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PODT- Treatment > 5. Receptor-Effector Coupling Mechanisms (2) > Flashcards

5. Receptor-Effector Coupling Mechanisms (2) Flashcards

1
Q

What is type 2 receptor superfamily?

A

Indirect (g-protein mediated) linkage to ion channel or enzyme

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2
Q

What is an example of phospholipase-C beta?

A

Smooth muscle contraction

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3
Q

What is IP3?

A

A second messenger which causes release of pre-stored calcium from intracellular organelles into the cytoplasm

(the opposite of cyclic AMP)`

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4
Q

What does the elevated cytoplasmic calcium ion conc regulates?

A

Activity of contractile proteins in smooth cardiac muscle
Secretion from exocrine and endocrine glands
Release of neurotransmitters
Activity of many enzymes and ion channels

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5
Q

What is DAG?

A

A second messenger which activates a phosphorylating enzyme called Protein Kinase C

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6
Q

What are the processes regulated by phosphorylation of cellular proteins by PKC?

A 
Contraction of smooth muscle 
Neurotransmitter 
Release of hormones from endocrine glands 
Receptor desensitization
Ion transport across membranes 
Inflammation
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7
Q

What are examples of drugs targeting receptors coupled to Phospholipase C-beta by G-proteins?

A 
Alpha1 adrenoreceptors  (blood vessels)
M3 muscarinic cholinoceptors (airway smooth muscle)
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8
Q

What are the agonists of alpha 1 adrenoceptors and examples?

A

Vasoconstrictors (noradrenaline/phenylephrine)

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9
Q

What are the antagonists of alpha 1 adrenoceptors?

A

Vasodilators

prazosin/doxazosin

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10
Q

What are the agonists of M3 muscarinic cholinoceptors?

A

Agonists are bronchoconstrictors (acetylcholine)

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11
Q

What are the antagonists of M3 muscarinic cholinoceptors?

A

Bronchodilators

ipratropium bromide, tiotropium

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12
Q

What is type 3 of receptor superfamilies?

A

Cell surface receptors that are enzymes (tyrosine kinase, guanylate cyclase)

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13
Q

What are examples of receptors of superfamily 3 that are linked to tyrosine kinase?

A

Insulin Receptor
Insulin- like growth factor receptor
Epidermal growth factor receptor

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14
Q

What are examples of receptors of superfamily 3 that are linked to guanylate cyclase?

A

Receptors for natruiretic peptides

Receptors for guanylin peptides

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15
Q

What is the structure of a receptor in superfamily 3?

A

Agonist binding site

N and C terminals connected by single transmembrane alpha helix

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16
Q

What is the significance of proteins changing shape during STM?

A

Shape change supports dimerization and coupling

17
Q

What does MAPK?

A

Mitogen activated protein kinase

18
Q

What are the characteristics of SH-2 domain-containing proteins?

A

Homologous to src oncogene product

SH-2 domain contains -100 amino acids

19
Q

What are examples of SH-2 domain-containing proteins?

A

Glucose transporter proteins responsible for glucose uptake across the cell membrane

MAPK enzyme involved in cell proliferation, differentiation and survival pathways

20
Q

Describe the JAK/STAT pathway

A
  • Receptor does not prossess its own tyrosine kinase
  • When agonist bind, receptor dimerizes and associates with cytosolic tyrosine kinase
  • Jak phosphorylates the receptor dimer
  • Phosphoylated receptor dimer is a binding site for transcription factor STAT
  • STAT is phosphorylated, travels to nucleus and alters gene expression
21
Q

Examples of drugs targeting tyrosine kinase linked receptor

A

Renal cancer drug (sunitinib)

Breast cancer drug (trastuzumab)

22
Q

Look at slide 23

A

Proccesses

23
Q

What is the action of natriuretic peptides?

A

Reducing the blood volume/pressure and returning to normal

24
Q

Look at slide 25

A

And diferences

25
Q

What is type 4 receptor superfamily?

A

Cytoplasmic/nuclear receptors (DNA-linked)

26
Q

What are the features of superfamily 4?

A

Small superfamily
Receptors for lipophilic steroid hormones
Receptors for lipid mediators already present in cell
Steroid and xenobiotic receptor
Receptors for lipophilic vitamins

27
Q

What is the structure of the receptor in superfamily 4?

A

Enitrely intracellular

Agonist binding site
DNA binding site with 2 zinc fingers
Hinge -influences receptor dimerisation
Regulatory domain

28
Q

What is the role of nuclear receptors?

A

Enhance or supress gene expression

29
Q

What is the mechanism of action of nuclear receptors?

A

Agonist bind to intracellular receptor

Zinc receptor domain will open up and and bind to Hormone Responsive Element located upstream from gene promoter region

30
Q

What does nuclear receptor therapeutics have inmplications for?

A 
Cancer
Inflammation
Reproductive disorders
Cardiovascular disease
Diabetes 
Obesity
31
Q

What are examples of nuclear receptor therapeutics?

A

Aldosterone receptor antagonists
-spironolactone

Glucocorticosteroid receptor agonists
-budesonide, beclometasone

Peroxisome proliferator-activated receptors (PPAR) for fatty acids
-pioglitazone

PODT- Treatment (12 decks)

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