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GPCRs Flashcards

(19 cards)

0
Q

G alpha i stimulated by

A

PGE1

Adenosine

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1
Q

G alpha s stimulated by

A

ACTH
Glucagon
Epinephrine

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2
Q

Acetylcholine binds ________________ receptor = activates _________________ effector protein estimating in cellular ___________ and __________________.

Effector from activated by G alpha or G beta gamma?

A

Muscarinic, K+ channel
Hyperpolarization,
slows rate of heart muscle contraction

G beta gamma

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3
Q

cAMP activates

A

PKA

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4
Q

cGMP activates

A

PKG

Opens cation channels in rod cells

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5
Q

DAG diacylglycerol activates

A

PKC

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6
Q

IP3 opens

A

Ca2+ channels in endoplasmic reticulum

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7
Q

Which G proteins activate PLC(beta)?

A

G alpha naught

G alpha q

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8
Q

Pathway that leads to DAG+ IP3?

A

Phosphatidylinositol PI-> PI 4 phosphate -> PIP2 (PI 4,5- bisphosphate) -> IP3+ DAG

Last rxn preformed by phospholipase C beta

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9
Q

4 modes if herceptin action

A
  1. Prevents EGF ligand binding to receptor
  2. Prevents dimerization heterodimer
  3. Prevents cleavage of extra cellular domain (high Her2 =dimerization= activate pathway so protease cleaved off extracellular domain= hyperactivation )
  4. Activate immune response, which can then trigger a response to cancer cells
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10
Q

Herceptin

A

Monoclonal antibody mAb drug

Targets high Her2(RTK) expression in breast cancer

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11
Q

SH2

A

Src homology 2 domain
Sarcoma
Binds phosphotyrosine e.g on RTK

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12
Q

SH3

A

Binds prolong e.g 2 SH3 on GRB2 bind SOS GEF

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13
Q

GRB2

A

Growth factor receptor bound protein

Adaptor protein

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14
Q

Viral Src

A

Like normal: myr SH3 SH2 kinase domains

BUT missing carboxy terminus that contains regulatory Y527, inhibitory P by csk

Therefore constitutively active

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15
Q

PTB

A

Phosphotyrosine binding domain

Multi-docking protein

16
Q

IRS-1

A

Insulin receptor substrate protein

Contains PTB
multi-docking protein= recruit other adapter proteins

17
Q

Ras

A
Molecular switch 
Monomeric G protein 
GTPase switch protein 
Lipid anchored to PM 
Low GTPase activity 
Not linked directly to cell surface receptor 
Similar to G alpha but smaller 
Regulated by GEFs and GAPs

Mutation in G12 prevents GAP binding = cancer bc constitutively on

18
Q

Which is not only a serine theronine kinase?

Raf
MEK
MAPK

A

MEK

Also P tyrosine