

A

Small​

Hydrophobic​

Bound to plasma proteins, so longer half-life (protected from degradation)​

Intracellular receptor (bc ligand can cross mem)​

Synthesised on demand (bc tricky to store inside, as they’re able to cross plasma mem)​

Excreted (thru urinary system)

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11
Q

characteristics of thyroxine

A

Small, potent​
Hydrophobic​
Bound to plasma proteins​
Intracellular receptor​
Stored in thyroid by binding partner (has BP inside cell, so able to build up amount before releasing)

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12
Q

characteristics of epinephrine

A

Small, potent​
Hydrophilic ​
Soluble (free) in blood​
Degraded​
Extracellular receptor​
Stored in adrenal medulla

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13
Q

receptors

A

Proteins​
Molecular switches​
Trigger cellular mechanism​
Extracellular or intracellular​
Specificity - accuracy​
Affinity - strength, higher affinity constant (Ka) = stronger​
Avidity = total strength (sometimes ligands bind at multiple places on receptor, so multiple interactions, so helpful to work out total strength)

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14
Q

types of intracellular receptors

A

Some receptors are cytoplasmic (e.g. cortisol, oestradiol, testosterone, progesterone)​

Some are nuclear (e.g. thyroid hormones) (affect gene reg, so take longer to have an effect)

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15
Q

how does extracellular signalling work?

A

Signalling cascades ‘amplify’ the original signal (i.e. highly sensitive to hormone - often potent) (can also include gene reg)​

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16
Q

which hormones use extracellular receptors?

A

Cortisol, oestradiol, testosterone, progesterone, vit D​

17
Q

what are GPCRs?

A

G Protein Coupled Receptors​
7 transmembrane domains​
Once activated, trigger action inside cell

18
Q

examples of GPCRs

A

adrenaline receptor
glucagon receptor
oxytocin
PTH
somatostatin
thyrotropin
vasopressin
dopamine

19
Q

what are enzyme-coupled receptors?

A

Only 1 transmembrane domain​
Ligand binds to 2 receptors, bringing them closer together (dimerisation)​
Activates intrinsic enzyme activity

20
Q

examples of enzyme-coupled receptors

A

insulin receptor
GH receptor
platelet derived growth factor receptor
epidermal growth factor receptor

21
Q

what are phosphorylation cascades?

A

Commonly kinases (add phosphate group)​
Amplification​
High sensitivity (small input causes big output)​
Multiple possible outcomes
Reg of enzymes in signalling cascades commonly by phosphorylation (tyrosine, threonine & serine residues)
(But phosphorylation doesn’t always switch on!)

22
Q

kinases vs phosphatases

A

add phosphate

remove phosphate

23
Q

what are second messengers? what do they do?

A

Small intracellular signalling molecules​

Generated in large numbers in response to extracellular signal (amplification)​

Diffuse away from their source, broadcasting the signal throughout the cell​

Activate ‘downstream’ signalling molecules

24
Q

examples of second messengers

A

caMP
diacylglycerol (DAG)
IP3
Ca2+