Lecture 10.5 - Signalling Molecules And Drug Targets Flashcards

1
Q

What does ordered physiological flow require?

A

Energy

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2
Q

What are the 2 types of signalling molecules?

A

Endogenous
Exogenous

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3
Q

What are the 3 types of classification of signalling molecules?

A

Endogenous
Exogenous I
Exogenous II

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4
Q

What is meant by an Endogenous signalling molecule?

A

Made within the body

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5
Q

What is meant by an Exogenous I signalling molecule?

A

Natural/plant based signalling molecule (not made in the body)

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6
Q

What is meant by an Exogenous II signalling molecule?

A

Synthetic/man made

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7
Q

What are the 3 ways by which signalling molecules act?

A

Endocrine
Paracrine
Autocrine

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8
Q

What is the importance of extracellular signalling molecules?

A

Allows separate parts of the body to work in synchrony

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9
Q

What are the tissues called which produce endocrine hormones/signalling molecules?

A

Glands

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10
Q

How do Endocrine signalling molecules act?

A

Travel over long distance in the body
Act on cells that have the specific receptors

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11
Q

What are some important body functions that are regulated by endocrine signalling molecules?

A

Digestion
Metabolism/respiration
Growth - Development
Behaviours

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12
Q

What is mean by a signalling molecule being highly potent?

A

Have a strong affect when in low concentration

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13
Q

Why is tight feedback control important in endocrine signalling?

A

Synthesis and degradation of hormones well controlled to ensure processes are well regulated

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14
Q

What are amines?

A

Amino acid derivatives

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15
Q

What are the 3 main types of Endocrine signalling molecules (Hormones)?

A

Amines (Catecholamines)
Peptides/proteins
Steroids

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16
Q

What is the solubility of Catecholamines?
Where are their receptors?

A

Hydrophilic
Plasma membrane receptors

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17
Q

What is the solubility of Peptides and Proteins?
Where are their receptors?

A

Hydrophilic
Plasma membrane receptors

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18
Q

What is the solubility of Steroids?
Where are their receptors?

A

Lipophilic/hydrophobic
Nuclear or cytosolic

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19
Q

What molecule are all steroids derived from?

A

Cholesterol

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20
Q

What is the time course of action for Catecholamines?

A

milliseconds to seconds

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21
Q

What is the time course of action for peptides and proteins?

A

Mins to hours

22
Q

What is the time course of action for steroids?

A

Hrs to days

23
Q

How do steroid hormones usually act?

A

Receptor hormone complex controls transcription/stability of mRNAs

24
Q

How do Catecholamine hormones usually act?

A

Change membrane potential or
Triggers second messengers

25
Q

How do peptide and protein hormones usually act?

A

Triggers second messengers
or
Triggers protein kinase activity

26
Q

How do Paracrine signalling molecules act? (Extracellular signalling)

A

Signalling coupled from cell to cell near to each other

27
Q

What sort of extracellular signalling molecule are neurotransmitters?

A

Paracrine signalling molecules

28
Q

How do neurotransmitters have an electrochemical action?

A

Chemical signal released from presynaptic membrane converts/stimulates electrical signal in post synaptic membrane

29
Q

What is an excitatory synapse?

A

Signal at presynaptic membrane stimulates an increase in firing rate post synaptically

30
Q

What is an inhibitory synapse?

A

Signal at presynaptic membrane decreases firing rate post synaptically

31
Q

What is a specific type of “Drug target” called?

A

Receptor

32
Q

What happens when a signalling molecule binds to its target receptor?

A

Bring about a change
(Could be changing a chemical/electrochemical signal)

33
Q

Are endogenous signalling molecules normally agonists or antagonists?

A

Mainly agonists

34
Q

How are exogenous signalling molecules different to endogenous signalling molecules?

A

Not made in the body
So the fit to receptors is not as optimal

35
Q

What is meant by exogenous signalling molecules act as Antagonists and Partial agonists?

A

Block or reduce/attenuate biological signal

36
Q

The majority of drug targets/signalling molecule targets can be remembered with what pneumonic?

A

RITE

37
Q

What does the pneumonic RITE for signalling molecule/drug targets stand for?

A

R - Receptors
I - Ion Channels (Voltage gated)
T - Transporters
E - Enzymes

38
Q

In chemotherapy, what is the target for the drugs?

A

Structural protein or DNA

39
Q

What are the 4 types of Receptors that can be targeted by drugs?

A

Kinase linked receptors
Ion Channels (Ligand gated)
Nuclear/Intracellular
G-Protein Coupled receptors

40
Q

What is the acronym that can be used to remember the 4 different types of receptors that can be targeted by drugs?

A

KING

Kinase linked receptors
Ion Channels (Ligand gated)
Nuclear/Intracellular
G-Protein Coupled receptors

41
Q

How kinase linked receptors work?

A

Ligand binds
Receptor self Phosphorylates
Triggers a further cascade affecting gene transcription/protein synthesis causing specific cellular effects

42
Q

How to ligand gated ion channels work?

A

Conformational change occurs once ligands bind
Ions can flow through causing hyperpolarisation or depolarisation

43
Q

How do nuclear receptors work?

A

Steroids move through to the receptor complex (can be ini the nucelus)
Affects gene transcription and so protein synthesis

44
Q

How do G-protein coupled receptors work?

A

Once bound activates G protein which will either bind to ion channel opening it
or trigger a second messenger cascade

45
Q

How doo voltage gated ion channels allow movement of channels?

A

Enable selective flow down its electrochemical gradient

46
Q

What is the difference between ligand gated ion channels and voltage gated ion channels?

A

Ligand gated ion channels = receptors

Voltage gated ion channels = ion channels

47
Q

What are voltage gated Na+/Ca2+ channel blockers used to treat?

A

Epilepsy, chronic pain and migraine

48
Q

How do GABA Cl- channels work?

A

GABA binds to chloride channel
Cl- comes in and causes hyperpolarisation

49
Q

What do transport/carrier proteins do?

A

Transport ions or small molecules

50
Q

What are the methods of transport that transporters or carriers use?

A

Facilitated diffusion
1º active transport (Directly use ATP against gradient)
2º uses pre-existing electrochemical gradient set up by a Na+/K+ ATPase

51
Q

What are the ways drugs can affect enzymes?

A

Bind to active site or bind to Allosteric site
Prevent their production

52
Q

The acronym king refers to the types of receptors What does the L stand for in KLING?

A

It is a reminder that the Ion channel is Ligand gated