G Protein coupled

Receptor (GPCR)
Adenylyl
Ligand
cyclase
binding

NH3+
M1 M2

outer
6 1 2 3 4 5 6 1 2 3 4 5 6
membrane
leaflets
1 4
inner
γ GTP α
γ α GDP after C1a
ATP
β ligand binding ATP
COO- β C2a

β/γ subunit Trimeric NH3+

COO- PPi
G Protein
2Pi
cAMP
β/γ subunits modify:
• phospholipase A (act.) GTP GeP cAMP activates:
• protein kinase C (act.) • cyclic AMP dependent protein kinases (e.g. protein kinase A)
• calcium channels (inh.) • phosphodiesterases
• Ras exchange factor (act.) • ions channels
• adenylyl cyclase II, IV (act.) GDP GeP • exchange proteins directly activated by cAMP (EPAC)
• adenylyl cyclase I, III, V, VI, VII (inh.) • cGMP phosphodiesterases adenylyl cyclases
• G protein coupled receptor kinases (GCRK) (act.) • formate-hydrolase transcription activator (GAF) proteins
 M1 M2

1 2 3 4 5 6 1 2 3 4 5 6

GTP α C1a
C2a
ATP ATP

NH3+
COO- PPi
2Pi cAMP
cAMP

R1 R2

C1 C2
P
CRE
PKAi P

CREB = cAMP response element-binding protein PKAa ATP ADP

CRE = cAMP response element sequence P
PKAa/i = protein kinase A (active/inactive) Energy metabolism regulation CREB CREB-P
 äußeres

Membran
leaflets

inneres

C=O C=O C=O C=O C=O C=O C=O C=O

O O O O O O O O
ATP ADP 1,2 Diacylglycerin
CH2 CH CH2 ATP ADP CH2 CH CH2 CH2 CH CH2 CH2 CH CH2 (DAG)
O O O Phospho- OH
P=O PI-5 kinase P=O
lipase C
O P=O PI-4 kinase O O
OH OH P H2O
O6 5 O6 5 O6 5 P P
Inositol

6 5
OH 1 OH 4 1 OH 4
1 4 OH HO OH HO
OH HO 1 OH 4
OH 2 3 P 2 P OH HO
2 3 3
2 3 P
Phosphatidyl- PI 4 phosphat PI 4,5 bisphosphat
(PIP2) PI 1,4,5 tris-
Inositol (PI) (PIP)
phosphat
(IP3)

Phospholipase C kann entweder

durch die aktivierte Gαq oder
durch die β/γ Untereinheit
aktiviert werden.