Lecture 17: Signalling through GPCRs Flashcards
What causes GPCRs to become activated?
Extracellular ligands
What causes GPCRs to become inactivated?
Phosphorylation and internalisation
What causes the G protein complex to become activated?
When its bound to GTP
What is the name for the structure of the G protein complex?
Trimeric
What is the interaction of activated G proteins with ion channels?
They interact and cause them to open or close
This changes the cells behaviour
What is the interaction between membrane bound enzymes and G proteins?
Enzymes are activated
Production of intracellular signalling molecules called second messengers
What are second messengers?
Rapidly produced diffusible signalling molecules that activate effector proteins
What are the two stages of signal transduction?
Amplification and termination
What are the three different second messengers?
cAMP
DAG
IP3
What is the process of cAMP being produced in the cell?
Adenylyl cyclase converts ATP to cAMP
cAMP is inactivated by phosphodiesterase
What is the relationship between cAMP and PKA?
cAMP can activate PKA for it to be involved in gene transcription
What is the process of PKA being involved in gene transcription?
- PKA activated in cytosol
- Translocation to nucleus
- Phosphorylation of transcription factors
- Suppression or acceleration of target genes
How are IP3 and DAG produced?
Phospholipase C cleaves PIP2 into IP3 and DAG
What are phospholipases C?
Involved in cleavage of membrane phospholipids
Hydrolyse phosphorylated forms of PI 3 main groups
What are the three main groups of phospholipases C?
Activated by GPCRs
Activated by RTKs
Present in cytoplasm