G proteins as drugs ( enzyme linked and intracellular receptors )

Question 1

tyrosine kinase linked recepits are agonists and they phosphorylates —- on key signalling molecules for the activation of —-

Answer 1

• tyrosines
• cell signalling

Question 2

intracellular receptors are agonist and they transport to —- and responsible for the activation of ——

Answer 2

• nucleas
• transcription and translation

Question 3

ligand gated ion channels are agonists that deals w — and activates —-

Answer 3

-Na
- conductance

Question 4

• G protein coupled receptors are agonist and the G protein activation causes the generation of —– which leads to activation of —-

Answer 4

• second messenger
• cell signalling

Question 5

how does the receptor tyrosine kinase ( RTK) structure allow it to receive and transmit signals?

Answer 5

-extracellular domain : responsible for capturing or binding signals ( ligands )
- intacellular tyrosine kinase domain: responsible for transmitting signal when ligand bound

Question 6

mechanism of action of receptor tyrosine kinase :
1. ligand —– , —— , and —
2. binding of —– to —-
- these —- proteins link — molecules together but they don’t —–
- growth receptor binding protein 2 is an —–
- one arm of Grb2 reconginizes a —-on active site ( SH2 domain )
- other arm recognises — on signalling molecules ( SH3 domain )
3. binding of — to active Ras
- —- is a g protein ( small GTPase ) required to transmits RTK cell signalling
- SoS acts to convert —- Ras into —- Ras by —- it and removing —–
- once this happens Ras binds to — and makes it —-
4. Ras —-
- active — triggers the activation of numerous cell signalling pathways which changes proteins — and —–
this leads to cell —-

Answer 6

• ligand binding
• dimerisation
• and autophorphorlation
• adapter protein
• active receptor
• adapter
• signalling
• they don’t signal
• adapter proteins
• phosphotryrosine
• proline
• RTK-Grb2-SoS
• Ras
• inactive
• active
• binding
• GDP
  -GTP
• active
• cell signalling
• Ras
• activity
• gene expression
• cell proliferation

Question 7

how does ligand-gated ion channels linked receptors structure allow it to receive and transmits signals?
- ligand gated ion channels contain —- subunits around a —-
- has —–
- membrane receptor coupled directly to —-
- example:

Answer 7

• receptors
• central pore
• transmembrane spanning
• ion channel
• neurotransmitter

Question 8

mechanism of action of ligand gated ion channel linked receptors:
1. — binds and channels —
-when a — binds to a receptor the channel — and activates a —- of ions
- —- of receptors and channel
- — response - hormones binding promots ion gates to open in —-

Answer 8

• hormone
• opens
• hormone
• opens
• influx
• direct coupling
• rapid
• milliseconds

Question 9

stages of ion channel linked receptors activation summary
1. resting —>
2. activated —>
3. inactivated —->

Answer 9

1. able to respond to ligand stimulus
2. open to ion flux
3. desensitised to stimulus

Question 10

glucorticodes is an example of —

Answer 10

nuclear receptor

Question 11

-in nuclear receptor , the ligand enters the cell to interact with its —
-recepor-ligand — throughout cell to interact directly w —-
- changes cell gene —-

Answer 11

• ligand
• translocates
• nucleas
• expression profile

Question 12

how does the nuclear receptor structure allow it to receive and transmits signals ?
it contains :
a —- binding site to bind to ligand and chaperone
a — binding site to interact w defined sites in genome

Answer 12

• hormone
• dna

Question 13

nuclear receptors mechanism of action:
1. —- ligand receptor binding
- — hormones enters via —-
- receptor in the —- bound to a molecular —-
- hormone binding to a receptor causes — of molecular chaperone
2. steroid complex can translocate to —-
- steroid hormone bound to a receptor can translocate to the — once the — is removed
3. — binding domain of steroid receptor complex binds to a specific —- region
- binds to — associated receptors to initiates —- programmes
4. generation of —- protein response
- the gene expression profile of cell changes due to initiation of —– programmes triggered by —

Answer 13

• intracellular
• steroid
• cell membrane
• cytosol
• dissociation
• nucleas
• nucleas
• chaperone
• dna
• genomic
• dna
• genomic
• dna
• gene expression
  ( info:
  LBD: ligand binding domain
  DBD: dna binding domain
  AD: activation domain )
• anti-inflammatory
• transcriptional
• steriod receptor complex