About this Research Topic
G protein-coupled receptors (GPCRs) are omnipresent in the human body and account as drug targets for more than one third of currently marketed drugs. The number of GPCRs targeted by drugs is currently ca. 16% of the GPCRs in the human genome, suggesting that the GPCR-ome to be explored for druggability is still large. Drugs targeting GPCRs are small organic molecules, but also peptides. Indeed, given the novel experimental and computational approaches we see a growing number of peptide drugs in the market and a revival of interest in peptide ligands and peptide binding receptors.
Recent advances in structural biology and both computational and experimental methods foster our mechanistic understanding of peptide-binding GPCRs. This is essential to cope with typical challenges in peptide ligand design such as the larger binding site and the ligand’s flexibility.
This special issue aims at drawing a comprehensive picture of the current attempts to pharmacologically use peptide-binding GPCRs as drug targets and to design peptides as GPCR drug candidates. We welcome submissions (reviews, research articles, methods, perspectives/opinions, etc.) that address, but are not limited to, the following areas:
- Computational analyses and simulations of peptide-binding GPCRs
- Functional characterization of peptide-binding GPCRs
- Rational design of new modulators of peptide-binding GPCRs
- Clinical studies of peptides/proteins targeting GPCRs
- Strategies for the design of peptidomimetics and drug-like peptides
This collection will be compiled in cooperation with ERNEST COST Action.
Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
Recent advances in structural biology and both computational and experimental methods foster our mechanistic understanding of peptide-binding GPCRs. This is essential to cope with typical challenges in peptide ligand design such as the larger binding site and the ligand’s flexibility.
This special issue aims at drawing a comprehensive picture of the current attempts to pharmacologically use peptide-binding GPCRs as drug targets and to design peptides as GPCR drug candidates. We welcome submissions (reviews, research articles, methods, perspectives/opinions, etc.) that address, but are not limited to, the following areas:
- Computational analyses and simulations of peptide-binding GPCRs
- Functional characterization of peptide-binding GPCRs
- Rational design of new modulators of peptide-binding GPCRs
- Clinical studies of peptides/proteins targeting GPCRs
- Strategies for the design of peptidomimetics and drug-like peptides
This collection will be compiled in cooperation with ERNEST COST Action.
Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
Keywords: peptides, GPCRs, bioinformatics, molecular modelling, functional studies, structural biology, drug design
Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
