Transporters as Drug Targets

4%
Percentage of drugs that work as transporters
1 of 25
Passive Diffusion
No protein required e.g. glycerol
2 of 25
Facilitated Diffusion
Protein required, along the concentration gradient e.g. glucose transporters
3 of 25
Primary Active Transport
Protein required, against the concentration gradient directed by ATP hydrolsis e.g. NA+K+ ATPase.
4 of 25
Secondary Active Transport
Protein required, against the concentration gradient directed by ATP hydrolsis. Gradient of ion used to couple transport, can be symporter or antiport.
5 of 25
P-class pumps
Transport of ions, specific to one or two kinds of ions, e.g Na+/K+
6 of 25
V-class pumps
Only transport H+. Maintain a low pH in vacuoles and lysosomes.
7 of 25
F-class pumps
Only transport H+. Transport protons down their electrochemical gradient, to power ATP synthesis pumps in mitochondria.
8 of 25
ATP binding cassette
Diverse class of pumps, transport all kinds of molecules e.g protein. Contains two trans-membrane domains and two cytosolic domains which bind to ATP.
9 of 25
Chloroquine
Prevent and treat malaria. Taken orally.
10 of 25
Vasicular Neurotransmitter Transports
Inhibitory/excitatory amino acid transporter, amine transporters. Used for neuronal identification.
11 of 25
Vesicular Glutamate Transporters
VGLUTs 1-3. Pack the neurotransmitter into synaptic vesicles, released into the synapse.
12 of 25
Plasma Membrane Transporters
Noradrenaline, dopamine, 5-HT, excitatory amino acid, GABA and glycine.
13 of 25
Glia
Non-neuronal cells in the CNS which maintain homeostasis, form myelin and provide support and protect for neurons,
14 of 25
Roles of Schwann Cells
Hold neurons in place to supply nutrients and oxygen; insulation; destroy pathogens and remove dead neurons; neurotransmitter and synaptic connections.
15 of 25
Serotonin
Monoamine neurotransmitter, contributes to well-being and happiness. Found in enteric nervous system of the GI tract. Produced in the raphe nuclei in the brain stem.
16 of 25
Citalopram
Antidepressant drug of the selective serotonin reuptake inhibitor class.
17 of 25
Dopamine Transporter
Pumps the neurotransmitter dopamine out of the synaptic cleft back into cytosol, turn it to vesicles for storage.
18 of 25
Dexamfetamine
Blocks monoamine transporters, potent in the CNS. Treats deficit hyperactivity disorder and narcolepsy.
19 of 25
Amfetamine
Increases levels of CNS stimulation
20 of 25
Cocaine
Inhibition of Dopamine Transporter (DAT) in through the Zn2+ binding site.
21 of 25
Glutamate Transporters
Neurotransmitter transporter proteins that move glutamate across the membrane. Two sub classes: vesicular glutamate transporter family and excitatory amino acid transporter family
22 of 25
Vesicular Glutamate Transporter Family
Move glutamate from the cell cytoplasm into synaptic vesicles
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Excitatory Amino Acid Transporter Tamily
Removes glutamate from synaptic cleft via glutamate reuptake into glial cells and neurons.
24 of 25
Riluzole
Drug which treats ALS. A disease which attacks nerve cells in the brain and spinal cord. The drug delays ventilator-dependence and increases survival rates by 2-3 months.
25 of 25

Other cards in this set

Card 2

Front

No protein required e.g. glycerol

Back

Passive Diffusion

Card 3

Front

Protein required, along the concentration gradient e.g. glucose transporters

Back

Preview of the back of card 3

Card 4

Front

Protein required, against the concentration gradient directed by ATP hydrolsis e.g. NA+K+ ATPase.

Back

Preview of the back of card 4

Card 5

Front

Protein required, against the concentration gradient directed by ATP hydrolsis. Gradient of ion used to couple transport, can be symporter or antiport.

Back

Preview of the back of card 5
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