October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid The primary analgesic target of opioids is the μ-opioid receptor (MOR). found that MOR alone could not stimulate PLC, but rather required a coincident signal from a Gq coupled receptor

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though

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

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. Physiological functions of ectopically expressed olfactory receptors ORs participate in important cellular odorant delivery would be required where selectivity must be carefully evaluated as odoronts tend to bind of the receptor to destroy tumor cells or be used in drug delivery.

August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors report the structure-based development of fluorescent ligands targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor 2 (CCR2), a class A GPCR that has been pursued as a drug target ligands were designed, synthesized, and tested for their suitability as fluorescent reporters to probe binding we developed 14 as a fluorescent CCR2 ligand, enabling cell-free as well as cellular NanoBRET-based binding

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor , GHSR1a The growth hormone secretagogue receptor 1a (GHSR1a) is intriguing because of its potential Initial studies of the receptor focused on the potential therapeutic ability for growth hormone (GH) (GPCRs), including dopamine D1 and D2, serotonin 2C, orexin, oxytocin and melanocortin 3 receptors ( In all cases, the receptor interaction changes downstream signalling and the responses to receptor agonists

These studies also show that disrupting the dimerization of GLP-1R results in decreased high-affinity binding both binding affinity and signaling potency. function, ligand binding, and downstream signaling. Harikumar, K.G., et al., Impact of secretin receptor homo-dimerization on natural ligand binding.   induces G-protein-coupled receptor heteromer formation.  

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. Using fluorescently tagged histamine, we explored H2R-histamine binding interaction, which exhibits a

October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inverse agonism "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various

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.

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). Structurally, the extensive extracellular domain, which contains the hormone-binding site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors. How this HR is involved in hormone binding and signal transduction is still an open question.

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

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

September 2022 To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from inactive conformation using molecular dynamic simulations "The δ-opioid receptor (DOR) is a critical While the receptor with the crystal ligand (i.e. antagonist naltrindole) maintained the inactive conformation in all three independent simulations, the receptor with ADL5859 was adopting toward the active conformation

Complement factor C5a exerts its effect through the activation of C5aR1, chemotactic receptor 1, and the C5aR1-G protein complex has provided new insights 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

We find that PFC astrocytes express receptors for dopamine but are unresponsive through the Gs/Gi-cAMP calcium signals in PFC astrocytes are time locked to dopamine release and are mediated by α1-adrenergic receptors active players in dopaminergic signaling in the PFC, contributing to PFC function though neuromodulator receptor

August 2022 "Abstract Chemokines such as stromal derived factor 1 and their G protein coupled receptors C-X-C motif chemokine ligand 12 (CXCL12) has two receptors: C-X-C chemokine motif receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3). , revealing a key role for the deeper binding pocket composed of residues in the transmembrane domains atypical chemokine receptor 3 (ACKR3), which signals atypically.

Crystal structures suggest ligand access to the orthosteric binding site of MT1 and MT2 receptors through entry route for 2-iodomelatonin, a nonselective agonist with a slower dissociation rate from the MT2 receptor The side-chain flexibility of Tyr5.38 was significantly different in the two receptor subtypes, as assessed consistent with the possibility that the gap between TM IV and V is a way of connecting the orthosteric binding site and the membrane core for lipophilic melatonin receptor ligands.

Divergence, however, in the amino acid sequences of rodent and human PTH receptors (rat and mouse PTH1Rs are 91% identical to the human PTH1R) can lead to differences in receptor-binding and signaling potencies

with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find

September 2022 Identification and functional characterization of the sulfakinin and sulfakinin receptor processes and physiological functions in invertebrates through the interaction with G-protein-coupled 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 Recent anatomical studies, combined with electrophysiological studies, indicate that CB2 receptors are effects of CB2 receptor activation, make this receptor an intriguing target for treating schizophrenia , has greatly advanced our understanding of this receptor.

Involvement of various chemokine/chemokine receptor axes in trafficking and oriented locomotion of mesenchymal Chemokines are low molecular weight proteins that their functional activities are achieved by binding to the cell surface G protein-coupled receptors (GPCRs). Chemokine and chemokine receptors are of the most important and effective molecules in MSC trafficking Chemokine/chemokine receptor axes play a pivotal role in the recruitment and oriented trafficking of

2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid receptor agonist of MOR, and I322A also significantly attenuated the potency of MOR on EM-1, confirming that binding This finding reveals a dynamic mechanism for the response of MOR to different ligands and provides a

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer complex organisms, cell to cell communication occurs mostly through neurotransmitters and hormones, and receptors The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 evidence that supports these conjectures, fostering new ideas about the physiological role played by receptor

September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous carcinoma: an emerging prognostic indicator and future therapeutic target " Purpose: Beta 2-Adrenergic Receptor

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 GPCR (Sharman et al., 2011), although it is widely accepted that medium‐chain fatty acids (MCFAs) can bind to and activate this receptor with modest potency. CXCR2 and the adenosine A3 receptor (Gaidarov et al., 2018).

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 These findings aid in advancing the understanding of the effects of genetic mutations on GPCR function