G protein-coupled receptors (GPCRs) are the largest family of cell-surface proteins, characterized by seven trans-membrane domains, a cytoplasmic C-terminus and an extracellular N-terminal domain. GPCRs respond to a wide variety of signaling molecules including light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. These receptors are expressed widely in the body and play a vital role in the regulation of several important biological processes. Dysregulation of GPCR signaling is associated with several diseases and therefore, they are the most common target for pharmaceutical drugs.
Intense research work on GPCRs has generated considerable knowledge about fundamental signaling mechanisms and continues to produce novel therapeutic opportunities. However, only a small number of GPCRs have successfully been targeted and a vast number of these receptors have still not translated into successful drug targets, indicating that there is still untapped therapeutic potential. There are many experimental challenges before the therapeutic potential of all GPCRs fully uncovered. First, most of the GPCRs are identified based on sequence homology and many remain “orphan receptors” without a known endogenous ligand. Second, the majority of GPCRs who have been de-orphanised in the recent past are still poorly characterized in terms of biological function and regulation of their expression. Functional characterization of these poorly understood GPCRs have attracted significant attention in the recent past and is expected to help uncover novel therapeutic possibilities. Furthermore, due to virtue of unique and specific GPCR signalling pattern, particular GPCR could be targeted by designing specific ligand and altering signalling to cause favourable biases in GPCR functions.
The current Research Topic aims to cover recent, and novel research trends in the GPCR field. The topics that will be covered include but are not limited to:
• Diverse signaling mechanisms of GPCRs
• GPCR regulating proteins
• Mutations in GPCRs and human genetic disease.
• Orphan GPCRs and their de-orphanization
• GPCRS and pathophysiology
G protein-coupled receptors (GPCRs) are the largest family of cell-surface proteins, characterized by seven trans-membrane domains, a cytoplasmic C-terminus and an extracellular N-terminal domain. GPCRs respond to a wide variety of signaling molecules including light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. These receptors are expressed widely in the body and play a vital role in the regulation of several important biological processes. Dysregulation of GPCR signaling is associated with several diseases and therefore, they are the most common target for pharmaceutical drugs.
Intense research work on GPCRs has generated considerable knowledge about fundamental signaling mechanisms and continues to produce novel therapeutic opportunities. However, only a small number of GPCRs have successfully been targeted and a vast number of these receptors have still not translated into successful drug targets, indicating that there is still untapped therapeutic potential. There are many experimental challenges before the therapeutic potential of all GPCRs fully uncovered. First, most of the GPCRs are identified based on sequence homology and many remain “orphan receptors” without a known endogenous ligand. Second, the majority of GPCRs who have been de-orphanised in the recent past are still poorly characterized in terms of biological function and regulation of their expression. Functional characterization of these poorly understood GPCRs have attracted significant attention in the recent past and is expected to help uncover novel therapeutic possibilities. Furthermore, due to virtue of unique and specific GPCR signalling pattern, particular GPCR could be targeted by designing specific ligand and altering signalling to cause favourable biases in GPCR functions.
The current Research Topic aims to cover recent, and novel research trends in the GPCR field. The topics that will be covered include but are not limited to:
• Diverse signaling mechanisms of GPCRs
• GPCR regulating proteins
• Mutations in GPCRs and human genetic disease.
• Orphan GPCRs and their de-orphanization
• GPCRS and pathophysiology
