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bio 124 Lecture 2
Basics of communication
38
Biology
Undergraduate 1
02/23/2013

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Term
what are the 3 stages of cell signalling?
Definition

reception

transduction

response

Term
which stage involves the detection of a signal molecule?
Definition

reception

 

this involves detection by cell of a signal molecule usually originating from the outside of the cell

Term
what must a signalling molecule directly interact with in order for a signal to be detected?
Definition

a receptor on the cell surface or inside the cell

 

this stage is referred to as receptor binding

Term
what are signalling molecules also known as?
Definition
Ligands - small molecules that can lead to the change in the shape of a protein or aggregation of 2 or more receptors to interact with other molecules
Term

true or false?

the reception of a signal depends on the receiver?

Definition
true. analogy; a radio station broadcasts at a certain wavelength but you only hear it if you are tuned into the same wavelength.
Term
what messengers are detected by membrane bound receptors, are water soluble and often too large to pass through the membrane?
Definition
hydrophilic messangers
Term
which messengers can move through the lipid layer of the pm thus can be located inside the cell?
Definition
hydrophobic messengers
Term
name the 3 main types of receptors in the plasma membrane
Definition

G protein coupled receptors

receptor tyrosine kinases

ion channel receptors

 

most water-soluble signal molecules bind to specific sites on receptor proteins that span the pm.

Term
animals do not have receptor tyrosine kinases. what do they have instead?
Definition
RLK receptor like kinases
Term
name the largest family of cell surface receptors
Definition
G protein coupled receptors (GPCR) ~ 1000 encoded in human genome.
Term
A GPCR is a pm receptor that spans the membrane in which form?
Definition

7 even alpha helices.

 

GPCR work with the help of a G protein

Term
what does moving around phosphate in a cell do?
Definition
releases energy
Term
a G protein can bind GTP and GDP. what do these acronyms stand for?
Definition

GTP guanosine triphosphate

GDP guanosine diphosphate

 

G protein is a molecular switch, it can switch on or off.

Term
when GDP is bound to the G protein the G protein is ...
Definition

inactive.

 

ie. the switch is OFF

Term
when GTP is bound to the G protein, the G protein is..
Definition

activated.

 

ie, the switch is ON

Term
G Proteins are made from 3 subunits. What are they?
Definition
alpha, beta and gamma
Term
which side of the cell membrane are G proteins loosely attatched to?
Definition
the cytoplasmic side
Term

when a signalling molecule binds to the extracellular side of a GPCR the receptor becomes activated.

 

what happens in this activation stage?

Definition

there is a change in the shape of the receptor - the cytoplasmic side of the GPCR binds to the inactive G protein.

 

Term
the interaction between G protein and GPCR leads to GTP displacing GDP which activates the G protein. what do activated G proteins do?
Definition
they dissociate from GPCR and diffuse along the membrane binding to an enzyme which cause change of shape in enzyme leading to activation leading to a cellular response.
Term
what determines how often signalling occurs?
Definition

ligand concentration.

 

binding of ligands is reversible and ligands bind and dissociate many times

Term
the changes in enzyme and G protein are temporary because the G protein also functions as a GTPase enzyme - what does this enzyme do?
Definition
it hydrolyzes GTP back to GDP. this inactivates the G protein and it leaves the enzyme making it available for reuse.
Term

t or f

epinephrine or adrenaline from adrenal gland stimulates glycogen breakdown in liver and skeletal muscle during stress - this is an example of a signalling pathway that uses G protein coupled receptors

Definition

 true

 

60% of all medicines used exert their effects by influencing G protein pathway

Term
what do whooping cough (pertussis), cholera and botulism have in common?
Definition
the bacterial toxins in them interfere with normal G protein coupled receptor function
Term
receptor tyrosine kinases (RTK) are also membrane bound receptors but how do they differ from GPCR?
Definition
they have intrinsic enzyme activity.
Term
how do RTK act as tyrosine kinases?
Definition

they add phosphate residues onto other proteins.

 

A RTK can trigger multiple signal pathways at once


Term
what is abnormal functioning of RTK associated with?
Definition
cancer.
Term
before ligand binding the receptors exist as inactive monomers. what 3 things are found on each monomer?
Definition

extra cellular ligand binding site

membrane spanning region

intracellular tail containing multiple tyrosines

Term
binding of ligand eg. growth factor causes the 2 monomers to come together. what is the structure when they come together known as?
Definition

a dimer.

 

dimerisation activates the tyrosine kinase region of EACH monomer. each tyrosine kinase adds a phosphate from an ATP molecule to a tyrosine on the tail of the other monomer (6 in total) . the receptor is now fully activated and recognised by specific relay proteins inside the cell.

Term
what specific tyrosine must relay proteins bind to in order to be activated?
Definition

phosphorylated (fully activated tyrosine)

 

now each activated protein triggers a transduction pathway

Term
abnormal RTK linked to cancer. name the one RTK associated with some breast cancer patients and what treatment is approved for early stage breast cancer?
Definition

excessive levels of HER2 - human epidermal growth factor 2

poor prognosis


herceptin, a monoclonal antibody that binds to receptor is approved for early stage breast cancer. it binds to HER2 on cells inhibiting their growth and division

Term
name the channels that are important in the nervous system eg. neurotransmitter molecules released at a synapse between 2 nerve cell
Definition

Ligand-gated ion channel.

 

some gated channels are control by electrical impulses. these are known as voltage-gated ion channels and are crucial to the functioning of the nervous system

Term
many drugs exert their effects through modulating ion channels. what does Verapamil do?
Definition
it is a calcium channel blocker used to treat hypertension and other cardiovascular disorders
Term
many drugs exert their effects through modulating ion channels. what does Lamictal do?
Definition
it is a sodium channel blocker used for treatment of epilepsy
Term
many drugs exert their effects through modulating ion channels. what does Lidocaine do?
Definition
it is a sodium channel blocker and is used as a local anaesthetic
Term
many drugs exert their effects through modulating ion channels. what does Glipizide do?
Definition
it is a potassium channel blocker used in the treatment of diabetes
Term
what does a chemical messenger need to be in order to cross the membrane and activate receptors?
Definition

small or hydrophobic.

 

eg steroid thyroid hormones and nitric oxide, of animals.

plant steroids called Brassiunosteroids

Term

t or f?

activated hormone-receptor complexes can act as a transcription factor to turn on specific genes?

Definition

true. 

 eg. testosterone secreted by cells in testes > travels in blood and enter cells in body > only cells with appropiate receptors can respond >testosterone activates and intercellular receptor > hormone receptor complex enters the nucleus and acts as a transcription factor > mRNA produced > protein synthesis

 

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