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Pharmacology > Receptors, signals ans responses > Flashcards

Receptors, signals ans responses Flashcards

1
Q

why is cell communication important?

A

there are lots of tissues, organs + cell types in the human body - need to keep responding to changes in environment.

Growth, infection, blood glucose, wounds, and time to die.

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2
Q

3 important steps in cell signalling

A

signal, receptor, response

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3
Q

cellular response without a signal can lead to

A

cancer

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4
Q

over reacting immunity signals

A

inflammatory response

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5
Q

not responding to immunity signals

A

immunodeficiency

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6
Q

which cells make insulin?

A

Beta cells in the islets of lagerhands, located in the pancreas

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7
Q

what do the alpha cells in the pancreas make?

A

glucagon

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8
Q

what happens when there are low blood sugar levels?

A

glucagon is released, tells the cells that you need fat cells to start releasing their energy source to maintain blood sugar levels

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9
Q

ENDOCRIN SIGNALLING

A

hormone secretion into the blood by an endocrine gland - to act on distinct target cells in the body

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10
Q

PARACRINE SIGNALLING

A

cells secrete signals close to the target cells

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11
Q

what are direct contacts?

A

in the epithelial sheet forming connections between cells.

they detect signals from neighbouring cells and the ECM (how rigid is the ECM)

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12
Q

what is synaptic signalling

A

where nerve cells release neurotransmitter into the synaptic cleft - taken up and causes a response in the target cells

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13
Q

example of hormones that use endocrine signalling

A

testosterone and insulin

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14
Q

examples of paracrine signalling

A

growth factors, cytokines (immune cells), NO

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15
Q

what are neurotransmitters derived from/

A

amino acids

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16
Q

what are steroids derived from?

A

cholesterol

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17
Q

example of a small molecule signal

A

adrenaline

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18
Q

examples of peptide hormones

A

hCG, LH

insuline

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19
Q

example of a steroid hormone

A

testosterone

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20
Q

what are the 4 main receptor types

A

steroid receptors, G protein coupled, ligand gated channels, enzyme linked

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21
Q

what are 2 main types of repsonsed to signals

A

Turn genes on or off

Modulate the activity of cellular proteins

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22
Q

what are steroid receptors?

A

they are transcription factors/activators that turn genes on and off

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23
Q

are steroid lipophilic or hydrophilic?

A

lipophilic

so they diffuse across cell membranes

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24
Q

where would you find a steroid receptor?

A

in the nucleus or cytoplasm

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25
sequence of events for steroid receptors
2 steroid receptors – form dimer – only in this form can the steroid recpetors act as transcription factor – need to bind to enhancer – induce recruitment of standard transcription machinery to the proton region (initiation complex) and then polymerases transcribe the gene
26
What does the enhancer region do?
coordinated signals and timing
27
what provides specificity for steroid receptors?
Different steroid receptors bind different steroids and different steroid receptors different enhancers
28
which drug is used for medical abortions?
Mifepristone
29
how does Mifepristone work in abortions?
receptor antagonist, antagonises the progesterone receptor, stop the cells being able to produce progesterone, progesterone cannot maintain pregnancy
30
what is cushing's syndrome?
over production of cortisol (adrenal gland tumours)
31
how would you treat cuttings syndrome?
Making too much steroid – inhibitors which inhibit pathway where cholesterol is turned into cortisol – blocking the formation of signal using ketonazole metyrapone
32
what drug would you use to break cushings
Ketoconazole Metyrapone
33
ligand gated ion channels open in response to...
a signal to allow ions to flow through
34
what type of receptors do neuromuscular junctions use?
ligand gated ion channels
35
what happens in neuromuscular junctions?
Ach is released into the synaptic cleft from the vesicles in the presynaptic knob, when the vesicles fuse with synaptic membranes they bind to the receptors and allow ions to flow through the channels into the muscle
36
which enzyme mops up/breaks down Ach?
Acetylcholinesterase
37
how does botulinum toxin work to stop muscle movement?
it inhibits Ach release, so there is no AP and so no muscle contraction
38
what affect does nerve gas have on muscle contraction and why?
nerve gas inhibits AchE - Ach can't be broken down so you get constant signal - excessive muscle contraction
39
what fraction of human genes code for GPRCs
1/20 genes
40
what percentage of pharmaceuticals work on GPRCs
40%
41
examples of what some GPRCs do
Immune modulators (chemokines), taste and smell, hormones (adreneline) synaptic (some) , eyes use to detect light
42
how does adrenaline affect skeletal and cardiac muscle - lung bound to GPRCs
More energy Increased blood and air (vasodilation) ``` Weaker contraction (smooth muscle) Stronger contraction (skeletal muscle) ```
43
how does adrenaline affect gut and skin bound to GPRCs
``` Less energy Less blood (vasoconstriction) ``` Stronger contraction (smooth muscle)
44
the same hormone can bind to
different receptors
45
where would you find a1 adrenoreceptors
in the GI tract
46
what response do a1 receptors have to adreneline
smooth muscle contraction and casoconctriction
47
where would you find B1 arenoreceptors
heart
48
what response do B1 adrenoreceptor have to adrenaline
inc. heart muscle contractility
49
where would you find B2 adrenoreceptors
in the lungs
50
what response would you get if B2 receptors were stimulated with adrenaline
smooth muscle relaxation and vasodilation in the lungs
51
GPRCs are molecular
switches ``` On = bound to GTP Off = bound to GDP ``` GTPases
52
GPRCs are coupled to
a heterotrimeric subunit
53
which part of the heterotrimeric subunit binds GTP/GDP
the a part
54
in GPRCs what amplifies the signal
second messengers - eg cAMP
55
how do B adrenergic receptors in heart, skeletal and lungs work
G protein receives signal, Gas dissociates from the other 2 when bound to GTP, stimulates adenylate cyclase to convert ATP to cAMP very quickly, which then activated PKA which will phosphorylate target proteins
56
what is so beneficial about second messengers
small , produced rapidly , produce lots cellular response
57
what do kinases do?
add phosphates to things
58
what do specific Specific serine/ threonine/ tyrosine residues do?
regulate activity and localisation
59
what is the chemical formulation of phosphate?
PO4
60
what do beta blockers do?
heart conditions, high blood pressure combating
61
what is an example of B adregenergic receptor antagonist
propanolol
62
what do B antagonists end in
-olol
63
what is a B antagonist in the lungs - for asthma
salbutamol
64
what turns off the signal in the in Gas
phosphodiesterase | converts cAMP back to AMP
65
which phosphodiesterase inhibitor is used to treat heart failure? how does this work?
PDE 3 inhibitor increase the amount of cAMP
66
how does the Kinase linked receptor work?
Outside portions bind – dimerise – brings kinases domains close together – phosphorylate one another Lots molecules in cell – recognise phophorylated target site – recruitment to receptor – turn on G protein This G protein is called ras
67
what is ras?
a small GTPase
68
in the kinase linked receptor what is the purpose of Ras?
induce a MAP cascade then the Pi binds to transcription factor (transcription factors are phosphorylated) and then move into the nucleus
69
what is the function of perception in cancer?
stops EGF binding to its tyrosine kinase receptor - so the to receptors cannot phosphorylate one another - cannot promote growth inside the
70
what would you use if you had a mutation in Ras so that you cannot turn it off?
inhibitor that block MAP kinase function
71
how does PKA affect cardiac muscle?
phosphorylates L type calcium channel - Ca2+ flows in and then myosin chains contract, muscle contraction.

Pharmacology (18 decks)

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