G-protein-coupled receptors (GPCRs) are membrane proteins that regulate several cellular functions involved in physiology and the human body's homeostasis and the onset and progression of different diseases. GPCRs-signalling pathways may be affected under pathological conditions because of changes in the receptors' expression or activity, leading to dysregulated systems. Therefore, the development and the study of molecular modulators for GPCRs are worthy of interest in the diagnostic and therapeutic scenarios.
The co-editors of this Research Topic welcome original research and review articles with a broad range of relevance to the design, development, and biological evaluation of molecular modulators of GPCRs-mediated signaling.
The Editors are interested in works covering the following areas:
• Design, synthesis, and characterization of small molecules as GPCRs modulators;
• Design, synthesis, and characterization of peptides and peptidomimetics as GPCRs modulators;
• Development of chemical probes (i.e., fluorescent tools) to investigate cell signaling mechanisms;
• Development of chemical probes for the high-resolution structural analysis of GPCR complexes;
• GPCRs allosteric modulators;
• Biased GPCR signaling;
This collection of articles would contribute to understanding the molecular mechanism of signal transduction cascade in support of the development of functionally selective therapeutics.
This collection has been generated as part of the
ERNEST COST Action collaboration.
G-protein-coupled receptors (GPCRs) are membrane proteins that regulate several cellular functions involved in physiology and the human body's homeostasis and the onset and progression of different diseases. GPCRs-signalling pathways may be affected under pathological conditions because of changes in the receptors' expression or activity, leading to dysregulated systems. Therefore, the development and the study of molecular modulators for GPCRs are worthy of interest in the diagnostic and therapeutic scenarios.
The co-editors of this Research Topic welcome original research and review articles with a broad range of relevance to the design, development, and biological evaluation of molecular modulators of GPCRs-mediated signaling.
The Editors are interested in works covering the following areas:
• Design, synthesis, and characterization of small molecules as GPCRs modulators;
• Design, synthesis, and characterization of peptides and peptidomimetics as GPCRs modulators;
• Development of chemical probes (i.e., fluorescent tools) to investigate cell signaling mechanisms;
• Development of chemical probes for the high-resolution structural analysis of GPCR complexes;
• GPCRs allosteric modulators;
• Biased GPCR signaling;
This collection of articles would contribute to understanding the molecular mechanism of signal transduction cascade in support of the development of functionally selective therapeutics.
This collection has been generated as part of the
ERNEST COST Action collaboration.
