Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in Targeting these receptors preclinically can mitigate pathogenic β-amyloid and tau neurotoxicity whilst accessible summary of the literature on Alzheimer's disease and the therapeutic potential of A1 and A2A receptors Although there are no available medicines targeting these receptors approved for treating dementia, we

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in Targeting these receptors preclinically can mitigate pathogenic β-amyloid and tau neurotoxicity whilst accessible summary of the literature on Alzheimer's disease and the therapeutic potential of A1 and A2A receptors Although there are no available medicines targeting these receptors approved for treating dementia, we

October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though Promising preclinical data support the applicability of CB2 activation in autoimmune and inflammatory

Odorant receptors function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR) family and are the largest known mammalian gene family with around 900 genes. Al 2017) and its activation promotes migration and angiogenesis (Kim S. et. al 2015). The development of antibodies directed towards an OR could either drive receptor inactivation or activation of the receptor to destroy tumor cells or be used in drug delivery.

Glycosylation and sulfation – N-terminal PTMs on chemokine receptors The interaction of chemokine receptors (CRS2), which will trigger conformational changes that ultimately lead to receptor activation (Scholten Other examples of O-glycosylation impact on chemokine receptors include the viral receptor US28 (Bagdonaite The atypical chemokine receptor 2 (ACKR2), US28 and sphingosine-1-phosphate receptor 1 (S1PR1) also carry endogenously together with relevant enzymes and co-receptor systems.

Biased agonism is a phenomenon where different ligands acting on the same receptor trigger distinct signaling receptors (GPCRs) like the glucagon-like peptide-1 receptor (GLP-1R). Additionally, GLP-1R couple to G protein-coupled receptor kinases (GRKs) and recruit β-arrestins, adding In contrast, ligands like oxyntomodulin that preferentially activate ERK1/2 signaling interact more significantly McNeill, S.M., et al., The role of G protein-coupled receptor kinases in GLP-1R β-arrestin recruitment

Lysophosphatidic acids (LPAs) are bioactive phospholipids implicated in a wide range of cellular activities They recognize two types of G protein-coupled receptors (LPARs): LPA1-3 receptors and LPA4-6 receptors This article provides an extensive review on the current status of ligand development targeting LPA receptors

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs The experimental structure of these receptors has yet to be determined, and key-residues controlling

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

G protein-coupled receptors (GPCRs) are membrane-bound proteins that sense external stimuli and relay homeostasis and metabolism, and they are activated by peptide hormones [5]. This dimerization allows the N-terminal activation domain of the receptor to repeatedly engage and disengage As a result, dimerized SecR receptors exhibit higher rates of G protein activation and release, improving determine activation.  

August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational Here, we investigated this issue in living cells for the CC chemokine receptor 5 (CCR5), a major receptor in inflammation and the principal entry co-receptor for Human Immunodeficiency Viruses type 1 (HIV-1 We used TIRF microscopy and a statistical method to track and classify the motion of different receptor These results suggest a link between receptor activation and immobilization.

October 2022 "CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), Numerous intracellular mediators are activated by these G protein-coupled receptors based on several factors, including the nature of the ligand, its concentration, and the binding sites with the receptor , levels of the receptor, cell type, and stimulatory environment. Much focus is currently being directed towards CXCR1/2 inhibitors, as these receptors primarily induce

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). FSHR is involved in reproductive processes such as gonadal development and maturation. site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors These models provide insights into the interface, important side-chain interactions, and activation mechanism

August 2022 "Host response to infection involves the activation of the complement system leading to the Complement factor C5a exerts its effect through the activation of C5aR1, chemotactic receptor 1, and into the activation mechanism of this distinct receptor. By comparing two C5aR receptors C5aR1 and C5aR2 we explained differences between their signaling pathways A comparison of microsecond MD trajectories started from active and inactive C5aR1 receptor conformations

August 2022 "CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), Numerous intracellular mediators are activated by these G protein-coupled receptors based on several factors, including the nature of the ligand, its concentration, and the binding sites with the receptor , levels of the receptor, cell type, and stimulatory environment. Much focus is currently being directed towards CXCR1/2 inhibitors, as these receptors primarily induce

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide range of physiological processes. 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.

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.

order to avoid a prolonged pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR) has to be rapidly terminated. Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination The medium chain fatty acid receptor GPR84 as well as formyl peptide receptor 2 (FPR2), receptors expressed

October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by Once activated, PAR2 is rapidly desensitized and internalized by phosphorylation and β-arrestin recruitment Due to its irreversible activation mechanism, some agonists that rapidly desensitized PAR2 have been Activation of PAR2 by GB83 markedly elicited an increase in intracellular calcium levels and phosphorylation Interestingly, unlike PAR2-AP, GB83 and trypsin induced sustained receptor endocytosis and PAR2 colocalization

August 2022 "Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types.

August 2022 "Abstract Chemokines such as stromal derived factor 1 and their G protein coupled receptors through any of the known mammalian G α isoforms and have generated a comprehensive map of the G α activation mutations, we studied the molecular characteristics that determine the ability of small molecules to activate in the CXCL12/CXCR4/ACKR3-signaling axis and better understand the structural determinants for ACKR3 activation SIGNIFICANCE STATEMENT: We are interested in the signaling produced by the G protein coupled receptor

September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled Here, we show that a combination of insulin and the GPCR agonist neurotensin induced rapid activation PANC-1 cells, as shown by FAK phosphorylation at Tyr576/577 and Tyr861, sensitive biomarkers of SFK activity Dasatinib-induced ERK activation was completely abolished by exposure to the FDA-approved MEK inhibitor

Rho1 signaling is activated by G-protein-coupled receptor (GPCR) signaling at the cell surface. During Drosophila embryonic salivary gland (SG) invagination, the GPCR ligand Folded gastrulation (Fog) activates The SG receptor that transduces the Fog signal into Rho1-dependent myosin activation has not been identified , we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin activation unexpected Fog-independent roles for Smog in maintaining epithelial integrity and organizing cortical actin

October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric modulation in angiotensin receptors: IUPHAR Review 34 "Functional advances have guided our knowledge Thus, we need to know much more about the structures of receptor-ligand complexes at high resolution. Recently, X-ray structures of both AngII receptors (AT1 and AT2 receptors) bound to peptide and non-peptide , as the basis of ligand selectivity, efficacy, and regulation of the molecular functions of the receptors

September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system effects of CB2 receptor activation, make this receptor an intriguing target for treating schizophrenia , has greatly advanced our understanding of this receptor. located in schizophrenia-relevant circuits, where the physiological consequence of CB2 receptor activation

September 2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid receptor (MOR), whereas naloxone, with only slight structural changes compared to morphine, To validate these processes, we employed GIRK4S143T, a MOR-activated Gβγ-protein effector, in combination residue I322, which leads to differential recognition of morphine and naloxone while assisting EM-1 in activating

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Many cause receptor misfolding and failure to reach the cell surface. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone receptors