Lecture 1 - Drug Action Flashcards

1
Q

What are the four types of proteins drugs act on?

A

Receptors
Ion Transporters
Enzymes
Transporters

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2
Q

What are the three main families of Receptors

A

G-Protein
Kinase-Linked
Nuclear Receptors

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3
Q

What class of receptor are GPCRs?

A

Metabotropic Receptors

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4
Q

GPCR N-Terminus

A

Extracellular
Site of Agonist Binding

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5
Q

GPCR C-Terminus

A

Intracellular
G-Protein coupled to an effector

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6
Q

How fast are GPCRs

A

Slow acting

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7
Q

GPCRs Class A

A

Neurotransmitters
Rhodosin Family

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8
Q

GPCRs Class B

A

Peptide Hormones

Secretin/Glucagon

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9
Q

GPCRs Class C

A

Metabotropic Glutamate and Ca2+

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10
Q

G-Protein: Ga(s)

A

Stimulates Adenylate Cyclase –> Increase cAMP

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11
Q

G-Protein: Ga(i)

A

Inhibits Adenylate Cyclase –> Decrease cAMP

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12
Q

G-Protein: Ga(q)

A

Activates Phospholipase C –> Increase IP3 and DAG

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13
Q

G-Protein: Ga(o)

A

beta and gamma subunits dissociate and cause effects

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14
Q

G-Protein: Ga(12/13)

A

Activates Rho & Rho Kinase
(Cell Growth)

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15
Q

G(beta/gamma)

A

Membrane Hyperpolarization
Activates K+ Channels
Inhibits voltage-gated Ca2+
Activate GPCR Kinase

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16
Q

What activates Kinase-Linked Receptors

A

Protein Mediators
Cytokines, Growth Factors, Hormones

17
Q

What process do Kinase-Linked Receptors control

A

Cell Division, Metabolism, Growth, Inflammation

18
Q

Main Types of Kinase-Linked Receptors

A

Receptor Tyrosine Kinases

Receptor Serine/Threonine Kinase

Cytokine Receptors

19
Q

What are Receptor Tyrosine Kinases

A

Phosphorylation of Tyrosine and then is incorporated intracellular

Regulate gene transcription

20
Q

What binds to RTKs

A

Growth Factors

21
Q

What are Receptor Serine/Threonine Kinases

A

Phosphorylates serine/threonine residues

22
Q

What are Cytokine Receptors

A

Receptors that when binded to activate kinases in the intracellular domain

Regulates Gene Transcription

23
Q

What are the characteristics of Ion Channels

A

Selectivity: What the channel is permeable to
Gating: What opens the channel

24
Q

Ionotropic Receptors

A

Ligand-Gated Ion Channel

25
Q

Metabotropic Receptors

A

G-Protein Coupled Receptors

26
Q

What are the 4 types of Ion Channels

A

Cys-loop type
Ionotropic Glutamate
P2X Type
Ca2+ Type

27
Q

Main families of transporters

A

ATP Binding Cassette (ABC)
Solute Carrier (SLC)
P-Type ATPase

28
Q

ATP Binding Cassette (ABC)

A

Use ATP hydrolysis to fuel efflux transporters

29
Q

Solute Carrier (SLC)

A

Involved in influx of small molecules

30
Q

P-Type ATPase

A

Na+/K+ ATPase

Helps maintain membrane potential

31
Q
A