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Final Year Project Pre-Reading: GPCR's in appetite and metabolic…
Final Year Project Pre-Reading:
GPCR's in appetite and
metabolic diseases
GPCR's
Activate internal signal transduction pathways.
Only found in eukaryotes
Two main signal transduction pathways
cAMP signal pathway
Phosphatigylinositol (IP3?) pathway
When a ligand binds to a GPCR, it changes structure and acts as a GEF. It then activates the associated G-protein by exchanging GDP for a GTP.
The G-proteins alpha subunnit then dissociates from the beta and gamma, affecting intracelular signalling proteins.
Three main classes: A, B and C
No sequence homology between the classes
Yet all have a common structure and mechanism of signal transduction.
Class A is the largest
Although this is the classic classification system used, there are many versions of classification of the GPCR's
The C class is dstinguished by their large N terminal tails
Structure
Integral membrane proteins
7 transmembrane helices
Extracellular loops can be glycosylated and contain 2 highly conserved Cys residues.
Extracellular N-terminus, intracellular C-terminus
Techniques
BRET
NanoBiT
TR-FRET
PCR
Site-directed mutagenesis cloning
Cell Culture
Receptors
GHSR
Ghrelin Receptor
SSTR's
Somatostatin Receptors
MC3-R
Melanocortin receptor-3
4 G-Protein Signalling Families
Monomeric (small) G-proteins
Heterotrimeric G-protein complexes
β
γ
α