Pharmacology: Receptors and Signalling Flashcards

1
Q

what is autocrine signalling

A

cell signals to itself

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is paracrine signalling

A

cell signals to its close neighbours

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what is endocrine signalling

A

blood vessels transport cell’s signalling molecules to distant target cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what are the 4 main types of receptors

A
  • LGICs
  • GPCRs
  • kinase-limited receptors
  • nuclear receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

where are LGICs and what are their ligands

A
  • plasma membrane

- hydrophilic signalling molecules, ‘fast’ neurotransmitters

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

where are GPCRs and what are their ligands

A
  • plasma membrane

- hydrophilic signalling molecules, ‘slow’ neurotransmitters

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

where are kinase-limited receptors and what are their ligands

A
  • plasma membrane

- hydrophilic protein mediators

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

where are nuclear receptors and what are their ligands

A
  • intracellular, cytoplams or nucleur membrane

- hydrophobic signalling molecules

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what are the 3 things that a ion channel may be gated by

A
  • transmembreane voltage (VGICs)
  • chemical signals (ligand)
  • physical stimuli (mechanical energy, temp)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what do ion channels do

A

create a ion conducting transmembrane pore

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what do LGICs consist of

A

several subunits creating a central ion-conducting channel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what can LGICs do

A

rapidly alter membrane potential

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

describe what happens when an agonist binds to a LGIC

A

agonist binds -> rapid conformational change -> ion channel opens -> ions conducted down electrochemical gradient -> cycles back to closed state

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what are secondary messenger system

A

receptor activation modulates an effectors activity

may increase or decrease rate of synthesis of secondary messenger molecules

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

basic structure of a G protein

A
  • peripheral membrane protein
  • 3 subunits - alpha, beta and gamma
  • alpha subunit has a binding site for GDP/GTP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

describe the difference between an active/inactive G protein

A
  • active, alpha subunit binds to GTP and dissociated from beta and gamma subunits (alpha-bound GTP and beta/gamme dimer)
  • inactive, alpha subunit binds to GDP
17
Q

describe what happens during GPCR activation

A
  • agonist binds and a conformational change occurs which:
  • alpha released GDP, allowing GTP to bind
  • alpha dissociates and regulates the effectors activity
  • agonist can dissociate but signalling can persist
18
Q

describe what happens when GPCR dissociates

A
  • the alpha subunit acts as an enzyme hydrolysing GTP to GDP + Pi
  • signal is turned off
  • alpha recombines with the beta and gamma subunits
  • G protein cycle complete
19
Q

describe GPCR signalling via adenyl cyclase and cAMP and pkA

A
  • G protein activated, Gs + GTP binds and activates adenyl cyclase
  • this converts ATP to cAMP
  • cAMP activate pkA, causing residue phosphorylation
  • cellular effects
  • G protein activated, Gi + GTP inhibits adenyl cyclase
20
Q

describe GPCR signalling via PLC, pkC, IP3, Ca2+ and DAG

A
  • G protein activated, Gq and GTP bind to phospholipase
  • PLC converts PIP2 to IP3 releasing DAG
  • IP3 binds to IP3 receptor in the ER, this releases Ca2+ causing cellular effects
  • DAG binds to pkC, causing phosphorylation of residues and finally cellular effects
21
Q

describe signalling via protein kinases

A
  • agonist binds and activated protein kinase
  • this causes autophosphorylation of residues
  • multiple adaptor proteins are recruited in response and phosphorylated
  • cellular effects
22
Q

what is another name for nuclear receptors

A

ligand-gated transcription factors

23
Q

describe signalling via nuclear receptors

A
  • steroid hormones enter the cell via diffusion and bind to the IC receptor
  • inhibitory protein dissociates and the steroid receptor moves to the nucleus
  • this forms a dimer and binds to the hormone response elements in DNA
  • transcription is switched on/off, altering mRNA levels and rate of synthesis of mediator proteins