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Pharm Week > Pharmacodynamics - Receptor types > Flashcards

Pharmacodynamics - Receptor types Flashcards

1
Q

What are drugs designed to target?

A

Regulatory proteins in existing cell signaling pathways

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2
Q

What are 5 major classes of drug targets?

A 
Membrane receptors
Nuclear receptors
Ion channels
Transport proteins
Enzymes
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3
Q

In an inactive state, describe the setup of a GPCR

A

alpha subunit bound to GDP, as well as to the beta and gamma subunits

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4
Q

Once the ligand binds the GPCR it is converted to its active state. Describe the setup

A

Alpha subunit dissociates from the beta and gamma subunits and binds GTP

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5
Q

What subunit of the GPCR contains the gtpase activity?

A

Alpha subunit

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6
Q

Gs

A

Activates Adenylyl Cyclase

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7
Q

Gi

A

Inhibits Adenylyl cyclase

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8
Q

Gq

A

Activates PLC

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9
Q

G12/13

A

Activates RHO GTPases which then activates cytoskeleton rearrangements

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10
Q

G proteins are classified based on?

A

Alpha subunit induced effects

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11
Q

What occurs if the GPCR is active for a continued amount of time?

A

Desensitization = DECREASED cAMP

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12
Q

If the agonist is removed quickly from the GPCR what will occur?

A

Resensitization - full response to a second agonist

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13
Q

If downregulation occurs, where is the GPCR delivered?

A

Lysosomes

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14
Q

What are the 3 new players in GPCR resensitization?

A

GRK
Beta-arrestin
Protein Phosphatase

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15
Q

Describe how GPCR resensitization occurs

A
  • GRK phosphorylates GPCR and prevents it from interacting with Gs
  • Beta-arrestin binds the phosphorylated GPCR
  • Beta-arrestin - GPCR complex binds to coated pits and is internalized
  • Agonist dissociated from GPCR = decreased beta-arrestin affinity
  • Protein Phosphatase dephosphorylates GPCR
  • GPCR returned to plasma membrane
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16
Q

Gs activates Adenylyl Cyclase. What does AC activate?

A

cAMP

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17
Q

What hydrolyzes cAMP?

A

PDE

18
Q

Gq activates PLC. PLC then activates?

A

PIP2

- IP3 and DAG

19
Q

JAKs

A

Janus Kinases

20
Q

What types of ligands will activate JAK-STAT pathway?

A

Hormones and Cytokines

21
Q

When a cytokine binds to its receptor, JAKs are activated. What do JAKs do?

A

Phosphorylate and activate STATs

22
Q

Once 2 STATs are activated and phosphorylated by JAKs, what occurs?

A

They form a dimer and move to the nucleus to alter transcription

23
Q

When the JAK-STAT pathway is ON, what diseases occur?

A

Excessive inflammation

Autoimmune diseases

24
Q

What 3 things can JAK-STAT pathway INHIBITORS help control?

A

Rheumatoid Arthritis
Psoriasis
Inflammatory Bowel Disease

25
Q

Describe the JAK-STAT pathway

A

Cytokine binds to receptor
JAKs activated
JAKs phosphorylate and activate STATs
STATs form dimers
STATs go to nucleus and alter transcription
= Control immune-mediated inflammatory diseases

26
Q

What ligands bind to Receptor Tyrosine Kinases?

A

GROWTH HORMONES

“GF”

27
Q

Growth Hormones bind?

A

Receptor Tyrosine Kinases

28
Q

Once 2 Growth Hormones bind a RTK at 2 locations, what happens?

A

2 RTKs will join to form a dimer = ACTIVE

29
Q

Once RTKs form a dimer, what happens?

A

Auto-phosphorylation of tyrosine residues

30
Q

Once Tyrosine residues are auto-phosphorylated, what occurs?

A

Their enzymatic activities are activated and they can phosphorylate other substrates

31
Q

What receptors are involved with RAS?

A

Receptor Tyrosine Kinases

growth hormones

32
Q

How is RAS activated?

A
  • An adaptor protein binds to the phosphorylated tyrosine residues
  • A RAS activating protein binds to the adaptor protein and activates RAS GTPase
  • RAS is then bound to GTP and is active
33
Q

RAS activates?

A

Raf
MEK
ERK
= cell cycle overstimulated

34
Q

Oncogenes often affect what type of receptor?

A

Receptor Tyrosine Kinases – RAS pathway

35
Q

Nuclear receptors modulate?

A

Gene expression

36
Q

Ligands that bind to nuclear receptors must be ____

A

Lipophilic

37
Q

What type of ligands bind to nuclear receptors?

A

Steroids and hormones and Vitamins

38
Q

Nuclear receptors have a ligand binding domain, dna binding domain and transcription activating domain. What binds to the receptor in absence of a ligand to inactivate it?

A

Heat Shock protein 90 (HSP90)

39
Q

What causes the HSP90 to dissociate from the nuclear (glucocorticoid) receptor?

A

Binding of a ligand

40
Q

Glucocorticoid nuclear receptor activation causes?

A

Transrepression of NF-KB and AP-1

41
Q

Verapamil is an example of a drug that targets?

A

L-type calcium channels

Pharm Week (6 decks)

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