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GPCR

GPCRs, also known as seven transmembrane receptors, are a protein family that senses molecules outside the cell and activates intracellular signal transduction pathways to ultimately produce cellular responses. They are classified into six classes based on sequence homology and function. GPCRs play wide physiological roles including vision, smell, behavior regulation, immune function, and the autonomic nervous system. They have a structure of seven transmembrane helices and activate signaling pathways by undergoing a conformational change upon ligand binding that activates an associated G protein. GPCR signaling can be regulated through both homologous and heterologous mechanisms involving phosphorylation and arrestin binding.

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317 views

GPCR

GPCRs, also known as seven transmembrane receptors, are a protein family that senses molecules outside the cell and activates intracellular signal transduction pathways to ultimately produce cellular responses. They are classified into six classes based on sequence homology and function. GPCRs play wide physiological roles including vision, smell, behavior regulation, immune function, and the autonomic nervous system. They have a structure of seven transmembrane helices and activate signaling pathways by undergoing a conformational change upon ligand binding that activates an associated G protein. GPCR signaling can be regulated through both homologous and heterologous mechanisms involving phosphorylation and arrestin binding.

Uploaded by

anaeshkl
Copyright
© Attribution Non-Commercial (BY-NC)
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as DOC, PDF, TXT or read online on Scribd
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GPCR

~ aka 7 tranmembrane receptors/heptahelical receptors/ 7 transmembrane domain receptors/ G


Protein Linked Receptors

protein family of TM receptors that sense molecules outside cell and activate inside signal
transduction pathways and ultimately cellular responses

Ligand that bind include:


Light sensitive compounds
Odours
Pheromones
Hormones
Neurotransmitters

Classification

6 classes based on sequence homology and functional similarity


Class A to Class F
GRAFS (glutamate, Rhodopsin, Adhesion, Frizzled/Taste2, Secretin)

Physiological roles
- wide variety
- visual sense; rhodopsin
- smell: odorant/pheromones
- behavioral and mood regulation: serotonin, dopa, GABA, glutamate
- immune system activity and inflammation: histamine receptors
- autonomic nervous system

Structure

- 7 TM helices
- extracellular parts of receptor can be glycosylated: extracellular loops contain 2 highly
conserved cysteine reidues that form disulphide bonds

Mechanism
- activated by ligand
- conformational change  activation of G protein ( depending on type of G protein)

Ligands
- examples
- 3 types of ligands: agonist, inverse agonist, neutral antagonist
Conformational change
- ligand recognized, receptor shifts conformation and mechanically activates G protein
- G protein detaches from receptor
- GPCR can then activate other G protein or switch to inactive state
- GPCR exist in conformational equilibrium between active and inactive state
- Activated G protein are bound to GTP
- G protein cycle activated

GPCR signaling without G protein

Receptor Regulation
- 2 forms: homologous and heterologous
- homologous- activated GPCR is downregulated
- heterologous- activated GPCR causes downregulation of a different GPCR ( via
phosphorylation of intracellular receptor domain by Protein kinase)

By CAMP- dependent PK by GPCR Kinases


- activated PK A phosphorylate GPCR - phosphorylate only active GPCR

- 2 consequences
translocation
GPCR embedded in
Dephosphorylation will bring
back to surface

Arrestin-linking
Prevent from binding to G
protein

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