G Protein-coupled Receptors are membrane proteins that transduce a vast array of extracellular signals into intracellular reactions ranging from cell-cell communication processes to physiological responses.

G Protein-coupled Receptors offers a unique view of academic and applied approaches aiming to reveal new ideas in pharmaceutical research.

Contents

Chemical Messengers and the Cell Membrane

1. Endocrine signalling by hormones
2. The nervous system and synaptic signalling by neurotransmitters
3. Paracrine signalling by local chemical messengers
4. Hydrophobicity: effect on release and transport of messengers
5. Membrane proteins and membrane receptors
6. Ligand receptor interactions

Radioligand Binding Studies

1. Technical aspects of radioligand binding
2. Saturation binding
3. Competition binding
4. Regional distribution of receptors

Functional Studies

1. Dose-response curves and associated problems
2. From receptor-occupation to stimulus and response
3. Receptor classification and antagonist affinity
4. Pharmacological models

G Protein-coupled Receptors

1. From receptor to response: introduction to GPCRs
2. GPCR structure
3. Ligand interaction with family A, B, C receptors
4. Receptor activation
5. Activated GPCRs: interaction with G proteins
6. Activated GPCRs: phosphorylation and internalisation
7. b-Arrestin- binding and MAP kinase activation
8. GPCR dimerisation and association with other proteins
9. Early models for GPCR activation
10. Restricted GPCR mobility and G protein coupling
11. Spontaneous receptor- G protein coupling
12. Interaction of two G proteins with one activated receptor state.
13. Multiple receptor conformations
14. Multistate receptors and multiple ligand binding sites
15. "Competitive", "non-competitive "and "insurmountable" antagonism
16. Naturally occurring mutations of GPCRs

Index

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