G Protein-Coupled Receptors: Molecular Mechanisms Involved in Receptor Activation and Selectivity

Dear Colleagues,

G Protein-Coupled Receptors (GPCRs) are seven-transmembrane receptors that upon activation predominately transduce their signals through the alpha subunits of heterotrimeric G proteins. GPCRs are present in all cell types and regulate a plethora of physiological functions, whose alterations lead to a pathogenic readout.

Many GPCRs show basal activity that can be modulated by ligands with different efficacy. Full agonists are able to induce the maximal signaling response, while some ligands, known as biased ligands, selectively activate certain receptor-associated pathways at the expense of others. The interaction of GPCRs with extracellular ligands induces an extremely variable response due to the distinct distribution of active conformations of these receptors. Ligand binding and downstream signaling have also been shown to be influenced by the dimeric nature of the receptors.

This Special Issue aims at presenting novel data focused on biochemical, pharmacological, and structural evidence regarding the molecular mechanisms of GPCR activation, whose understanding is crucial to design new highly specific drugs with reduced side effects.

Dr. Rossella Miele
Dr. Roberta Lattanzi
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Life is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2600 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.