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MCM-1 > Receptors and Ligands... > Flashcards

Receptors and Ligands... Flashcards

1
Q

What are the 6 enzyme-coupled receptors we discussed in MCM-1?

A
  1. receptor tyrosine kinase
  2. tyrosine-kinase-associated receptors
  3. cytokine receptor
  4. protein tyrosine phosphatases
  5. receptor guanylyl cyclases
  6. serine/threonine receptors
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2
Q

Generally speaking what type of receptor could you classify a receptor tyrosine kinase receptor as?

A

enzyme-coupled receptor

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3
Q

Generally speaking what type of receptor could you classify a tyrosine kinase associated receptor as?

A

enzyme coupled receptor

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4
Q

Generally speaking what type of receptor could you classify a cytokine receptor as?

A

enzyme coupled receptor

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5
Q

Generally speaking what type of receptor could you classify a protein tyrosine phosphatase as?

A

enzyme coupled receptor

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6
Q

Generally speaking what type of receptor could you classify a receptor guanylyl cyclase as?

A

enzyme coupled receptor

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7
Q

Generally speaking what type of receptor could you classify a serine/threonine receptor as?

A

enzyme coupled receptor

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8
Q

A receptor tyrosine kinase is an enzyme tyrosine kinase receptor that binds what ligands and has what effect?

A
  1. binds Growth Factors (GF) and membrane bound ligands

2. activation leads to phosphorylation of signal proteins

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9
Q

A tyrosine kinase associated receptor is an enzyme tyrosine kinase receptor that binds what ligand with what effect?

A
  1. binds to cytokines and interleukins

2. phosphorylation of singaling proteins

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10
Q

What is the difference between the receptor tyrosine kinases and the tyrosine kinase associated receptors?

A
  1. receptor tyrosine kinase bind with intracellular kinase domain.
  2. TKAR associates with a soluble cytosolic kinase domain which must migrate to the receptor tail in order to continue the signal sequence.
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11
Q

What role does protein tyrosine phosphatase play in the signaling pathway?

A
  1. these don’t have specific ligands, but when activated will lead to dephosphorylation of phosphotyrosines.
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12
Q

What is the role of the enzyme-coupled receptor, receprot guanylyl cylcase have in the signaling pathway?

A

activation by a ligand allows formation of cGMP

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13
Q

What is the ligand and activaiton effect of the serine/threonine receptor?

A
  1. ligand is TGF-beta

2. activation leads to Smad phosphorylation and transcription

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14
Q

What are receptors that require downstream proteolysis in order to lead to transcription activation? (shuold be 3)

A
  1. Notch receptor
  2. Frizzled receptor
  3. Patched receptor
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15
Q

Notch receptor must be bound with what ligand in order to cleave its cytosolic tail and allow the tail to migrate into the nucleus to activate transcription?

A

Delta

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16
Q

Notch and delta binding produces what sequence of events?

A
  1. notch tail is cleaved
  2. tail migrates through nuclear pore complex
  3. binds and activates transcription (or assists with activation)
17
Q

Frizzled receptor must bind with what ligand in order to prevent the phosphorylation and subsequent degradation of beta-catenin, which inhibits transcription?

A

must bind with Wnt

18
Q

Frizzled binding with Wnt will set into motion what sequence of events?

A
  1. beta-catenin is not phosphorylated.
  2. the APC unit is attracted to the frizzled/wnt complex
  3. beta-catenin (unphosphorylated) migrates into nucleus to assist with transcription activation
19
Q

To prevent the degradation of the Ci protein, the transmembrane protein Patched must be bound with what ligand?

A

hedgehog

20
Q

What are the subsequent events of Hedgehog and patched binding?

A
  1. patched activates smoothened
  2. preventing phosphorylation of protein “Ci”
  3. unphosphorylated “Ci” helps induce transcription.
21
Q

What are some common secondary messengers?

A
  1. cAMP
  2. cGMP
  3. PIP2
22
Q

What is a second messenger?

A
  • small intracellular signaling molecule that is generated in high amounts very quickly to diffuse to various parts of the cell.
23
Q

How is cAMP formed?

A
  1. ATP is acted on by adenylyl cyclase to form cAMP
24
Q

What is used to reduce the amount of cAMP?

A

cAMP phosphodiesterase

25
Q

What is the mechanism of action of how cAMP leads to convey a donwstream signal?

A
  1. 4 cAMP bind to regulatory domain on protein kinase A (2 per domain)
  2. Bind cAMP to the regulatory domain then releases the catalytic domain which can go on to activate whatever it needs to.
26
Q

Which enzymes are responsible for forming and degrading cGMP?

A
  1. formed with GTP and guanylyl cyclase.

2. degraded by GMP phosphodiesterase

27
Q

What are a few things that cGMP can move on to activate?

A
  1. activate protein kinase
  2. phosphodiesterases
  3. ion channels.
28
Q

The activation of protein lipase C will convert PIP2 into what secondary molecules that will have what effect?

A
  1. DAG–> protein kinase C

2. IP3–> Ca channels opening

29
Q

Aside from being cleaved to form IP3 and DAG, PIP2 can be activated to form what other secondary messenger?

A
  1. PIP3 with help from PI-3 kinase
30
Q

PIP3 activation is able to activate what kinase? What is the effect of activating that kinase?

A
  1. activates Akt

2. Akt leads to cell survival and protein synthesis.

31
Q

MAP kinases are responsible for what major process that occur within cells?

A
  1. regulation of growth and differentiation.
32
Q

What is the process of MAP kinase activation?

A
  1. growth factor binds (enzyme coupled receptor)
  2. forms Ras-GTP
  3. Ras-GTP binds with Raf
  4. Ras/Raf complex (map kinase kinase kinase) activate MEK
  5. MEK (map kinase kinase) then activates ERK (map kinase)
  6. ERK activates nuclear OR cytoplasmic proteins
33
Q

A cytokine binds and induces the dimerization of a JAK/STAT receptor. What is the process and final outcome of the cytokine binding?

A
  1. JAK phosphorylate cytoplasmic tail of the cytokine receptor
  2. phosphorylated tails attract the STAT molecules which then become phosphorylated themselves.
  3. The phosphorylated STAT, dimerize
  4. dimer migrates into nucleus to induce transcription
34
Q

The serine/threonine receptors are bound with TGF-beta leading to form a heterodimer. What happens next?

A
  1. the cytoplasmic regions phosphorylate each other
  2. leads to phosphorylation of protein “Smad”
  3. “Smad” migrates into nucleus to act as transcription factor.
35
Q

What is the role of NF-kappa B?

A

regulate the cell’s proliferation and survival.

36
Q

NF-kappa B promotes transcription.

A

TNFR binds with TNF, FASR binds with FASL, lingands that also bind with TNFR are cytokines, GF, or PAMPS. This binding will lead to the degradation of I-k-B, allowing free and now active NF-k-B to bind with DNA and induce trnascription

37
Q

Rho is able to alter the cytoskeletal changes. Meaning this molecule can be found in areas of the cell with high levels of what?

A

actin, and Rho is activated by integrin or growth factor receptors.

MCM-1 (8 decks)

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