Here we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone Seventeen FSHR mutations described in patients with reproductive dysfunction were expressed in HEK 293T reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% to 84% of WT for 4, and not reduced for 2. expression, restoration to ≥57% of WT levels was achieved for 6 by treatment with 1 µM CAN1404 for 24

September 2022 "In the Wnt-β-catenin pathway, Wnt binding to Frizzled (Fzd) and LRP5 or LRP6 (LRP5/6) Using purified Fzd proteins reconstituted in lipid nanodiscs, we investigated the factors that promote Our findings suggest a positive feedback loop in which Wnt-stimulated local PI(4,5)P2 production enhances

We found that astrocyte Gi -DREADD stimulation using clozapine N-oxide (CNO) inhibits neuroinflammation Subsequent experiments using primary astrocyte cultures revealed that Gi -DREADD stimulation significantly

September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent ROCK and Phosphorylation of Smad2L "In addition to the carboxy region, Smad2 transcription factor can western blotting using protein-specific antibodies against phospho-Smad2 linker region residues (Ser245/250 /255),<br />phospho-Smad2 carboxy residues (465/467), ERK1/(Thr202/Thr204), and PAI-1. <br /><strong>Results:</strong> TGF (2 ng/ml), EGF (100 ng/ml) and ET-1 (100 nM) induced the phosphorylation

We uncovered a novel neuroprotective mechanism involving interaction between neurotrophic factor-α1 ( Treatment of 5-HTR1E stable cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented

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

September 2022 "Experimental studies proposed a direct effect of follicle-stimulating hormone (FSH) on

September 2022 " Background: Colorectal cancer is the third most common cancer and requires more prognostic The clinical significance of GPR39 in colon cancer has never been reported. Materials: In our study, we compared GPR39 expression between colon cancers and tumor-adjacent tissues by retrieving TCGA data and detected the expression of GPR39 in colon cancers with qPCR and immunohistochemistry clinical significance of GPR39 was evaluated by analyzing the correlations with clinicopathological factors

October 2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards more GLP-1 receptor interaction "Background and purpose: To fully elucidate the regulatory role of the GLP-2 system in the gut and the bones, potent and selective GLP -2 receptor (GLP-2R) antagonists are needed. or competition binding using 125 I-GLP-2(1-33)[M10Y].

September 2022 "Evaluation of stimulus salience is critical for any higher organism, as it allows for The paraventricular nucleus of the thalamus (PVT) has recently been identified as an integrator of stimulus Here we report that neuropeptide S (NPS) signaling in the PVT is necessary for stimulus salience encoding The PVT appears to provide stimulus salience encoding in a dose- and NPS-dependent manner. Overall, these results demonstrate that stimulus salience encoding is critically associated with NPS

GPCR Activation and Signaling Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion Internal and external modulation factors of the orexin system (REVIEW). Structure-based pharmacophore modeling 2. (July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Retreat (November 2 - 4, 2023) Registration

August 2022 "The X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism 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 in the pathogenesis of KS. of PK2/PKR2 activity by anosmin 1, since this protein is able to enhance the activation of the ERK1/2 (extracellular signal-regulated kinase 1/2) pathway elicited by PK2 through PKR2.

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

to 25, 2024. Let’s dive into the Classified GPCR News from May 27th to June 2nd, 2024. inverse agonist improves lung functioning in preclinical asthma GPCR Events, Meetings, and Webinars June 2 Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 23 - 25, 2024 | 11th Adhesion GPCR Workshop July

Save the dates: November 2 - 4: We're sponsoring the GPCR Retreat and would love to meet you there! - 27, 2023 | 3rd Annual Meeting IRN I-GPCRNet November 2 - 4, 2023 | GPCR Retreat- Registration Closed November 15 - 17, 2023 | MPGPCR Conference November 20 - 23, 2023 | ASCEPT Annual Scientific Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2

July 2022 " G.CLIPS biotech is 2 years old today🎂.

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

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

Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β -Arrestin Interaction The β 2-adrenergic receptor ( β 2AR) is a prototypical and extensively studied GPCR that can provide This single point mutation in extracellular loop 2 of the β 2AR is sufficient to intrinsically bias the the extracellular loops of the receptor and the extracellular pocket formed by transmembrane domains 2, Our studies reveal that F193 in extracellular loop 2 in the β2-adrenergic receptor mediates interactions

Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Options 📍  Boston, MA 📅 October 2 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November 5 - 7, 2024 | 16th Annual PEGS Europe   NEW November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 mechanism of some class B1 GPCR family members Structural basis of Frizzled 4 in recognition of Dishevelled 2

GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer March 2023. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. June 11-16, 2023. 19th World Congress of Basic & Clinical Pharmacology 2023. July 2 - 7. Metabolism and Pharmacokinetics PhD Opportunity - Investigation Of The Role Of The Formyl Peptide Receptor 2

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

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

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron We hypothesized that isoform 2 of rho-kinase (ROCK2), acting as downstream GPCRs, mediates adjustment ROCK activity assays were performed to evaluate the ability of various physiological GPCR ligands to stimulate physiological neuromodulator lysophosphatidic acid (LPA) through a mechanism entailing Gαi/o-protein stimulation two neurotransmitters, TRH, and 5-HT, which are both known to increase MN IME by TASK1 inhibition, stimulated

September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing Transfected HEK-293 cells were assessed for Ca2+o -stimulated Ca2+i mobilization using mutations in either the VFT domains and/or HH bundle intraloop-2 or intraloop-3. Finally, we observed that the Ca2+o -stimulated CaSR operated exclusively via signaling in-trans and We consider how receptor asymmetry may support the underlying mechanisms. © 2022 The Authors.

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle Prolonged vasoconstrictor GPCR signalling increases arterial contraction and stimulates signalling pathways In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs Furthermore, GRK2-knockdown ablated the sustained phase of endothelin-1 and angiotensin-II-stimulated Vasoconstrictor-stimulated phosphorylation of the Akt substrates GSK3α and GSK3β was ablated following

We investigated the feasibility of this lipophilic entry route for 2-iodomelatonin, a nonselective agonist calculations. 2-Iodomelatonin unbinding was investigated with steered molecular dynamics simulations unbinding it frequently assumes an open conformation in the MT1 but not in the MT2 receptor, favoring 2- Taken together, our simulations are consistent with the possibility that the gap between TM IV and V Our simulations also suggest that the open state of Tyr5.38 generates a small pocket on the surface of

October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. advanced NanoLuc/FlAsH-based biosensors reveals distinct conformational signatures of β-arrestin1 and 2