BIOL1025 - Hydrophilic signalling - G-protein linked receptor Flashcards
orphan receptor
unknown
G-protein receptor
superfamily of around 800 protein in human genome
structure of G-protein
has 7 pass structure - start N-terminus out of cell and end C terminus
roles
senses
neurotransmission
hormone secretion
chemotaxis etc
trimetric G-protein - large protein
a, b, y
a
has GTP and GDP binding and GTPase activity - GTP to GDP
GTP bind active signalling forming complex GDP - inactive
larges G protein
link to inner membrane associated with receptor
signal transduction by G-protein (inactive state)
GPCR bound to G-protein - if GTP -outer subunit then signal stops
ligand binds at extracellular of GPCR causing conformational change in receptor transmitted to Ga subunit to release GDP exchanging for GTP
which dissociates from Gby dimer and receptor - both active complex
when active
Ga and Gby causes signalling effects
no. of Ga
20
depends on form = different signalling events
Gas, Gai, Gaq
no. Gb
5
some can interact with ion channels
no. Gy
13
when active there are differences in … due to specificity to signals
expression pattern
receptor binding
effects produced in cells
target of activated Gas-subunit
activate GPCR by noradrenaline bind to receptor activates adenylyl cyclase
converting ATP to cAMP activating PkA by binding of cAMP to regulatory subunit of PkA by release catalytic subunit
PkA
protein kinase A - phosphorylating function