L02: Membrane receptors Flashcards
What are the 4 main types of receptors
- ligand gated ion channels (ionotrophic)
- G protein coupled receptors (metabotrophic)
- nuclear receptors
- kinase linked receptors
How do g-protein coupled receptors work
1) an agonist binds to the receptor
2) G proteins that contain alpha , beta and gamma subunit are attached to the proteins
3) nucleotide exchange occurs, so GTP is exchanged with GDP.
4) this activates gpcrs
5) alpha and beta+gamma subunit dissociate
6) alpha subunit is involved in secondary messengers
7) beta + gamma is involved in regulating ion channels
8) alpha subunit hydrolysed GDP back to GTP and everything resets.
What are the main alpha subunit types
- Gas
- Gai
- Gaq/11
- Ga12/13
What is the role of Gas
Stimulate the production of adenyly cyclase to make CAMP (second messenger)
What is the role fo Gai
Inhibit the production of adenyly cyclase so less CAMP is made
What is the role of gaq/11
Phospholipase C
What is the role of ga12/13
Regulates small G proteins of actin in muscle
Explain in detail what Gas does
- Converts ATP to CAMP by adenyly cyclase
- CAMP phosphodiesterase phosphorylates CAMP to degrade it to give AMP and limits the reaction
Explain in detail what Gaq/11 does
- stimulates an enzyme - phospholipase C
- Phospholipase C uses phopsholipids in particular PIP2 as a substrate
- this gives DAG and INSP3 (second messengers)
- INSP3 activates channels on the end plastic reticulum that releases calcium for muscle contraction
- DAG converts protein kinase C
How can CAMP become involved in glycogen activity after been made from Ga/s
- CAMP activates protein kinase A
- protein kinase A phosphorylates phosphorylase kinase to become active : phosphorylase kinase-p
- phosphorylase kinase p phosphorylates glycogen phosphorylase b to become active glycogen phosphorylase a
- glycogen phosphorylase a phophorlyates glycogen to remove glucose from it.
- protein kinase a phosphorylates glycogen syntrase to inactive p-glycogen syntrase to stop production of glycogen.
Which G proteins are involved in muscle contraction
- gas
- Gai
- gaq
What are the roles of gas and Gai
Gas activates adenyly cyclase to produce CAMP (second messenger) . CAMP inhibits MLCK so muscle relaxes.
Gai increases MLCK activity so muscle contracts.
What is the role of gaq.
Calcium influx so calcium activates MLCK for muscle contraction
Is phosphorylation of protein kinase and protein phosphatase reversible or irreversible
Reversible