Research Topic

Molecular Modulators of GPCRs signal transduction

About this Research Topic

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 signalling.
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 signalling 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.


Keywords: GPCRs, chemical probes, small molecules, peptides, GPCRs-complexes, biased signal


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.

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 signalling.
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 signalling 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.


Keywords: GPCRs, chemical probes, small molecules, peptides, GPCRs-complexes, biased signal


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.

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Submission Deadlines

28 February 2021 Abstract
30 September 2021 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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Topic Editors

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Submission Deadlines

28 February 2021 Abstract
30 September 2021 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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