Cell signalling G proteins
Cell signalling is a type of
communication that cells do with one another or with itself. It involves
transmitting ligands which are signalling molecules which then bind to a
receptor protein to create a change such a release a chemical or hormone.
G-Proteins
guanine-nucleotide binding protein.
G-Proteins coupled receptor
structure:
-7 transmembrane alpha
helices with a extracellular N terminus and a cytosolic C terminus containing a
ligland (signalling molecules) binding site also there is a cytosolic loop
between segment 5 and 6 binds specific G proteins.
GPCR (G protein coupled
receptors) are very common types of receptors on the plasma membrane and most
drugs produced work around these types of receptors.
1-Many G protein coupled
receptors have a large extracellular ligland binding domain when an
appropriate protein ligland binds to
this domain the receptor undergoes a conformation change that is transmitted
to its cytosolic regions which now activate a trimeric GTP binding protein also
called g protein.
2-A G protein consists of 3
protein sub units; Alpha beta and Gamma. Alpha and Gamma have contently
attached lipid tails which help anchor the G protein to the membrane, In the
absence of a signal the alpha sub unit has a GDP bound to it and the G protein
is inactive .
3-An activated receptor
induces a conformational change in the
alpha subunit causing the GDP to dissociate and GTP in the cytsol binds in its place
which causes a conformational change activating
both alpha sub unit and beta gamma complex now it can regulate the activity of target
proteins in the plasma membrane
4-The activated target proteins
then relay the signal to other components in the signalling cascade eventually the
alpha sub unit hydrolyses its bound GTP to
GDP which inactivates the sub unit. This is sped up by a protein called RGS (regulator
of g protein signalling). The inactivated alpha sub unit reforms with the beta and
gamma sub units which turns off other downstream events.
5-As long as the signalling receptor
remains stimulated it can continue to activate G proteins but after a very long
time it begins to get inactive. so a receptor kinase phosphorylates the cytosolic
portions of the activated receptor and then binds to a high affinity to arrestin
protein which inactivates the receptor by preventing any interactions with G proteins.
**REMEMBER TO STAY POSITIVE LIKE A PROTON!!**
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