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 within myotubes and tissues of skeletal muscle from both murines and humans, thus representing a potentially The part played by CB1 receptor activation or inhibition with respect to these functions and relevant The impact of ACEA is inhibited by the selective CB1 receptor antagonist, rimonabant. and NR4A3 mRNA gene expression; these actions may have possible clinical benefits.

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

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 In this review, we will focus on the evidence for PAR interactions with members of their own family, as well as with other types of receptors.

Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall webworm Hyphantria cunea Background: Insect G protein-coupled receptors (GPCRs) have been identified as a new generation

Endogenous parathyroid hormone (PTH) and PTH-related peptide (PTHrP) bind to the parathyroid hormone receptor distinct signaling and physiological properties: PTH evokes prolonged Gs activation, whereas PTHrP evokes transient The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation A comparison of the PTH-bound and PTHrP-bound structures reveals distinct ligand-receptor interactions computational analyses, provide insights into the unique and complex process of ligand dissociation from the receptor

October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation signaling upon ligand binding occurs solely at the cell surface and that duration of the stimulation is transient 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. This is the case for the parathyroid hormone (PTH) type 1 receptor (PTHR), which engages on sustained

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

Endogenous parathyroid hormone (PTH) and PTH-related peptide (PTHrP) bind to the parathyroid hormone receptor distinct signaling and physiological properties: PTH evokes prolonged Gs activation, whereas PTHrP evokes transient The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation A comparison of the PTH-bound and PTHrP-bound structures reveals distinct ligand-receptor interactions computational analyses, provide insights into the unique and complex process of ligand dissociation from the receptor

all these situations, chemokines interact with seven-transmembrane chemokine-type G protein-coupled receptors 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 M, et al. 2023). To comprehensively elucidate the role of scavenging in normal physiology and the potential implications

August 2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous ligand CX3CL1, which shows notable potential as a therapeutic target in atherosclerosis, cancer, and Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field of vision of

August 2022 "The calcium-permeable cation channel TRPM3 can be activated by heat and the endogenous steroid However, the channel is expressed in various tissues and cell types including neurons as well as glial However, a clear picture is needed to unravel TRPM3's full potential as experimental tool, diagnostic

2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid receptor naloxone from an inhibitor directly into an agonist of MOR, and I322A also significantly attenuated the potency

Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial Mode – from CRS1 to CRS3 Chemokines possess a conserved tertiary structure known as the interleukin 8- The spacing between the cysteine residues in the N-loop determines the subfamily-specific arrangement one specific subfamily. which displays a significantly smaller outward tilt of TM6, and instead TM7 and the intracellular helix 8

October 2022 "Melanocortin 3 receptor (MC3R) is a G-protein coupled receptor (GPCR) that is defined

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

September 2022 "The complement fragment C5a is one of the most potent proinflammatory glycoproteins 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.

performed both at Sosei Heptares and Glasgow University characterizing the role of the muscarinic M1 receptor in cognitive and neurodegenerative disorders and the potential therapeutic benefit of muscarinic M1

October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system The mGlu5 receptor is a promising target for the treatment of psychiatric and neurodegenerative diseases lead-like compounds were confirmed to bind to the allosteric site with affinities ranging from 0.43 to 8.6

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Quantum Chemical Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR) drug development by displaying subtype selectivity and more specific receptor modulation. Among the allosteric sites known to date, cavities at the receptor-lipid interface represent an uncharacteristic In this work, we analyze interactions in the allosteric sites of the PAR2, C5aR1, and GCGR receptors

Numerous physiological effects of melatonin are mediated via its specific G protein-coupled receptors (GPCRs) named the MT1 receptor, which couples to both Gq and Gi proteins, and the MT2 receptor, which We investigated whether melatonin receptors are expressed on airway smooth muscle; whether they regulate Activation of melatonin MT2 receptors with either pharmacological concentrations of melatonin (10-100 by itself did not induce an initial [Ca2+]i increase and airway contraction, melatonin significantly potentiated

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic analysis and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors Moreover, through systematic survival analysis on OR genes, OR51E1 (mouse Olfr558) was identified as a potential biomarker of unfavorable overall survival, and OR2C1 (mouse Olfr15) was identified as a potential biomarker analysis and review of the genomic and transcriptomic profiles of ORs in glioma, we suggest that ORs are potential

potential target for immunotherapy, which is reflected on the amount of ongoing clinical trials (currently Furthermore, both chemokines and receptors can homo- and hetero-oligomerize, impacting receptor/ligand-binding bioavailability, and frequency of administration are particularly rigorous for this class, as the majority of potential Overall, the future potential lies in using different therapeutic modalities to modulate the stromal system in different malignancies is crucial to avoid potential side effects and enhance the efficacy

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors

These dimeric forms, which can either be transient or stable, are believed to influence the function while GLP-1R is also known to heterodimerize with the GIPR in recombinant cell system [8]. both binding affinity and signaling potency. Bouvier, M., Oligomerization of G-protein-coupled transmitter receptors.   Proc Natl Acad Sci U S A, 2012. 109 (45): p. 18607-12. 8.         

September 2022 "Introduction Protease activated receptors 1 (PAR1) and 4 (PAR4) agonists are used to

Tirzepatide's success underscores the potential of designing drugs that selectively target beneficial for cAMP production at the GLP-1R which minimal ability to recruit β-arrestins, relative to GLP-1 [8- obesity market toward $66 billion by 2030 and on track to become one of the most lucrative drug classes, potentially Nat Commun, 2015. 6 : p. 8918. 7.          Endocr Rev, 2023. 44 (3): p. 492-517. 8.