GPCRs 2 Flashcards
Membrane lipids may be targeted by receptor regulated lipases to generate 2 kinds of 2nd messengers :
(i) will be water soluble & diffuse through the cytoplasm eg. IP3
(ii) hydrophobic molecules, which remains in the membrane eg. DAG
role of lipid kinases
Lipid kinases add phosphate groups to lipids eg. To DAG to make phosphatidic acid , or to PI to generate PIP, PIP2, PIP3
what are PKCs
PKCs are Ser/Thr kinases , activated by DAG (C1 domain), and Ca2+ (C2 domain)
what are PMAs?
PMA phorbol ester is an analogue of DAG used in research to activate PKCs
how are PKCs activated
- DAG binding causes dissociation of intramolecular pseudosubstrate domain from active site
- Once activated PKCs can provide either Positive or Negative feedback in signaling pathway
• 5 processes regulated by calcium signaling
• 5 processes regulated by calcium signaling
Synaptic transmission
Hormone secretion & synthesis in some cases
Fertilization
Muscle contraction
Cytokenesis
2 ways that calcium is regulated in the cell
A- Calcium influx into the cytosol is regulated by voltage gated and ligand gated channels in the PM and ligand gated channels in the ER.
B- Store operated channels made up of ORAI and gated by STIM are responsible for store refilling
how is Information transfer encoded by calcium
Information transfer is encoded by the the amplitude, duration and frequency of store-released calcium signaling and translated by calcium-binding proteins to bring about changes in cell functions
difference between L,N,P type calcium channels
all voltage controlled
L type - in skeletal and cardiac muscle, brain
N type - neurones and endocrine cells
P-type - purkinje neurones