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Molecular Medicine > Cell Signalling > Flashcards

Cell Signalling Flashcards

0
Q

EC50

A

Ligand concentration that results in 50% activity of the receptors

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1
Q

Kd

A

Concentration that ligand occupies 50% of receptors

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2
Q

Binding vs activity

A

Hormone induces adenylyl cyclase activity in proportion to its binding ability.

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3
Q

Agonist

A

Binds and activates receptor

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4
Q

Antagonist

A

Bind receptor, prevents activation. Itself has no effect on receptor activity

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5
Q

Partial agonist

A

Bind and activate receptor to lesser extent than agonist

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6
Q

Inverse agonist

A

Binds active receptor and blocks the activity

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7
Q

Rate limiting step in G proteins

A

Catalysed release of GDP

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8
Q

Gs induces

A

Increase adenylyl cyclase, Ca and cAMP

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9
Q

Gi induces

A 
Decrease adenylyl cyclase, Ca and cAMP
Increase PLC (Ga and GBy)
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10
Q

GQ induces

A

Phospholipase C

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11
Q

Classification of GPCR

A

Class A - rhodopsin
Class B - secretin
Class C - glutamate
Other - adhesion R, frizzled/ taste 2

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12
Q

How to measure G protein association in cells

A

FRET - Fluorescence resonance energy transfer

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13
Q

Effect of cholera toxin

A

Inhibits GTPase (NAD dependent)

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14
Q

Effect of pertussis toxin

A

Prevents activation of Gi by receptor

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15
Q

Phospholipase C activated by two pathways

A

PTX insensitive - Gaq

PTX sensitive - Gai (direct activation by GBy, + Gai is called conditional)

16
Q

Compound that blocks inositol recycling

A

Lithium

17
Q

Molecules that can bypass receptor ligand and activate PKC

A

Phorbol

Ca ++ iodophors

18
Q

CAMP -> PKA ->

A

Activate metabolic enzymes

CREB - cAMP response element binding protein.

19
Q

Ca-calmodulin steps

A

Ca binds calmodulin. Conformational change. Binds inactive Calmodulin dependent protein kinase. Causes auto phosphorylation. Now fully active.

20
Q

RTKs regulate

A

Cell proliferation
Differentiation
Metabolism

21
Q

SH3 binds..

A

Pro line rich targets. Eg, sos

22
Q

RTK process

A

Ligand binds
Dimerisation
Trans auto phosphorylation

23
Q

Ras is required for..

A

DNA replication / entry in S phase

24
Q

GEF

A

Guanine nucleotide exchange factor

25
Q

GAP

A

GTPase activating protein

26
Q

Map kinase pathway

A

Raf binds Ras.

Raf now membrane bound. Activates MEK. Activates ERK. Activates transcription factor.

27
Q

What can stimulate Ras

A

GPCR ( PKC )
Arrestin
TKRs

28
Q

Homologous desensitization

A

Ligand stimulation causes reduced response of active receptor
GRK - G protein receptor kinases, phosphorylate ser/thr on c terminal and c3.

29
Q

Heterologous desensitization

A

Ligand stimulation causes decreased responsiveness of inactivated receptors.
PKA

30
Q

Give two formulas need for ligand hormone stuff

A

Get it right son.

Molecular Medicine (12 decks)

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