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Fall 2019: OPT 112 AHP > Seven transmembrane domain receptors > Flashcards

Seven transmembrane domain receptors Flashcards

1
Q

Examples of seven-transmembrane domain receptors

A
  • Beta androgenic receptor
  • alpha androgenic receptor
  • muscarinic cholinergic receptor
  • VIP (vasoactive intestinal polypeptide (important for front part of the eye) and angiotensin II both affect blood vessels
  • 5HT (Serotonin)
  • DA (dopamine)
  • SP (pain receptor and neurotransmitter in the spinal cord)
  • Leutinizing hormone, folicle stimulating hormone, and thyroid stimulating hormone.
  • Rhodopsin
  • Platelet activating factor
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2
Q

Where on the receptor are binding sites for signaling molecules located?

A

Within the extracellular loops. This is also a great target for drugs and can influence the ability of the G protein to produce a result.

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3
Q

Internal loops are associate with what

A

The g-protein, microtubules, and cytoskeletal structures.

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4
Q

What happens when the first messenger binds to its receptor?

A

Intracellular calcium levels increase. Ca2+ is the second messenger and can enter through the membrane via Ca2+ channels or it can be released from the ER. (Calcium cannot be free in the cytosol because it can cause excitotoxicity- cell dies from over working itself).

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5
Q

An example of a cytotoxic disease, one where calcium is free in the cytosol and causes excitotoxicity.

A

ALS

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6
Q

Proteins that bind Ca2+

A

Calmodulin, calreticulin, and paravalbumin.

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7
Q

What is the role of a second messenger inside the cell

A

Modifies the signal, like a pansy scheme in reverse. (AKA it amplifies)
This is a slower ionotropic mechanism, but has a much wider effect with a low amount of stimulus.

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8
Q

Calsequesterin

A

Brings Ca2+ in and out (sequesters and isolates the calcium)

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9
Q

When Ca2+ is released from the ER, it is typically mediated by

A

IP3

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10
Q

4 alpha G-protein subunit types and their role when activated by GTP (Transducers)

A

Gs- adenylyl cyclase stimulation (increase CAMP)
Gi/o- adenylyl cyclase inhibitor (ion channels inhibitor CAMP phospholipase)
Gq- Phospholipase C activation. (increase DAG and IP3)
G1- Transducin cGMP phosphodiesterase found in the rod outer segment (activates Rho)

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11
Q

Kinase that can autophosphorylate itself

A

Tyrosine kinase can add a phosphate to itself or other tyrosine residues.

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12
Q

What does an activated protein kinase do?

A

Add Phosphates to serine or threonine residues to mobilize Ca2+

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13
Q

Protein kinases can be dependent on

A

CAMP, cGMP, PKc, calmodulin

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14
Q

Structure of tyrosine kinase

A

Exists as a single unit molecule (inactive monomers), but when it becomes a dimer, it can add phosphate groups to serine or threonine residues on molecules. Can mobilize Ca2+ and bring proteins to itself.

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15
Q

Inactive and active tyrosine kinase

A

Inactive- monomers not together

active- when phosphorylated, 2 monomers will form a dimer.

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16
Q

4 second messengers

A

cAMP, IP3, Arachindonic Acid (AA), and DAG

17
Q

Requirements for a first messenger

A

Must be external

18
Q

Calcium can be considered 2 things in a cascasde

A

Second messenger and a secondary effector

19
Q

cAMP system-

  1. External signal
  2. Receptor it binds
  3. Transducer
  4. Primary effector
  5. Second messenger
  6. Secondary effector
A
  1. NE
  2. B-adrenergic receptor
  3. Alpha subunit is Gs, which means it acts to increase cAMP.
  4. Adenlylyl cyclase
  5. cAMP
  6. cAMP dependent protein kinase (PKA)
20
Q

Phosphoionsitol system

  1. External signal
  2. Receptor it binds
  3. Transducer
  4. Primary effector
  5. Second messenger
  6. Secondary effector
A
  1. ACh
  2. Muscarinic ACh receptor
  3. Go (same Gi) ion channel inhibitor of cAMP phospholipases
  4. phospholipase C
  5. IP3 is created from PIP2 and goes to the ER to release calcium stores. Ca2+ activates DAG, which activates PKC.
  6. Ca2+ release from ER due to IP3 and Protein Kinase C activated by DAG
21
Q

Arachinodic acid system

  1. External signal
  2. Receptor it binds
  3. Transducer
  4. Primary effector
  5. Second messenger
  6. Secondary effector
A
  1. Histamine
  2. Histamine receptor
  3. Go/i, which is an ion channel inhibitor of cAMP phospholipase
  4. Phospholipase A2
  5. Arachidonic acid
  6. 5 lipoxygenase, 12 lipoxygenase, and cyclooxyrgenase
22
Q

cAMP pathway. PKA activation causes phosphorylation of ___

A

CREBP, cAMP response element binding protein, which modifies DNA.

23
Q

What is adenylyl cycalse

A

An integral membrane bound enzyme that synthesizes cAMP when stimulated

24
Q

IP3 is made by the hydrolysis of _____ and by which enzyme

A

PIP2, a phospholipid that is located in the plasma membrane by phospholipase C.

25
Q

Calmodulin can bind to how many molecules of calcium?

A
  1. Discovered at St. Jude.
26
Q

Rho

A

A type of GTPase that reorganizes the cytoskeleton through serine or threonine protein kinases

27
Q

Eicosinoids are made where and derived from what by what enzyme

A

Made in the plasma membrane, derived from arachidonic acid by PLA2 (phospholipase A2)

28
Q

Cyclooxygenase pathway (AA)

A

Produces prostaglandins, which have vascular and inflammation actions. Activates smooth muscle and regulates blood flow locally.

Produces thromboxjnes, which assist with blood clotting and other vascular actions.

29
Q

Lipooxygenase pathway (AA)

A

Produces leukotrienes, which mediate allergic and inflammatory reactions.

30
Q

Role of prostaglandins

A

Activates smooth muscle and regulates blood flow locally. Has vascular and inflammation actions

Produced through the cyclo-oxygenase pathway.

31
Q

Structure and role of leukotrienes

A

Has 3 conjugate double bonds.
Involved with vascular contraction and permeability regulators. Mediates allergic and inflammatory response.

Activated through the lipo-oxygenase pathway.

32
Q

NSAIDS and COX inhibits which AA pathway

A

Inhibits the cyclo-oxygense pathway, inhibiting the production of prostaglandins and thromboxjnes, both which play a role in blood clotting/blood flow and inflammation.

Fall 2019: OPT 112 AHP (28 decks)

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