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October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance to initiate downstream effector signaling. This review aims to explore the signaling pathways, dynamic structures, and physiological relevance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins is increasing appreciation for the elegance of the regulatory mechanisms that mediate intracellular signaling

October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors (GPCRs) that act in an allosteric manner to modulate the activity of GPCRs. This review will focus in particular on pepducins designed from protease-activated receptors, C-X-C motif chemokine receptors, formyl peptide receptors, and the β2-adrenergic receptor. , signaling, pathophysiologic consequences, and therapeutic potential for each pepducin class."

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR ) signaling pathway because of its quantifiable stimulus, non-redundancy of genes, and immense importance published cryo-electron tomography (cryo-ET) data on the ROS with structural knowledge on individual proteins maintaining the spacing between ROS discs, suggesting a plausible mechanism by which intrinsic optical signals

October 2022 "Enzymatic and cellular signalling biosensors are used to decipher the activities of complex Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Their applications have continually expanded our understanding of this important protein class. briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling signalling complexes."

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer Information flow from a source to a receiver becomes informative when the recipient can process the signal are responsible for signal recognition at the membrane level and information transduction inside the The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 genes coding for these proteins.

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors In all cases, the receptor interaction changes downstream signalling and the responses to receptor agonists This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs, and explores the physiological consequences of GHSR1a coupling with other GPCRs.

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane protein-coupled receptor (GPCR) drug development by displaying subtype selectivity and more specific receptor modulation. Among the allosteric sites known to date, cavities at the receptor-lipid interface represent an uncharacteristic In this work, we analyze interactions in the allosteric sites of the PAR2, C5aR1, and GCGR receptors

Most acquired genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors (vGPCRs), chemokines, and chemokine-binding proteins. These include receptors from human cytomegalovirus, which encodes four vGPCRs: US27, US28, UL33, and We discuss ligand binding, signaling, and structures of the vGPCRs in light of robust differences from endogenous receptors.

counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical on the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling."

Historically, ligands for GPCRs have been identified before their receptor counterparts. With the cloning revolution, several unidentified receptors have been found and were labelled as “orphan GPR84 is a Gi‐coupled class A GPCR mainly expressed in immune cells and microglia in the brain (Wojciechowicz and 2. which ligands can be used as tool compounds to study the function and biology of this receptor CXCR2 and the adenosine A3 receptor (Gaidarov et al., 2018).

The transport proteins that facilitate this process are classified as pump-like flippases and floppases Unexpectedly, Class A G protein-coupled receptors (GPCRs), a large class of signaling proteins exemplified by the visual receptor rhodopsin and its apoprotein opsin, are constitutively active as scramblases Conformational changes that facilitate scrambling are distinct from those associated with GPCR signaling

Calcium (Ca2+) signaling is known to direct processes that govern chondrocyte gene expression, protein Synthetic signaling platforms permitting precise and selective Ca2+ signal transduction can improve dissection One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs dynamics, proliferation, and protein deposition in 2D ATDC5 cultures. This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide Recently, AlphaFold2 has been developed to predict structure models of many functionally important proteins We revealed that AlphaFold2 could capture the overall backbone features of the receptors.

Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes: Impact of ligand type and receptor activation state G protein-coupled receptors (GPCR) are the largest family of cell surface receptors in vertebrates. Their abundance and role in nearly all physiological systems make GPCR the largest protein family targeted Receptor conformational sampling in advance of docking or receptor conformational adjustment after docking

August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein Coupled Receptors (GPCRs). GPR21 couples to the Gq family of G proteins and is expressed in macrophages. GPR21 expression was evaluated at gene and protein level, the signalling pathway was investigated by

September 2022 "Sound is converted by hair cells in the cochlea into electrical signals, which are transmitted G protein-coupled receptors (GPCRs) are crucial receptors that regulate a wide range of physiological And A1, A2A, and CB2 activation by agonists has protective functions on noise- or drug-induced hearing and discuss the role of GPCR in the cochlea, such as stem cell fate, PCP, hearing loss, and hearing protection

October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance to the field of cardiovascular medicine due to the critical physiological roles of these receptors and Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new rapidly due to their biochemical tractability and their ability to recognize defined states of native proteins Here, we review how nanobodies have been adopted to elucidate the structure, pharmacology, and signaling

protein-coupled receptors (GPCRs) in complex with G proteins or arrestins. However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack strategy has the potential to broadly facilitate cryo-EM structure determination of GPCRs alone without signaling protein, the critical determinants that make this approach successful are not yet clear. of antagonist bound A2A adenosine receptor at 3.4 Å resolution and unliganded Smoothened at 3.7 Å resolution

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the fine-tuning of Gi/o signaling "Aims: Cardiac contractility, essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled receptor (GPCR) signaling. Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early (Daphnia magna) reveals a high level of orthological relationship of amine, neuropeptide, and opsin receptor repertoire, while purinergic and chemokine receptors were highly differentiated in humans.

Despite this, the prognosis remains poor, with an impacted quality of life during treatment coupled with In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets. To date, the most promising targets are the chemokine, cannabinoid, and dopamine receptors, but future work should further examine the melanocortin receptor-4 (MC4R), adhesion, lysophosphatidic acid (LPA ) and smoothened (Smo) receptors to initiate new drug-screening strategies and targeted delivery of safe

November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures These structures have been studied by protein mapping using the FTMap server, which determines the clustering of small organic probe molecules distributed on the protein surface. Mapping of Alphafold2 generated models of these proteins confirms that the same sites can be identified These sites cluster at nine distinct locations, and each can be found in many different proteins.

October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system The mGlu5 receptor is a promising target for the treatment of psychiatric and neurodegenerative diseases compounds with the highest affinities were demonstrated to be negative allosteric modulators of mGlu5 signaling

August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing levels of selectivity and affinity as GPR84 antagonists. Although blockade of GPR84 may potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation of metabolism or energy sensing is compromised. Here, we consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural information, recent developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field of vision of

August 2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous correlate with three cholesterol molecules that play essential roles in conformation stabilization and signaling Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor ) signaling and provide insights into the diversity of G protein coupling."

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein protein signaling. consequences of selective elimination of GPR3-mediated β-arrestin signaling in vivo. We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease Collectively, these studies indicate that GPR3-mediated G protein and β-arrestin signaling produce discrete

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental G protein-coupled receptors, the largest family of membrane proteins in eukaryotes and the largest drug Among them, the secretin/adhesion (Class B) G protein-coupled receptors are essential drug targets for Given the great value of the secretin/adhesion (Class B) G protein-coupled receptors in the regulation of cardiovascular system function and the drug target exploration, we summarize the role of these receptors