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Receptor Signalling
Created @January 21, 2025 12:59 PM
Class Principles to Neuroscience and Pharmacology
Learning Objectives:
Basic principles of Ligand- Receptor Interactions
General principles of G-protein receptors
Basic principles of GPCR and Intracellular Targets
Adenylyl cyclase-cAMP-PKA signalling pathway
Phospholipase C-PIPIP and DAG signalling pathway
GPCR regulation of ion channels
GPCR as drug targets
Basic principles of Ligand- Receptor Interactions
Ligands
Chemicals act on specific receptors to produce a particular response
Specificity
Certain ligands bind to certain receptors that can recognise specific drugs
Agonists
Drug bound to its receptor and mimics its response
Antagonist
Receptor Signalling 1
, Competes with agonists to stop the signal between the agonists and
the receptor
Blocks certain responses
Principles of Signal Transduction:
4 families of receptors
Most endogenous ligands are hydrophilic and are unable to across the cell
membrane
Nuclear Receptors can cross the cell membrane and are activated by
steroid hormones and other lipid soluble signals
Receptors acts as transducers by receiving a signal and transform it into a
different signal type, known as signal transduction
In GPCR- Ligands induce intracellular second messenger release that act
on different signalling pathways
General Principles of G-Protein Receptors:
Big family of cell surface receptors
Contains lots of ligands including neurotransmitters
All ligands have transmembrane domains
Extracellular domain binds to ligand
Intracellular domain binds to G-protein
G-protein binds to guanine nucleotides GDP and GTP
G proteins have subunits Alpha, Beta and Gamma
Subunits bind to GDP, GTP and undergo GTPase activity
Receptor Signalling 2
Receptor Signalling
Created @January 21, 2025 12:59 PM
Class Principles to Neuroscience and Pharmacology
Learning Objectives:
Basic principles of Ligand- Receptor Interactions
General principles of G-protein receptors
Basic principles of GPCR and Intracellular Targets
Adenylyl cyclase-cAMP-PKA signalling pathway
Phospholipase C-PIPIP and DAG signalling pathway
GPCR regulation of ion channels
GPCR as drug targets
Basic principles of Ligand- Receptor Interactions
Ligands
Chemicals act on specific receptors to produce a particular response
Specificity
Certain ligands bind to certain receptors that can recognise specific drugs
Agonists
Drug bound to its receptor and mimics its response
Antagonist
Receptor Signalling 1
, Competes with agonists to stop the signal between the agonists and
the receptor
Blocks certain responses
Principles of Signal Transduction:
4 families of receptors
Most endogenous ligands are hydrophilic and are unable to across the cell
membrane
Nuclear Receptors can cross the cell membrane and are activated by
steroid hormones and other lipid soluble signals
Receptors acts as transducers by receiving a signal and transform it into a
different signal type, known as signal transduction
In GPCR- Ligands induce intracellular second messenger release that act
on different signalling pathways
General Principles of G-Protein Receptors:
Big family of cell surface receptors
Contains lots of ligands including neurotransmitters
All ligands have transmembrane domains
Extracellular domain binds to ligand
Intracellular domain binds to G-protein
G-protein binds to guanine nucleotides GDP and GTP
G proteins have subunits Alpha, Beta and Gamma
Subunits bind to GDP, GTP and undergo GTPase activity
Receptor Signalling 2
