September 2022 "GPCR signaling and function depend on their associated proteins and subcellular locations Besides G-proteins and β-arrestins, 14-3-3 proteins participate in GPCR trafficking and signaling, and they connect a large number of diverse proteins to form signaling networks. Multiple 14-3-3 isoforms exist, and a GPCR can differentially interact with different 14-3-3 isoforms

and anosmia, is due to mutations in the ANOS1 gene that encodes for the extracellular matrix (ECM) protein Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled We have previously shown interaction between PKR2 and anosmin 1 in vitro. current report we present evidence of the modulation of PK2/PKR2 activity by anosmin 1, since this protein The whey acidic protein domain (WAP) is necessary for this modulatory activity, although data from GST

C5a is established to interact with a set of genomically related transmembrane receptors, like C5aR1 The C5aR1 is a classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that tailors immune cell activity potentially through β-arrestins rather than G-proteins. In addition, the structure of C5aR2 and its interaction specificity toward C5a is not structurally elucidated dynamics data presented in the current study are expected to further enrich the understanding of C5a-C5aR2 interaction

A Gαs preferentially interacts with dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane are called promising candidates in G protein-coupled receptor (GPCR) drug development by displaying binding location that raises many questions about the ligand interactions and stability, the binding In this work, we analyze interactions in the allosteric sites of the PAR2, C5aR1, and GCGR receptors The availability of polar atoms for interactions in such cavities can be assessed by water molecules

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.

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel This study, published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 During this process, APEX2 can label proteins in the vicinity, allowing the capture of a snapshot of After the labeling reaction, the researchers purified and biotinylated proteins (those that have been this analysis provided insights into the molecular composition of the endosomal environment and the proteins

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor 1a (GHSR1a) is intriguing because of its potential as a therapeutic target and its diverse molecular interactions In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors , serotonin 2C, orexin, oxytocin and melanocortin 3 receptors (MCR3), as well as the MCR3 accessory protein In all cases, the receptor interaction changes downstream signalling and the responses to receptor agonists

October 2022 Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of Adhesion Receptor GPR97 "Adhesion G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play Markov state models revealed that the overall conformation of GPR97 is preferred to be fully active when interacting with palmitoylated Go protein. network analysis suggests that the palmitoylation of Go not only allosterically strengthens the internal interactions

October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular

cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G 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 In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly Here, we address this shortcoming by exploring different fusion protein designs, which lead to structures

October 2022 "Background: Uncoupling proteins (UCPs) are unpaired electron carriers that uncouple oxygen hypothesised to be triggered by superoxide and then reduce mitochondrial free radical production, potentially protecting Objectives: The objectives of the study are to find out the newest ways to treat diabetes mellitus through protein

October 2022 Design and validation of recombinant protein standards for quantitative Western blot analysis radioligand binding methods "Background: Replacement of radioligand binding assays with antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR) levels requires the use of purified protein standards containing the antigen. Results: Here we generated highly soluble and stable recombinant protein constructs GST-CB1414-472 and

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 transmembrane domains, the shape of the ligand-binding pockets, and the conformation of the transducer-binding interfaces

Most acquired genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors (vGPCRs), chemokines, and chemokine-binding proteins.

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte Cardiac contractility, essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause G protein dysregulation, contributing to modest blood pressure elevation and exaggerated cardiac hypertrophic Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in One candidate effector of PKA-dependent transcriptional regulation is the BET protein Brd4. However, it is unknown whether BET proteins, or Brd4 specifically, are involved in transcriptional activation Here, we demonstrate that in adult rats, inhibition of BET proteins with the bromodomain inhibitor JQ1 Our findings identify the BET protein family, and Brd4 in particular, as novel regulators of basal and

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous GPR15L(71-81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling using a G protein activation assay and second messenger assay conducted on living cells.

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 genes coding for these proteins. The recognition that GPCRs may physically interact with each other has led to the hypothesis that their

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein behavior, reduced fertility, and memory impairment, which are potentially associated with impaired G protein In contrast to Gpr3-deficient mice, G protein-biased GPR3 mice do not display elevated anxiety levels We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease glial response that may limit amyloid plaque development in G protein-biased GPR3 AD mice.

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR published cryo-electron tomography (cryo-ET) data on the ROS with structural knowledge on individual proteins

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its N-terminal fragment 1 to 36 "The parathyroid hormone (PTH)-related protein (PTHrP) is indispensable amino acids, our current understanding on how endogenous PTHrP transduces signals through its cognate G-protein production, acute intracellular Ca2+ (iCa2+) release and β-arrestin recruitment mediated by ligand-PTHR interactions together, our results contribute to a better understanding of the biased signaling process of a native protein

Regulator G protein Signaling (RGS) proteins are critical components of the intracellular signaling pathways Role of RGS proteins in regulating GPCR signaling: Recent studies have revealed that the interaction The interaction between RGS proteins and GPCRs is highly specific and tightly regulated; mutations in domain and other structural motifs have been shown to alter the specificity and potency of the RGS-GPCR interaction For example, μ opioid receptor (MOR) interacts with Gαi/o and Gαz subunits, which have a slow enzymatic

August 2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Recent studies showed that some AVPR2 mutations could cause biased Gαq/11 protein coupling rather than In this study, R68W and V162A were analyzed to whether they show a bias to Gαs or Gαq/11 proteins. R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor.

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance their function and mechanism of action, there is a greater understanding of how effector molecules interact in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins We will first summarize their prominent roles in GPCR pharmacology before transitioning into less well-explored

September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor Cryo-electron microscopy studies revealed a drastic conformational change upon activation and a unique G protein We find that the inactive GP first interacts with TM3, which further leads to the TMD rearrangement and

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

October 2022 Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu5a receptor internalization "The internalization of G protein-coupled GPCR kinase 2 and 3 (GRK2 and GRK3) KO cells, and a receptor containing a mutated putative adaptor protein complex 2 (AP-2) interaction motif, we demonstrate that internalization of rat mGlu5a is mediated by Gαq/11 proteins (77% of the response), GRK2 (27%), and AP-2 (29%), but not GRK3.