GPR84 has been additionally proposed to be a potential biomarker in different inflammatory diseases ( towards clinical validation, as well as radiopharmaceuticals, including potential PET ligands, and suitable CXCR2 and the adenosine A3 receptor (Gaidarov et al., 2018). From these series of compounds, GLPG1205 progressed into clinical development for the potential treatment investment in better tools to study its function in both disease and physiological settings will likely potentiate

September 2022 "The G-protein-coupled bile acid receptor, Gpbar1 or TGR5, is characterized as a membrane receptor specifically activated by bile acids. and activator of transcription 3 (STAT3), cyclic adenosine monophosphate (cAMP), Ras homolog family member A (RhoA), exchange protein activated by cAMP (Epac), and transient receptor potential ankyrin subtype

October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz Previous assays verified that a typical G protein-coupled receptor, β-adrenergic-like octopamine receptor

September 2022 Sweet taste receptor agonists attenuate macrophage IL‐1β expression and eosinophilic inflammation eosinophilic CRS (ECRS) via macrophage IL‐1β overproduction, thereby suggesting autophagy regulation as a potential We sought to investigate the therapeutic potential of autophagy‐enhancing agent, trehalose, or related were assessed using specific inhibitor, genetic knockdown or knockout, and overexpression of cognate receptors

pre-association enables β-arrestin to explore its surroundings through lateral diffusion and engage in highly transient Transient interaction with the receptor catalyzes β-arrestin activation, including β-arrestin inter-domain M., Medel-Lacruz, B., Baidya, M., Makarova, M., Mistry, R., Goulding, J., Drube, J., Hoffmann, C., Owen M., Kawakami, K., Masureel, M., Maeda, S., Garcia, K. C., von Zastrow, M., Inoue, A., & Kobilka, B. Pharmacology & therapeutics, 89(2), 139–147. https://doi.org/10.1016/s0163-7258(00)00107-8

August 2022 "Abstract The β3 -adrenergic receptor (β3 -AR) is found in several tissues such as adipose Out of 35 tested compounds, 4 compounds were active in CHO-K1 cells expressing the human β3 -AR, and 8

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance With continued study of their function and mechanism of action, there is a greater understanding of how effector molecules interact with a receptor to initiate downstream effector signaling. We will first summarize their prominent roles in GPCR pharmacology before transitioning into less well-explored

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. tools and drug leads is aided by molecular docking simulations that allow critical analysis of the potential Receptor conformational sampling in advance of docking or receptor conformational adjustment after docking

September 2022 "Given the promising clinical value of allosteric modulators of G protein-coupled-receptors Here, we report the crystallographic and cryo-electron microscopy structures of the cannabinoid receptor ZCZ011 exerts a PAM effect by promoting TM2 rearrangement in favor of receptor activation and increasing the population of receptors that adopt an active conformation. Our findings fill a gap in the understanding of CB1 allosteric regulation and could guide the rational

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in the human body, are plentiful and vary in utility, form and function. briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric

Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled receptors (GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations in the PK2 and PKR2 genes are involved could assist the WAP domain both in the binding to PKR2 and in the modulation of the activation of the receptor

transport proteins that facilitate this process are classified as pump-like flippases and floppases and channel-like 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 Atomistic molecular dynamics simulations of opsin in a lipid membrane reveal conformational transitions

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR Although hypothetical, the reconstruction of the rod phototransduction system highlights the potential

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, behavior, and neurophysiology "The awareness of the potential importance of functional selectivity/biased A major pan-receptor focus has been to identify GPCR-selective ligands that have bias in G protein-dependent the past two decades, it is only recently that highly β-arrestin biased ligands for the dopamine D1 receptor

affect processes related to perception, cognition and sensory processing mostly via the serotonin 5-HT2A receptor amphetamine 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), is receiving renewed attention for their potential Current studies focused on the potentially clinical effects of psychedelics on human subjects tend to tested the effects of DOI on head-twitch behavior (HTR) - a mouse behavioral proxy of human psychedelic potential

August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic Therefore, S1R ligands possess a variety of potential clinical applications with a great interest in We have explored hydrophobic groups of different sizes on both sides of the five-membered ring scaffold Upon optimization, this series of compounds could represent potential clinically useful S1R ligands for

September 2022 β2-Adrenergic Receptor Expression and Intracellular Signaling in B Cells Are Highly Dynamic In the past, treatment of arthritic B cells with a β2-adrenergic receptor (β2-ADR) agonist has been shown Adrenergic receptors on B cells and intracellular β2-ADR downstream molecules (G protein-coupled receptor agonist terbutaline by flow cytometry. β2-ADR-expressing B cells increase during CIA without a change in receptor during sustained inflammation might be an integral part of the switch from pro- to anti-inflammatory action

amplification and compartmentalization in T cell activation, focusing on the role of CD28, chemokine receptors

Class B G protein-coupled receptors (GPCRs) are notoriously difficult to target by small molecules because Using the parathyroid hormone type 1 receptor (PTHR) as a prototypic class B GPCR target, and a combination Here we found a key mechanical site that modulates the collective dynamics of the receptor and used this molecules with strong negative allosteric and biased properties for PTHR signaling in cell and PTH actions

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

August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) A variety of ligands for CB1 receptors have been developed as promising drug candidates for the treatment New high-resolution structures of CB1 receptor in different functional states have significantly improved In this review, we describe the structural determinants for modulation of CB1 receptors by different types of ligands, as well as the differences between CB1 and its homologous, the CB2 receptor.

November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies Using a co-immunoimmobilization assay, we found that transient β2-AR dimers exist in a resting state,

The binding pockets for serotonin were virtually identical between the receptor-Gs and receptor-Gi complexes The structural differences found between the receptor-Gs and receptor-Gi complexes evidenced that 5-HT4 Interestingly, in the case of promiscuous receptors they found that these receptors shared conserved These findings contribute to progress in understanding how serotonin receptors, one of the largest subfamilies of class A GPCRs and potential therapeutic targets that are activated by the same endogenous ligand,

G protein-coupled receptors (GPCRs) are crucial receptors that regulate a wide range of physiological

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

One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs We previously demonstrated hM3Dq's ability to precisely and synthetically initiate robust [Ca2+]i transients This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, GPR110 belongs to adhesion GPCR and was the functional receptor of N-docosahexaenoyl ethanolamine (also Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand

August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein Coupled Receptors (GPCRs).