G-Protein-Coupled Receptors (GPCRs)

Dear Colleagues,

G-protein-coupled receptors (GPCRs) are the cell surface protein that constitute the largest family in the human genome (>800gene), and are involved in a wide variety of function in the peripheral and central system. GPCRs, primarily confined within the plasma membrane, and their structural findings revealed that they consist of seven transmembrane-spanning α-helix domains linked by three altering intracellular and extracellular loops and N- and C-terminals. GPCRs have the ability to bind or are activated by multiple ligands, including hormones, photons, ions, neurotransmitters, odorants, peptides, and light, and are involved in the regulation of multiple signaling pathways. The majority of transduction events in cells are under the influence of GPCRs, which is a testament to their significance as a major target of therapeutic drug discovery; at present, >40% of therapeutic drugs represent GPCR, worth an estimated >$850 billion. In the last two decades, our understanding regarding GPCRs’ functionality and pharmacology has significantly changed. The concept that GPCRs exist and function in a monomeric entity has been rephrased, and growing pharmacological, biochemical, and biophysical evidence supports that GPCRs form functionally active homo- and hetero-dimers, even a higher order of oligomers, and modulate pharmacological properties and receptor mediated regulation of downstream signaling pathways that are different from the native receptor. Despite recent progress in the field of GPCRs, the structure biology of these surface proteins is poorly understood; however, functional interactions between different GPCRs, including adrenergic, cannabinoid, GABA, dopamine, opioid, and somatostatin receptor subtypes are now well established.

As Guest Editor, I invite submission of manuscripts dealing with different aspects of GPCRs for publication in this Special Issue of Biomedicine.

Prof. Ujendra Kumar
Guest Editor

Manuscript Submission Information

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• agonist
• dimerization
• G-proteins
• receptor coupling
• G-protein-coupled receptor kinases
• G-protein-coupled receptors
• internalization
• ligand binding
• monomers
• pharmacology phosphorylation
• signaling pathways