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 In recent years, the LPA signaling pathway has captured an increasing amount of attention because of This article provides an extensive review on the current status of ligand development targeting LPA receptors to modulate LPA signaling and their therapeutic potential in various diseases.

all these situations, chemokines interact with seven-transmembrane chemokine-type G protein-coupled receptors (chemokine receptors, CKRs) and glycosaminoglycans (GAGs) to regulate the movement of leukocytes throughout In humans there are approximately 45 chemokines, 19 chemotactic or G-protein coupled chemokine receptors (CKRs) that signal via Gαi and 4 official atypical chemokine receptors (ACKRs) which engage in ligand CCR2 is an example of a dual-function receptor that directly regulates both cell migration and scavenging

The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors Several S1PR therapeutic drugs have been developed to treat these diseases; however, they lack receptor In this article, we describe a 2.2 Å resolution room temperature crystal structure of the human S1P5 receptor demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies the receptor

influence predominantly arises via engagement with the principal two G-protein-coupled cannabinoid receptors Earlier publications have indicated that expression of CB1 receptor mRNA and protein has been recognized The part played by CB1 receptor activation or inhibition with respect to these functions and relevant This can be deduced from the qRT-PCR assays; triggering CB1 receptors amplifies both NR4A1 and NR4A3 The impact of ACEA is inhibited by the selective CB1 receptor antagonist, rimonabant.

Several neurotransmitters and neuromodulators, acting through G-protein-coupled receptors (GPCRs), fine-tune MN IME was also augmented by the physiological neuromodulator lysophosphatidic acid (LPA) through a mechanism These outcomes suggest that LPA and several neurotransmitters impact MN IME via Gαi/o/Gαq-protein-coupled receptors, downstream ROCK2 activation, and subsequent inhibition of TASK1 channels.

September 2022 "Serotonin receptor 5-HT2A and tropomyosin receptor kinase B (TrkB) strongly contribute decreased TrkB autophosphorylation, preventing its activation with agonist 7,8-DHF, even with low 5-HT2A receptor A blockade of 5-HT2A receptor with the preferential antagonist ketanserin prevented the receptor-mediated Our data reveal the functional role of 5-HT2A–TrkB receptor heterodimerization and suggest that the regulated

Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial chemokine system exhibits great versatility, with more than 50 chemokines interacting with over 20 receptors complexes and revealing the diverse and multifaceted nature of the chemokine receptor system. Currently, there are more than 40 available structures of chemokines and their receptors in the Protein This structural variation may explain why chemokine receptors typically recognize chemokines from only

October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation In this model, GPCR signaling is turned-off by receptor phosphorylation via GPCR kinases (GRKs) and subsequent recruitment of β-arrestins, resulting in receptor internalization into endosomes. Internalized receptors can then recycle back to the cell surface or be trafficked to lysosomes for degradation This is the case for the parathyroid hormone (PTH) type 1 receptor (PTHR), which engages on sustained

The chemokine receptor system is implicated in a wide range of inflammatory, autoimmune and infectious The involvement of chemokines and their receptors in several aspects of cancer biology, represents a This redundancy can be seen as problematic in drug discovery as blocking a single receptor might not Therefore, an alternative approach is to make use of chemokine receptors redundancy and the fact that Furthermore, both chemokines and receptors can homo- and hetero-oligomerize, impacting receptor/ligand-binding

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 "Melanocortin 3 receptor (MC3R) is a G-protein coupled receptor (GPCR) that is defined

October 2022 "Protease activated receptors (PARs) are among the first receptors shown to transactivate other receptors: noticeably, these interactions are not limited to members of the same family, but involve receptors as diverse as receptor kinases, prostanoid receptors, purinergic receptors and ionic channels the evidence for PAR interactions with members of their own family, as well as with other types of receptors pathological relevance of these interactions, since this additional level of molecular cross-talk between receptors

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

Biased agonism is a phenomenon where different ligands acting on the same receptor trigger distinct signaling is gaining significant attention in drug discovery, especially in the context of G protein-coupled 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 For instance, the interaction of GLP-1 with ECL3, which leads to a tight conformation of the receptor's

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

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.

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 of the receptor to destroy tumor cells or be used in drug delivery. The chimeric antigen receptor T cell therapy could also be a way to target tumor cells expressing ectopic

G protein-coupled receptors (GPCRs) are membrane-bound proteins that sense external stimuli and relay from the receptor’s core, which is crucial for G protein recruitment. Bouvier, M., Oligomerization of G-protein-coupled transmitter receptors.   induces G-protein-coupled receptor heteromer formation.   Wootten, D., et al., Allostery and Biased Agonism at Class B G Protein-Coupled Receptors.  

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

August 2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor

performed both at Sosei Heptares and Glasgow University characterizing the role of the muscarinic M1 receptor

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that

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

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

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

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). ACKR3 has been described as an atypical "biased" receptor because it does not appear to signal through atypical chemokine receptor 3 (ACKR3), which signals atypically.

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